Information on EC 3.4.21.98 - hepacivirin

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The expected taxonomic range for this enzyme is: Flaviviridae

EC NUMBER
COMMENTARY
3.4.21.98
-
RECOMMENDED NAME
GeneOntology No.
hepacivirin
-
REACTION
REACTION DIAGRAM
COMMENTARY
ORGANISM
UNIPROT ACCESSION NO.
LITERATURE
Hydrolysis of four peptide bonds in the viral precursor polyprotein, commonly with Asp or Glu in the P6 position, Cys or Thr in P1 and Ser or Ala in P1'
show the reaction diagram
-
-
-
-
REACTION TYPE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
hydrolysis of peptide bond
-
-
-
-
SYNONYMS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
Cpro-2
-
-
-
-
Cpro-2 proteinase
-
-
-
-
Den2 protease
-
-
-
-
HCV NS3 protease
-
-
-
-
HCV NS3/4A
-
-
Hepacivirin
-
-
-
-
hepatitis C virus NS3 serine protease
-
-
-
-
non-structural 3 protein
-
-
non-structural protein 3 serine protease
-
-
nonstructural 3 protease
-
-
nonstructural protein 3
-
-
NS2/3 protease
O92972
-
NS2B-NS3 proteinase
-
-
-
-
NS2B/NS3 protease
-
-
NS2B/NS3 protease
-
-
NS2B/NS3 protease
-
-
NS3
-
-
-
-
NS3
O92972
-
NS3 protease
-
-
-
-
NS3 protease
-
-
NS3 protease
-
-
NS3 protease
O92972
-
NS3 protease
Hepatitis C virus J
-
-
-
NS3 protease
-
-
NS3 protease
-
-
NS3 protease
-
-
NS3 proteinase
-
-
-
-
NS3 serine protease
-
-
-
-
NS3 serine protease
-
-
NS3 serine protease
-
-
NS3 serine proteinase
-
-
-
-
NS3 serine proteinase
-
-
NS3 serine proteinase
-
-
NS3-4A protease
-
-
NS3-4A serine protease
Hepatitis C virus H
-
-
-
NS3-4A serine protease complex
-
-
-
-
NS3-4A serine proteinase
-
-
NS3-NS4A protease
-
-
-
-
NS3-NS4A protease
-
-
NS3-protease
A6N6Q4, A6N6T5
-
NS3/4A protease
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
-
NS3/4A serine protease
-
-
NS5A-5B protease
-
-
-
-
P70
-
-
-
-
polyprotein-processing proteinase NS3
-
-
-
-
proteinase NS3
-
-
-
-
proteinase, polyprotein-processing, NS3
-
-
-
-
sc-protease
-
single-chain NS3 protease domain
sc-protease
Hepatitis C virus J
-
single-chain NS3 protease domain
-
serine protease NS3
-
-
serine proteinase NS3
-
-
-
-
CAS REGISTRY NUMBER
COMMENTARY
149885-80-3
-
ORGANISM
COMMENTARY
LITERATURE
SEQUENCE CODE
SEQUENCE DB
SOURCE
proteases from all four serotypes
-
-
Manually annotated by BRENDA team
; type 1b
-
-
Manually annotated by BRENDA team
expression in human osteosarcoma cells
-
-
Manually annotated by BRENDA team
genotype 1a, 1b, and 3a
-
-
Manually annotated by BRENDA team
genotype 1b
-
-
Manually annotated by BRENDA team
genotypes 1a, 1b, and 3a
-
-
Manually annotated by BRENDA team
genotypes 1b
-
-
Manually annotated by BRENDA team
genotypes 1b, 2a, 4a, 5a, and 6a
-
-
Manually annotated by BRENDA team
strain H
-
-
Manually annotated by BRENDA team
strain J
-
-
Manually annotated by BRENDA team
Hepatitis C virus H
strain H
-
-
Manually annotated by BRENDA team
Hepatitis C virus J
strain J
-
-
Manually annotated by BRENDA team
recombinant protein consisting of a 40-residue component of cofactor NS2B tethered via a noncleavable nonapeptide to the N-terminal 184 residues of enzyme
-
-
Manually annotated by BRENDA team
recombinantenzyme
-
-
Manually annotated by BRENDA team
GENERAL INFORMATION
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
physiological function
-
the impact of NS3/4A protease activity and quasispecies complexity on virus clearance after IFN-based therapy is examined in HCV-HIV-1-coinfected patients: NS3/4A protease efficiency in cleaving caspase recruitment domain adaptor-inducing IFN-beta (Cardif) may be associated with the pegIFN-RBV treatment response
SUBSTRATE
PRODUCT                      
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
2-Naph-3Pya-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
2-Naph-Cit-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
2-Naph-Cit-Orn-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
2-Naph-hArg-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
2-Naph-Lys-AcLys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
2-Naph-Lys-Arg-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
2-Naph-Lys-Cit-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
2-Naph-Lys-hArg-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
2-Naph-Lys-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
2-Naph-Lys-Orn-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
2-Naph-Orn-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
2-Naph-Orn-Orn-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
4-(4-dimethylaminophenylazo)benzoyl-DEMEECASHE-5-(2-aminoethylamino)-1-sulfonic acid + H2O
4-(4-dimethylaminophenylazo)benzoyl-DEMEEC + ASHE-5-(2-aminoethylamino)-1-sulfonic acid
show the reaction diagram
-
-
-
?
7-methoxycoumarin-4-acetyl-DEMEECASHLPYK-(epsilon-NHCOCH3) + H2O
7-methoxycoumarin-4-acetyl-DEMEEC + ASHLPYK-(epsilon-NHCOCH3)
show the reaction diagram
-
-
-
?
7-methoxycoumarin-4-acetyl-EDASTPCSGSN-(4-nitro)Phe + H2O
7-methoxycoumarin-4-acetyl-EDASTPC + SGSN-(4-nitro)Phe
show the reaction diagram
-
-
-
?
9-fluorenylmethyloxycarbonyl-YQEFDEMEECASHLPYIEQG + H2O
9-fluorenylmethyloxycarbonyl-YQEFDEMEEC + ASHLPYIEQG
show the reaction diagram
-
-
-
?
Abz-AAGRK-SLTLnY-amide + H2O
Abz-AAGRK + SLTLnY-amide
show the reaction diagram
-
-
-
-
?
Abz-AGRK-SLTnY-amide + H2O
Abz-AGRK + SLTnY-amid
show the reaction diagram
-
-
-
-
?
Abz-AGRK-SnY-amide + H2O
Abz-AGRK + Ser-(3-nitro)Tyr-amide
show the reaction diagram
-
-
-
-
?
Abz-AGRKGTGNnY-amide + H2O
Abz-AGRK + GTGNnY-amide
show the reaction diagram
-
-
-
-
?
Abz-ARRK-SLTLnY-amide + H2O
Abz-ARRK + SLTLnY-amide
show the reaction diagram
-
-
-
-
?
Abz-FAAGRK-SLTLnY-amide + H2O
Abz-FAAGRK + SLTLnY-amide
show the reaction diagram
-
-
-
-
?
Abz-GRK-SLTLnY-amide + H2O
Abz-GRK + SLTLnY-amide
show the reaction diagram
-
-
-
-
?
Abz-GRK-SnY-amide + H2O
Abz-GRK + Ser-(3-nitro)Tyr-amide
show the reaction diagram
-
-
-
-
?
Abz-KKQR-AGVLnY-amide + H2O
Abz-KKQR + AGVLnY-amide
show the reaction diagram
-
high degree of cleavage efficiency, based on the NS2B/NS3 polyprotein cleavage site
-
-
?
Abz-KKQR-SAGMnY-amide + H2O
Abz-KKQR + SAGMnY-amide
show the reaction diagram
-
-
-
-
?
Abz-NRRRR-SAGMnYamide + H2O
?
show the reaction diagram
-
-
-
-
?
Abz-RK-SLTLnY-amide + H2O
Abz-RK + SLTLnY-amide
show the reaction diagram
-
-
-
-
?
Abz-RK-SnY-amide + H2O
Abz-RK + SnY-amide
show the reaction diagram
-
-
-
-
?
Abz-RRRR-nY-amide + H2O
Abz-RRRR + 3-nitro-L-tyrosine amide
show the reaction diagram
-
-
-
-
?
Abz-RRRR-SAGMnY-amide + H2O
Abz-RRRR + SAGMnY-amide
show the reaction diagram
-
-
-
-
?
Abz-RRRR-SAGnY-amide + H2O
Abz-RRRR + SAGnY-amide
show the reaction diagram
-
efficient substrate of the NS3 protease, based on the Dengue virus capsid protein processing site
-
-
?
Abz-RRRR-SLTLnY-amide + H2O
Abz-RRRR + SLTLnY-amide
show the reaction diagram
-
-
-
-
?
Abz-RRRR-SnY-amide + H2O
Abz-RRRR + Ser-(3-nitro)Tyr-amide
show the reaction diagram
-
-
-
-
?
Abz-SKKR-AGVLnY-amide + H2O
Abz-SKKR + AGVLnY-amide
show the reaction diagram
-
-
-
-
?
Abz-SKKR-SAGMnY-amide + H2O
Abz-SKKR + SAGMnY-amide
show the reaction diagram
-
-
-
-
?
Ac-Aib-Lys-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Aoc-Lys-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Asp-Glu-Asp(EDANS)-Glu-Glu-Abu-psi-(COO)Ala-Ser-Lys(DABCYL)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Asp-Glu-Asp(EDANS)-Glu-Glu-Abu-psi-[COO]Ala-Ser-Lys(DABCYL)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Asp-Glu-Asp(EDANS)-Glu-Glu-Abu-PSI[COO]Ala-Ser-Lys(DABCYL) + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Asp-Glu-Glu(EDANS)-Glu-Glu-AlgPSI[COO]-Ala-Ser-Lys(DABCYL)-amide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide + H2O
?
show the reaction diagram
-
efficient substrate for the protease
-
-
?
Ac-Cha-Lys-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Chg-Lys-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-DED-(EDANS)-EEAbupsi[COO]ASK(Dabcyl)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-DEEMECASHLPYK-NH2 + H2O
Ac-DEEMEC + ASHLPYK-NH2
show the reaction diagram
-
-
-
?
Ac-DPNRKR-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-DTEDVVP(Nva)-O-4-PAP + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester + H2O
?
show the reaction diagram
P27958
-
-
-
?
Ac-EMEECASHLP + H2O
Ac-EMEEC + ASHLP
show the reaction diagram
-
-
-
?
Ac-FASGKR-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-KPGLKR-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Leu-3Pya-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Leu-4Pya-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Leu-aPhe-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Leu-Cit-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Leu-hArg-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Leu-Lys-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Leu-nPhe-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Leu-Orn-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-LQYTKR-4-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Nle-Lys-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Nva-Lys-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Tbg-Lys-Lys-Arg-p-nitroanilide + H2O
?
show the reaction diagram
-
-
-
-
?
Ac-Thr-Arg-Arg-7-amido-4-methylcoumarin + H2O
Ac-Thr-Arg-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Ac-YQEFDEMEECAS + H2O
Ac-YQEFDEMEEC + AS
show the reaction diagram
-
-
-
?
Ac-YQEFDEMEECASH + H2O
Ac-YQEFDEMEEC + ASH
show the reaction diagram
-
-
-
?
Ac-YQEFDEMEECASHL + H2O
Ac-YQEFDEMEEC + ASHL
show the reaction diagram
-
-
-
?
Ac-YQEFDEMEECASHLP + H2O
Ac-YQEFDEMEEC + ASHLP
show the reaction diagram
-
-
-
?
acetyl-Asp-Glu-Asp-(5-[(2'-aminoethyl)-amino]naphthalenesulfonic acid)-Glu-Glu-(alpha-aminobutyryl)PSI[COO]Ala-Ser-Lys-(4-[[4'-(dimethylamino)phenyl]azo]-benzoic acid)-NH2 + H2O
?
show the reaction diagram
-
-
-
?
acetyl-DED(EDANS)EEalpha-aminobutyryl-psi(COO)ASK(DABCYL)-NH2 + H2O
?
show the reaction diagram
Hepatitis C virus, Hepatitis C virus H
-
-
-
-
?
acetyl-DEMEECASHLPYL-(epsilon-NHCOCH3) + H2O
acetyl-DEMEEC + ASHLPYL-(epsilon-NHCOCH3)
show the reaction diagram
-
-
-
?
acetyl-DTEDVVCCSMSYTWTGK + H2O
?
show the reaction diagram
-
-
-
-
?
acetyl-DTEDVVP-norvaline-O-4-phenylazophenol + H2O
?
show the reaction diagram
-
-
-
?
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH + H2O
?
show the reaction diagram
-
-
-
-
?
anthranilyl-DDIVPAbu[C(O)-O]AMY(3-NO2)TW-OH + H2O
?
show the reaction diagram
Hepatitis C virus, Hepatitis C virus J
-
-
-
-
?
Boc-Gly-Arg-Arg-7-amido-4-methylcoumarin + H2O
Boc-Gly-Arg-Arg + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Boc-Gly-Arg-Arg-AMC + H2O
?
show the reaction diagram
-
-
-
-
?
Boc-Gly-L-Arg-L-Arg-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Boc-GRR-7-amido-4-methylcoumarin + H2O
Boc-GRR + 7-amino-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Boc-RVRR-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Bz-nKRR-7-amido-3-carbamoylmethyl-4-methylcoumarin + H2O
Bz-nKRR + 7-amino-3-carbamoylmethyl-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Bz-nKRR-7-amino-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
Bz-nKTR-7-amido-3-carbamoylmethyl-4-methylcoumarin + H2O
Bz-nKTR + 7-amino-3-carbamoylmethyl-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Bz-Nle-Lys-Arg-Arg-AMC + H2O
?
show the reaction diagram
-
-
-
-
?
Bz-nTRR-7-amido-3-carbamoylmethyl-4-methylcoumarin + H2O
Bz-nTRR + 7-amino-3-carbamoylmethyl-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Bz-TKRR-7-amido-3-carbamoylmethyl-4-methylcoumarin + H2O
Bz-TKRR + 7-amino-3-carbamoylmethyl-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
Bz-TTRR-7-amido-3-carbamoylmethyl-4-methylcoumarin + H2O
Bz-TTRR + 7-amino-3-carbamoylmethyl-4-methylcoumarin
show the reaction diagram
-
-
-
-
?
CARDIF + H2O
?
show the reaction diagram
-
-
-
-
?
CARDIF + H2O
?
show the reaction diagram
-
NS3-4A cleaves Cardif (adaptor protein of retinoic acid-inducible gene I or melanoma differentiation-associated gene-5), resulting in an interruption of the Cardif-mediated pathway in non-neoplastic human hepatocyte PH5CH8 cells
-
-
?
CARDIF + H2O
?
show the reaction diagram
-
NS3-4A cleaves Cardif (CARD adaptor-inducing) by generating a 70 kDa fragment. NS3-4A-mediated cleavage, is not caspase-dependent. Cardif mutant C508A is resistant to NS3-4A-mediated cleavage
-
-
?
caspase recruitment domain adaptor-inducing IFN-beta (Cardif) + H2O
?
show the reaction diagram
-
-
-
-
?
CD8-1 + H2O
?
show the reaction diagram
-
synthetic substrate consisting of lymphocyte surface antigen CD8alpha, an enzyme cleavage site and a membrane anchor featuring an endoplasmic reticulum retention sequence
-
-
?
DCSTPCSGSW-NH2 + H2O
DCSTPC + SGSW-NH2
show the reaction diagram
-
-
-
?
DDICPCSMSYTW-OH + H2O
DDICPC + SMSYTW-OH
show the reaction diagram
-
-
-
?
DEMEECASHLPYK + H2O
DEMEEC + ASHLPYK
show the reaction diagram
-
-
-
?
DEMEECSQHLPYI + H2O
DEMEEC + SQHLPYI
show the reaction diagram
-
-
-
?
DTEDVVCCSMSYTWTGK + H2O
DTEDVVCC + SMSYTWTGK
show the reaction diagram
-
-
-
?
EAGDDIVPCSMSYTWTGA-OH + H2O
EAGDDIVPC + SMSYTWTGA-OH
show the reaction diagram
-
-
-
?
EAGDNIVPCSMSYTWTGA-OH + H2O
EAGDNIVPC + SMSYTWTGA-OH
show the reaction diagram
-
-
-
?
EAGNDIVPCSMSYTWTGA-OH + H2O
EAGNDIVPC + SMSYTWTGA-OH
show the reaction diagram
-
-
-
?
EAGNNIVPCSMSYTWTGA-OH + H2O
EAGNNIVPC + SMSYTWTGA-OH
show the reaction diagram
-
-
-
?
ECTTPCSGSWIRD + H2O
ECTTPC + SGSWIRD
show the reaction diagram
-
-
-
?
EDVV-4-aminobutyric acid-CSMSY-NH2 + H2O
EDVV-4-aminobutyric acid-C + SMSY-NH2
show the reaction diagram
-
-
-
?
EDVV-4-aminobutyryl-CSMSY + H2O
EDVV-4-aminobutyryl-C + SMSY
show the reaction diagram
-
-
-
?
EDVV-4-aminobutyryl-CSMSY + H2O
EDVV-4-aminobutyryl-C + SMSY
show the reaction diagram
Hepatitis C virus, Hepatitis C virus H
-
-
-
-
?
EDVV-Abu-CSMSY + H2O
?
show the reaction diagram
-
-
-
-
?
EDVVPCSMSYN + H2O
?
show the reaction diagram
O92972
-
-
-
?
Glu-Asp-Val-Val-4-aminobutyryl-Cys-p-nitroanilide + H2O
Glu-Asp-Val-Val-4-aminobutyryl-Cys + 4-nitroaniline
show the reaction diagram
-
-
-
?
hepatitis C virus polyprotein + H2O
?
show the reaction diagram
-
mutational cleavage
-
?
hepatitis C virus polyprotein + H2O
?
show the reaction diagram
-
the enzyme is essential for processing of viral polyprotein
-
?
hepatitis virus C polyprotein + H2O
?
show the reaction diagram
-
maturation of the viral polyprotein
-
-
-
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
123% catalytic efficiency
-
-
?
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
165% catalytic efficiency
-
-
?
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
23.5% catalytic efficiency
-
-
?
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
38.4% catalytic efficiency
-
-
?
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
39.1% catalytic efficiency
-
-
?
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
53.2% catalytic efficiency
-
-
?
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
58.8% catalytic efficiency
-
-
?
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
68.4% catalytic efficiency
-
-
?
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
70.6% catalytic efficiency
-
-
?
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
72.6% catalytic efficiency
-
-
?
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
73.9% catalytic efficiency
-
-
?
Hepatitis virus C polyprotein NS5A/NS5B + H2O
?
show the reaction diagram
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
86.5% catalytic efficiency
-
-
?
interferon promoter stimulator-1 + H2O
?
show the reaction diagram
-
protease domain of NS3-4A is sufficient for targeting and cleavage. Targeted cleavage inhibits downstream signaling to interferon regulatory factor-3 and nuclear factor kappaB
-
-
?
MAVS/IPS-1 + H2O
?
show the reaction diagram
-
-
-
-
?
myelin basic protein + H2O
?
show the reaction diagram
-
-
-
-
?
non-structural protein NS5B of hepatitis C virus + H2O
? + DDIVPC-OH
show the reaction diagram
-
-
-
-
?
non-structural protein NS5B of hepatitis C virus + H2O
? + DDIVPC-OH
show the reaction diagram
-
-
N-terminal hexapeptide
?
NS5A/5B + H2O
?
show the reaction diagram
-
-
-
-
?
NS5A/B polyprotein + H2O
?
show the reaction diagram
-
-
-
-
?
NS5AB polyprotein + H2O
?
show the reaction diagram
-
-
-
-
?
o-aminobenzoyl (Abz)-L-Asp-L-Asp-L-Ile-L-Val-L-Pro-L-Cys-L-Ser-L-Met-L-Ser-L-Tyr(3-NO2)-L-Thr-NH2 + H2O
?
show the reaction diagram
-
i.e. IQGS-1, internally quenched fluorogenic substrate
-
-
?
precursor polyprotein of hepatitis C virus + H2O
?
show the reaction diagram
-
-
-
-
?
Pyr-RTKR-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
RetS1 peptide substrate + H2O
?
show the reaction diagram
-
-
-
-
?
SEAP-1 + H2O
?
show the reaction diagram
-
synthetic substrate consisting of alkaline phosphatase, an enzyme cleavage site and a membrane anchor featuring an endoplasmic reticulum retention sequence
-
-
?
succinyl-DEMEECASHPYPY-NH2 + H2O
succinyl-DEMEEC + ASHPYPY-NH2
show the reaction diagram
-
-
-
?
succinyl-EDVVPCSMYSTW-NH2 + H2O
?
show the reaction diagram
-
-
-
-
?
TRIF + H2O
?
show the reaction diagram
-
-
-
-
?
viral polyprotein + H2O
?
show the reaction diagram
-
-
-
?
viral polyprotein + H2O
?
show the reaction diagram
-
proteolytic cleavage at the four junctions NS3/NS4A, NS5A/NS5B, NS4A/NS4B and NS4B/NS5A. NS3-dependent cleavage sites of the polyprotein have the consensus sequence Asp/Glu-(Xaa)4-Cys/Thr-Ser/Ala-(Xaa)2-Leu/Trp/Tyr, with the most efficient cleavage occurring after cysteine
-
-
?
Z-RR-7-amido-4-methylcoumarin + H2O
?
show the reaction diagram
-
-
-
-
?
mitochondrial antiviral signaling protein + H2O
?
show the reaction diagram
-
i.e. MAVS, cleavage at Cys-508
-
-
?
additional information
?
-
-
decameric peptide spanning from P6-P4' required as a minimum
-
-
-
additional information
?
-
-
ATPase activity
-
-
-
additional information
?
-
-
cleavage pattern for structural and non-structural proteins of hepatitis C virus
-
-
-
additional information
?
-
-
enzyme shows strong preference for basic amino acid resiudues at the P1 position, preferences for the R2-4 positions are in the decreasing orders of Arg, Thr, Gln/Asn/Lys for P2, Lys, Arg, Asn for P3, and Nle, Leu, Lys, Xaa for P4. Prime site substrate specificity is for small and polar amino acid residues in P1 and P3. P2 and P4 positions show minimal activty. Analysis of ground state binding and influence of P4 position for transition state through single substrate kinetics
-
-
-
additional information
?
-
-
no substrate: Boc-AGPR-AMC, Boc-QAR-AMC, Boc-O-benzyl-EGR-pNA
-
-
-
additional information
?
-
-
substrate P1 R residue strongly interacts with S1 residues D129, Y150, and S163. P2 K residue makes an essential interaction with N152 at S2
-
-
-
additional information
?
-
-
chimeric form of the Gal4VP16 transcription factor is activated in the presence of the hepatitis C virus NS3/4A protease to induce different reporter genes (choramphenical acetyltransferase, green fluorescent protein and the cell-surface marker H-2Kk) through the (Gal4)5-E1b promoter. NS5A/5B trans-cleavage motif of hepatitis C virus of genotype 1a inserted between Gal4VP16 and the N terminus of the endoplasmic reticulum-resident protein PERK is cleaved specifically by NS3/4A
-
-
-
additional information
?
-
-
enzyme's requirement of peptide substrates of 10 amino acids in length, spanning from P6 to P4'
-
-
-
additional information
?
-
-
no activity with 2-Naph-Lys-aPhe-Arg-p-nitroanilide, 2-Naph-Lys-nLeu-Arg-p-nitroanilide and 2-Naph-Lys-Phe-Arg-p-nitroanilide
-
-
-
additional information
?
-
O92972
NS2/3 precursor is able to auto-cleave
-
-
-
additional information
?
-
-
preferred substrate size for the Dengue virus NS3 protease encompasses the residues from P4 to P3'. Serine is the preferred P1' residue
-
-
-
additional information
?
-
-
NS3-4A lacks the ability to cleave endogenous TRIF, regardless of HCV strains derived from patients with different stages of hepatic disease. Inflammatory cytokine production by NF-kappaB activation via the TRIF-mediated pathway also remains unsuppressed by NS3-4A
-
-
-
additional information
?
-
-
NS3 needs NS4a as a cofactor
-
-
-
additional information
?
-
-
NS3/4A protease is responsible for cleaving the viral polyprotein at junctions 3-4A, 4A4B, 4B5A, and 5A5B and two host cell adaptor proteins of the innate immune response, TRIF and MAVS
-
-
-
additional information
?
-
-
comparison of the cleavage efficiencies of all known HCV NS3-4A cleavage sequences in a cell-based system is reported. NS4B/NS5A and NS5A/NS5B are both processed efficiently in trans, in contrast to NS3/NS4A and NS4A/NS4B, which are not processed significantly above background. ER-anchoring of the substrate is critical for its cleavage by NS3-4A. Other HCV proteins or replicase components do not change NS3-4A substrate selectivity or activity
-
-
-
NATURAL SUBSTRATES
NATURAL PRODUCTS
REACTION DIAGRAM
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
(Substrate)
LITERATURE
(Substrate)
COMMENTARY
(Product)
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
CARDIF + H2O
?
show the reaction diagram
-
NS3-4A cleaves Cardif (adaptor protein of retinoic acid-inducible gene I or melanoma differentiation-associated gene-5), resulting in an interruption of the Cardif-mediated pathway in non-neoplastic human hepatocyte PH5CH8 cells
-
-
?
CARDIF + H2O
?
show the reaction diagram
-
NS3-4A cleaves Cardif (CARD adaptor-inducing) by generating a 70 kDa fragment. NS3-4A-mediated cleavage, is not caspase-dependent. Cardif mutant C508A is resistant to NS3-4A-mediated cleavage
-
-
?
caspase recruitment domain adaptor-inducing IFN-beta (Cardif) + H2O
?
show the reaction diagram
-
-
-
-
?
hepatitis C virus polyprotein + H2O
?
show the reaction diagram
-
mutational cleavage
-
?
hepatitis C virus polyprotein + H2O
?
show the reaction diagram
-
the enzyme is essential for processing of viral polyprotein
-
?
hepatitis virus C polyprotein + H2O
?
show the reaction diagram
-
maturation of the viral polyprotein
-
-
-
mitochondrial antiviral signaling protein + H2O
?
show the reaction diagram
-
i.e. MAVS, cleavage at Cys-508
-
-
?
additional information
?
-
-
NS3-4A lacks the ability to cleave endogenous TRIF, regardless of HCV strains derived from patients with different stages of hepatic disease. Inflammatory cytokine production by NF-kappaB activation via the TRIF-mediated pathway also remains unsuppressed by NS3-4A
-
-
-
additional information
?
-
-
NS3/4A protease is responsible for cleaving the viral polyprotein at junctions 3-4A, 4A4B, 4B5A, and 5A5B and two host cell adaptor proteins of the innate immune response, TRIF and MAVS
-
-
-
COFACTOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
KKGSVVIVGRIVLSCK
-
-
KKGSVVIVGRIVLSGK
-
NS4A cofactor
KKGSVVIVGRIVLSGK
-
cofactor peptide KK4A
KKGSVVIVGRIVLSGK
-
-
KKGSVVIVGRIVLSGKPAIIPKK
-
NS-4A cofactor
additional information
-
NS4 required
-
additional information
-
solution structure and dynamics of the single-chain hepatitis C virus NS3 protease NS4A cofactor complex. The NS4A-bound NS3 protease is in slow conformation exchange with the NS4A-free conformation
-
additional information
-
NS2B required
-
additional information
-
requires the noncovalently-associated viral protein NS4A for optimal catalytic activity. NS4A increases the enzymatic activity of NS3 by stabilizing the N-terminal domain of the protease, by optimizing the orientation of the residues of the catalytic triad and by contributing to the formation of the substrate recognition site
-
additional information
-
NS4A cofactor peptide
-
additional information
-
NS4A cofactor, KKGSVVIVGRIVLSGK
-
additional information
-
NS-4A cofactor
-
additional information
-
cofactor NS2B strongly influences the preference of flavivirus proteases for lysine or arginine at P2 in substrates
-
additional information
-
efficient NS3-4A proteolytic activity requires the protease domain and its NS4A cofactor but does not require the NS3 helicase domain
-
additional information
-
full NS3 protease activity requires association with NS4A
-
additional information
-
NS2B domain important in substrate-based inhibitor binding
-
additional information
A8DX91, A8DXI7, A8DXT5, B0L492, B0L493, B0L494, B0L495, B0L496, B0L497, Q8JRC7
enhancement of NS3 catalytic efficiency by the NS4A cofactor depends on a few specific amino acid residues; enhancement of NS3 catalytic efficiency by the NS4A cofactor depends on a few specific amino acid residues; enhancement of NS3 catalytic efficiency by the NS4A cofactor depends on a few specific amino acid residues; enhancement of NS3 catalytic efficiency by the NS4A cofactor depends on a few specific amino acid residues; enhancement of NS3 catalytic efficiency by the NS4A cofactor depends on a few specific amino acid residues; enhancement of NS3 catalytic efficiency by the NS4A cofactor depends on a few specific amino acid residues; enhancement of NS3 catalytic efficiency by the NS4A cofactor depends on a few specific amino acid residues; enhancement of NS3 catalytic efficiency by the NS4A cofactor depends on a few specific amino acid residues; enhancement of NS3 catalytic efficiency by the NS4A cofactor depends on a few specific amino acid residues; enhancement of NS3 catalytic efficiency by the NS4A cofactor depends on a few specific amino acid residues; enhancement of NS3 catalytic efficiency by the NS4A cofactor depends on a few specific amino acid residues
-
METALS and IONS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
Zinc
-
His149 may be an integral part of zinc coordination, may have a structural rather than a catalytic role, effects on protein folding or post-folding stability
Zn2+
O92972
both auto-cleavage and NS3 protease activity are zinc-dependent. NS2/3 auto-cleavage activity is more sensitive to zinc chelation by 1,10-phenanthroline than the NS3 protease activity
Zn2+
-
plays a critical role in maintaining structural stability and integrity of the protein
Zn2+
-
zinc-dependent serine protease. zinc ion is not involved in the catalytic mechanism but it is essential for the structural integrity of the protein. The global unfolding heat capacity is dominated by the zinc dissociation step, suggesting that the binding of zinc induces a significant structural rearrangement of the protein. Contrary to other homologous zinc-dependent proteases, the zinc-free NS3 protease is not completely unstructured
INHIBITORS
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(ethyl)phosphinic acid
-
-
((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(methyl)phosphinic acid
-
-
(-)-epicatechin-3-O-gallate
-
-
(-)-epigallocatechin-3-O-gallate
-
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclobutane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclohexane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopentane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopropane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
-
(10R,13R)-N-(1-[[(2-[[(1R)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10-cyclohexyl-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-oxo-2,7-dioxa-8-thia-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide 8,8-dioxide
-
-
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2,7-dioxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(methylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
(11R,14R)-N-(1-[[(2-[[(1R)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-cyclohexyl-9,12-dioxo-2-oxa-10,13-diazabicyclo[14.3.1]icosa-1(20),16,18-triene-14-carboxamide
-
-
(11S,14S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-cyclohexyl-9,12-dioxo-1,10,13,17-tetraazabicyclo[14.2.1]nonadeca-16(19),17-diene-14-carboxamide
-
-
(1R)-1-([(4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]heptanoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
50% inhibition at 0.0000004 mM, NMR and molecular dynamics analysis
(1R)-1-([(4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]heptanoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
-
(1R)-2-but-3-en-1-yl-1-[[(4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]hept-6-enoyl]-4-(quinolin-4-yloxy)-L-prolyl]amino]cyclopropanecarboxylic acid
-
-
(1R,12E,19S,22S)-19-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,17,20-trioxo-2,16-dioxa-4,18,21-triazatetracyclo[19.2.1.14,7.06,11]pentacosa-6,8,10,12-tetraene-22-carboxamide
-
-
(1R,12E,20S,23S)-20-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
-
(1R,12E,20S,23S)-20-cyclohexyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
-
(1R,12E,20S,23S)-20-cyclopentyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-4-methyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatricyclo[20.2.1.06,11]pentacosa-6,8,10,12-tetraene-23-carboxamide
-
-
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-(1-methylcyclohexyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
-
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-isopropyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
-
(1R,12E,21S,24S)-21-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10,12-tetraene-24-carboxamide
-
-
(1R,12E,22S,25S)-22-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,20,23-trioxo-2,19-dioxa-4,21,24-triazatetracyclo[22.2.1.14,7.06,11]octacosa-6,8,10,12-tetraene-25-carboxamide
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(1R,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
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(1R,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
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(1R,21S,24S)-21-(tert-butoxymethyl)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
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(1R,21S,24S)-21-cyclohexyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
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(1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
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(1R,21S,24S)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-21-(1-methylcyclohexyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
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(1R,2S)-1-[([(1R,2R,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopentyl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[[(1R,2R,4S)-2-((S)-1-cyclopentylcarbamoyl-2,2-dimethyl-propylcarbamoyl)-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
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(1R,2S)-1-[[(1R,2R,4S)-2-((S)-1-tert-butylcarbamoyl-2,2-dimethyl-propylcarbamoyl)-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
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(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyldimethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethylpropylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
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(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
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(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-methyl-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
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(1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl](methyl)carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylic acid
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(1R,5S)-3-(N-[[(1S)-1-cyclohexyl-2-cyclopropyl-2-oxoethyl]carbamoyl]-3-methyl-L-valyl)-N-[1-(cyclopropylamino)-1,2-dioxohept-6-yn-3-yl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1R,5S)-3-[2(S)-[[[[1-[(1-azetidinylsulfonyl)methyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]butyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-3-[2(S)-[[[[1-[[[cyclobutyl(methyl)amino]sulfonyl]methyl]cyclohexyl]amino] carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-[N-(tert-butylcarbamoyl)-3-methyl-L-valyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyll]-butyl]-3-[2(S)-[[[[1-[[(dimethylamino)sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[(2S)-2-[[[[1-[1(R)-[(dimethylamino)sulfonyl]ethyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyll-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[(2S)-[[[[1-[1(S)-[(dimethylamino)sulfonyl]ethyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyll-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-(2-cyclopropyl-1,1-dioxido-5(R)-isothiazolidinyl)cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[(2-fluoro-1,1-dimethylethyl)methylamino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[(cyclopropylmethyl)methylamino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[cyclopropyl(1-methylethyl)amino]-sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)amino]sulfonyl]-methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[ethyl(methyl)amino]sulfonyl]methyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[3,3-dimethyl-2(S)-[[[[1-[(4-morpholinylsulfonyl)-methyl]cyclohexyl]amino]carbonyl]amino]-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[3,3-dimethyl-2(S)-[[[[1-[[(methylamino)sulfonyl]-methyl]cyclohexyl]amino]carbonyl]amino]-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[3,3-dimethyl-2(S)-[[[[1-[[[methyl(1-me5thylethyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-pemtyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)amino]sulfonyl]-methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
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(1R,5S)-N-[3-(cyclopropylamino)-1(S)-(2-cyclopropylethyl)-2,3-dioxopropyl]-3-[2(S)-[[[[1-[[[cycloppropyl(methyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
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(1R,5S)-N-[3-(cyclopropylamino)-1(S)-(cyclopropylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
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(1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide
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Boceprevir: EC50 and EC90 values, determined in a bicistronic, subgenomic, cell-based replicon assay run over 72 h using Huh-7 hepatoma cells, are 200 and 400 nM, respectively. Preclinical, metabolism and pharmacokinetics data are very promising. Currently ongoing phase II clinical trials demonstrate the compound to be well tolerated
(1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl)octahydrocyclopenta[c]pyrrole-1-carboxamide
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(1S,5R)-6,6-dichloro-3-[cyclohexyl[[[(1,1-dimethylethyl)amino]carbonyl]amino]acetyl]-N-[1-[1,2-dioxo-2-(2-propenylamino)ethyl]butyl]-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide
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(1S,5R)-N-((S)-5-cyclopropyl-1-(cyclopropylamino)-1,2-dioxopentan-3-yl)-3-((S)-2-(3-(1-((N-cyclopropyl-N-methylsulfamoyl)methyl)cyclohexyl)ureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(1-amino-5,5-difluoro-1,2-dioxoheptan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(1-amino-5,5-difluoro-1,2-dioxohexan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(1-amino-6,6,6-trifluoro-1,2-dioxohexan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(1-amino-7,7,7-trifluoro-1,2-dioxoheptan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-((1s,3S)-3-hydroxycyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-(1-fluorocyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-(1-hydroxycyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-(2,2-difluorocyclopropyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-(3,3-difluorocyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(1S,5R)-N-(5-amino-1,1,1-trifluoro-4,5-dioxopentan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
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(2-(3-((12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo-(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid
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(2-(3-((12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo-(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
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(2-(3-((12-cyclohexyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,-13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
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(2-(3-((3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)henicosa-13(21),14,16(20)-triene-18-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid
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(2-(3-((3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)henicosa-13(21),14,16(20)-triene-18-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
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(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2,10-dioxa-13-azatricyclo[15.2.2.13,7]docosa-1(19),3(22),4,6,17,20-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
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(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[15.2.2.13,7]docosa-1(19),3(22),4,6,17,20-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
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(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[16.2.2.13,7]tricosa-1(20),3(23),4,6,18,21-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
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(2R)-2-(acetylamino)-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
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(2R)-2-[(tert-butoxycarbonyl)amino]-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-2-phenylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methyl-2-phenylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-2-(4-methoxyphenyl)-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(6-methylpyridin-2-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(pyridin-3-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(pyridin-4-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-2-[[2-(morpholin-4-yl)quinazolin-4-yl]oxy]-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
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(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-4,14-dioxo-2-[(2-phenylquinazolin-4-yl)oxy]-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2R,4S,7S,14Z)-7-tert-butyl-N-[(1R,2S)-1-[(cyclopropylsulfonyl)carbamoyl]-2-ethenylcyclopropyl]-6,9-dioxo-3,4,6,7,8,9,12,13-octahydro-2H,11H-16,18-etheno-2,5-methanopyrido[2,3-k][1,10,3,6]dioxadiazacyclononadecine-4-carboxamide
-
-
(2R,6R,12Z,13aR,14S,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14-carboxylic acid
-
-
(2R,6S,10E,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
50% inhibition at 0.000077 mM, NMR and molecular dynamics analysis
(2R,6S,10E,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,10E,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-5,16-dioxo-2-(quinolin-4-yloxy)-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,10Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14
-
-
-
(2R,6S,12Z,14aR,16aS)-2-[(8-chloro-2-ethoxyquinolin-4-yl)oxy]-6-[[(cyclopentyloxy)carbonyl]amino]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-([7-methoxy-2-[2-(methylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
50% inhibition at 0.000011 mM, NMR and molecular dynamics analysis
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxyquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[(4-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[2-(1H-imidazol-1-yl)-7-methoxyquinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(1H-pyrazol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(1H-pyrrol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(4-methyl-1H-pyrazol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(5-methyl-1,3,4-oxadiazol-2-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,12Z,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[(5-ethoxythieno[3,2-b]pyridin-7-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2R,6S,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxohexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
50% inhibition at 0.000027 mM, NMR and molecular dynamics analysis
(2R,6S,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxohexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(2S)-([N-[3-([[(10S,13S)-10-cyclohexyl-8,11-dioxo-2,7-dioxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-trien-13-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
(2S)-([N-[3-([[(3S,18S)-18-cyclohexyl-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinolin-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
(2S)-([N-[3-([[(3S,6S)-6-cyclohexyl-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-trien-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
(2S)-([N-[3-([[(7R,9S,12S)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
(2S)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[17.2.2.13,7]tetracosa-1(21),3(24),4,6,19,22-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
(2S)-2-[(tert-butoxycarbonyl)amino]-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
-
-
(2S)-2-[([(1R,4R)-2-[[(1R)-1-[[(1R)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]butanoic acid
-
-
(2S)-2-[[(2-[[(1S)-1-(methoxycarbonyl)-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
(2S)-[([[3-([[(6S,8S,9R,10S,13S)-13-cyclohexyl-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-trien-10-yl]carbonyl]amino)-2-oxohexanoyl]amino]acetyl)amino](phenyl)ethanoic acid
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-([7-methoxy-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinazolin-4-yl]oxy)-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(3-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxyquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-2-[[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]oxy]-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-4,14-dioxo-2-([2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinazolin-4-yl]oxy)-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
-
(2S,3aR,11Z,12aS,13aR,15aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methyl-2-phenylquinazolin-4-yl)oxy]-4,15-dioxo-1,2,3,3a,4,5,6,7,8,9,10,12a,13,14,15,15a-hexadecahydro-13aH-cyclopenta[c]cyclopropa[g][1,6]diazacyclopentadecine-13a-carboxamide
-
-
(2S,3aR,11Z,12aS,13aR,15aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-4,15-dioxo-1,2,3,3a,4,5,6,7,8,9,10,12a,13,14,15,15a-hexadecahydro-13aH-cyclopenta[c]cyclopropa[g][1,6]diazacyclopentadecine-13a-carboxamide
-
-
(2S,4S)-1-((S)-2-((R)-2-cyclohexyl-2-(prop-1-en-2-ylamino)acetamido)-3,3-dimethylbutanoyl)-N-((1S,2R)-1-(cyclopropylsulfonylcarbamoyl)-2-vinylcyclopropyl)-4-phenylpyrrolidine-2-carboxamide
-
-
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,15-trioxo-1,4,10-triazacyclopentadecane-5-carboxamide
-
-
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,16-trioxo-1,4,10-triazacyclohexadecane-5-carboxamide
-
-
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,17-trioxo-1,4,10-triazacycloheptadecane-5-carboxamide
-
-
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,18-trioxo-1,4,10-triazacyclooctadecane-5-carboxamide
-
-
(2S,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
(3R)-2-[2-[(tert-butylcarbamoyl)amino]-3,3-dimethylbutanoyl]-N-[1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
comparison of binding affinity with human neutrophil elastase, selectivity of 420
(3R)-2-[2-[(tert-butylcarbamoyl)amino]-3,3-dimethylbutanoyl]-N-[1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
comparison of binding affinity with human neutrophil elastase, selectivity of 35
(3R)-2-[[(tert-butylcarbamoyl)amino](cyclohexyl)acetyl]-N-[1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
-
(3R)-2-[[(tert-butylcarbamoyl)amino](cyclohexyl)acetyl]-N-[1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
-
(3R,12S,16R,17aS)-12-[(tert-butoxycarbonyl)amino]-16-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-1,13-dioxohexadecahydro-1H-pyrrolo[1,2-a][1,4]diazacyclopentadecine-3-carboxylic acid
-
-
(3S)-3-[(7R,9S,12R)-9-[(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-12-yl]cyclohexanecarboxylic acid
-
-
(3S,12S,16R,17aS)-12-[(tert-butoxycarbonyl)amino]-16-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-1,13-dioxohexadecahydro-1H-pyrrolo[1,2-a][1,4]diazacyclopentadecine-3-carboxylic acid
-
-
(3S,18S)-18-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinoline-3-carboxamide
-
-
(3S,6S)-6-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-triene-3-carboxamide
-
-
(4-acetylphenoxy)acetic acid
-
-
(4-aminophenyl)(2-aminopyridin-3-yl)methanone
-
-
(4-aminophenyl)(phenyl)methanone
-
-
(4-methoxyphenyl)(1H-pyrrol-2-yl)methanone
-
-
(4R)-4-[[(2S)-2-(acetylamino)-3-carboxypropanoyl]amino]-5-[(1-[[(1R)-1-([(2S,4R)-4-(benzyloxy)-2-[(2-[[(1S)-1-phenylethyl]carbamoyl]-2-propylhydrazino)carbonyl]pyrrolidin-1-yl]carbonyl)-2-methylpropyl]carbamoyl]-2-methylbutyl)amino]-5-oxopentanoic acid
-
noncovalent binding to enzyme active site, 50% inhibition at 0.000078 mM
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[16.6.2.14,7.022,26]heptacosa-16,18(26),19,21-tetraene-6-carboxamide
-
-
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[20.3.1.14,7.018,23]heptacosa-16,18,20,22-tetraene-6-carboxamide
-
-
(4S,7S,9R)-4-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2,5-dioxo-10,15-dioxa-3,6-diazatricyclo[14.3.1.16,9]henicosa-1(20),16,18-triene-7-carboxamide
-
-
(5R,7S,10S)-10-cyclopentyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo(prop-2-en-1-ylamino)acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo[(1-phenylethyl)amino]acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
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-
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo[(pyridin-2-ylmethyl)amino]acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclobutylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopentylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-1,6,7,9,10,11,12,14,15,16,17,18-dodecahydro-5H-2,22:5,8-dimethano-4,13,2,8,11-benzodioxatriazacycloicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[[(1-methylpropyl)amino](oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,7S,10S)-N-[(1S)-1-[(benzylamino)(oxo)acetyl]butyl]-10-tert-butyl-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
(5R,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-methyl-3,6-dioxo-11,15-dioxa-2,4,7-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
(5R,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-11,15-dioxa-2,4,7-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
(5R,8S,10R)-5-tert-butyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-2,11,15-trioxa-4,7-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
(5S,8S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5-cyclohexyl-3,6,14-trioxo-4,7,13-triazabicyclo[14.2.2]icosa-1(18),16,19-triene-8-carboxamide
-
-
(5S,8S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5-cyclohexyl-3,6,14-trioxo-4,7,13-triazabicyclo[14.3.1]icosa-1(20),16,18-triene-8-carboxamide
-
-
(5S,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-11,16-dioxa-4,7-diazatricyclo[15.3.1.17,10]docosa-1(21),17,19-triene-8-carboxamide
-
-
(6R,8S,11R)-11-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[14.3.1.16,9]henicosa-1(20),16,18-triene-8-carboxamide
-
-
(6R,8S,11S)-11-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[13.3.1.16,9]icosa-1(19),15,17-triene-8-carboxamide
-
-
(6R,8S,11S,18E)-11-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3-methyl-4,10,13-trioxo-5,14-dioxa-3,9,12-triazatricyclo[18.3.1.16,9]pentacosa-1(24),18,20,22-tetraene-8-carboxamide
-
-
(6S,11S,20S)-11-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[13.3.1.16,9]icosa-1(19),15,17-triene-20-carboxamide
-
-
(6S,8S,9R,10S,13S)-13-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-triene-10-carboxamide
-
-
(7R,9S)-12-(2,3-dihydro-1H-inden-1-yl)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-15-methyl-11,14-dioxo-2,6-dioxa-10,13,15-triazatricyclo[15.3.1.17,10]docosa-1(21),17,19-triene-9-carboxamide
-
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-18-methoxy-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-18-methyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-19-methyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2-oxa-6-thia-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-6-(phenylsulfonyl)-2-oxa-6,10,13-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-hydroxy-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-[(1S)-1-[[(2-[[(1S)-2-hydroxy-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-12-cyclohexyl-N-[(1S)-1-[[[4-(dimethylamino)-2,4-dioxo-3-phenylbutyl]amino](oxo)acetyl]butyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
50% inhibition at 400 nM
(7R,9S,12S)-12-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-12-(1-methylethyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-12-(2-methylpropyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7R,9S,12S)-N-(1-[[(2-[[(S)-cyano(phenyl)methyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
(7S,12S,21S)-12-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-21-carboxamide
-
-
(R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(4-methoxybenzyl)phosphinic acid
-
-
(R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(isopropyl)phosphinic acid
-
-
(R)-((1S,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(phenyl)phosphinic acid
-
-
(R)-(4-chlorobenzyl)((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
-
(R)-4-((S)-2-acetamido-3-carboxypropanamido)-5-((2S,3S)-1-((S)-1-((2S,4R)-4-(benzyloxy)-2-(2-butyl-2-((S)-1-phenylethylcarbamoyl)hydrazinecarbonyl)pyrrolidin-1-yl)-3-methyl-1-oxobutan-2-ylamino)-3-methyl-1-oxopentan-2-ylamino)-5-oxopentanoic acid
-
-
-
(R)-benzyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
-
(R)-butyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
-
(S)-((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)(2-methoxybenzyl)phosphinic acid
-
-
(S)-((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)(2-methoxybenzyl)phosphinic acid
-
-
(S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
-
(S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
-
(S)-2-[[(1R,2R,4S)-2-[(R)-1-[((R)-cyclohexylmethoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-butyric acid
-
21% inhibition at a concentration of 10 micromol
(S)-2-[[(1R,2R,4S)-2-[(R)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
35% inhibition at a concentration of 10 micromol
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((R)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
37% inhibition at a concentration of 10 micromol
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-butyric acid
-
65% inhibition at a concentration of 10 micromol
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
100% inhibition at a concentration of 10 micromol
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methylcarbamoyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-4,4-difluoro-butyric acid
-
-
(S)-2-[[(1R,4R)-2-[(R)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopent-2-enecarbonyl]-amino]-pentanoic acid
-
-
(S)-2-[[(1S,4S)-2-[(R)-1-[((S)-cyclohexyl-methoxycarbonylmethyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopent-2-enecarbonyl]-amino]-pentanoic acid
-
-
(S)-benzyl((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
-
(S)-benzyl((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
-
(Z)-(1R,4R,6S,14R,16R)-12-tert-butoxycarbonylamino-16-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,13-dioxo-3,12-diaza-tricyclo[12.3.0. 04, 6]heptadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,15R,17R)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,15R,17R)-13-tert-butoxycarbonylamino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,15R,17R)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-13-methyl-2,14-dioxo-3,13-diazatricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,15R,17S)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo-[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,16R,18R)-14-amino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diazatricyclo[14.3.0.04,6]nonadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,16R,18R)-14-tert-butoxycarbonylamino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diaza-tricyclo[14.3.0.04,6]nonadec-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,17R) and (1S,4R,6S,17S)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadeca-7,15-diene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,17R,19R)-15-amino-19-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,16-dioxo-3,15-diaza-tricyclo[15.3.0.04,6]icos-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,17R,19R)-15-tert-butoxycarbonylamino-19-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,16-dioxo-3,15-diaza-tricyclo[15.3.0.04,6]icos-7-ene-4-carboxylic acid
-
-
(Z)-(1R,4R,6S,18R) and (1S,4R,6S,18S)-14-amino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diaza-tricyclo[14.3.0.04,6]nonadeca-7,16-diene-4-carboxylic acid
-
-
1,1-dimethylethyl [1-cyclohexyl-2-[(1S,5R)-6,6-dichloro-2(S)-[[[1-[1,2-dioxo-2-(2-propenylamino) ethyl]butyl]-amino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-2-oxoethyl]carbamate
-
-
1,1-dimethylethyl [2-[(1S,5R)-2(S)-[[[1-(2-amino-1,2-dioxoethyl)butyl]amino]carbonyl]-6,6-dichloro-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxoethyl]-carbamate
-
-
1,1-dimethylethyl[1-cyclohexyl-2-[(1S,5R)-6,6-dichloro-2(S)-[[[1-[2-[[2-[[2-(dimethylamino)-2-oxo-1(S)-phenylethyl]amino]-2-oxoethyl]amino]-1,2-dioxoethyl]-butyl]amino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-2-oxoethyl]carbamate
-
-
1,1-dimethylethyl[2-[(1S,5R)-6,6-dichloro-2(S)-[[ [1-(cyclopropyl-methyl)-3-[[2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl]amino]-2,3-dioxopropyl]-amino]carbonyl]-3-azabicyclo[3.1.0]-hexan-3-yl]-1-cyclohexyl-2-oxoethyl]carbamate
-
-
1,1-dimethylethyl[2-[(1S,5R)-6,6-dichloro-2(S)-[[1-(cyclobutylmethyl)-3-[[2-[[2-(dimethylamino)-2-oxo-1(S)-phenylethyl]amino]-2-oxomethyl]amino]-2,3-dioxopropylamino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxomethyl]carbamate
-
-
1,10-phenanthroline
O92972
inhibits NS2/3 auto-cleavage and NS3 protease activity
1,10-phenanthroline
-
0.26 mM, 50% inhibition
1,3,4-tri-O-galloyl-beta-D-glucose
-
from Saxifraga melanocentra
1,3,6-tri-O-galloyl-beta-D-glucose
-
from Terminalia chebula
1-(4-aminophenyl)-2-phenylethane-1,2-dione
-
-
1-([1-[(1,2-diphenylhydrazino)carbonyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
-
1-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbonyl]-amino)-2-vinyl-cyclopropanecarboxylic acid
-
IC50: 0.0097 mM
1-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
-
IC50: 0.33 mM
1-([1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-hydroxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
-
IC50: above 1 mM
1-([1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-phenoxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
-
IC50: above 0.08 mM
1-([4-(3'-Acetylamino-biphenyl-3-yloxy)-1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
1-aminocyclopropane-1-carboxylic acid ketoacid
-
electrophilic and acidic compound
1-aminocyclopropane-1-carboxylic acid ketotetrazole
-
electrophilic and acidic compound
1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone
-
electrophilic and non-acidic compound
1-aminocyclopropanecarboxylic acid
-
non-electrophilic and acidic compound
1-benzofuran-2-carboxylic acid
-
-
1-benzothiophene-2-carboxylic acid
-
-
1-methyl-1H-indole-2-carboxylic acid
-
-
1-O-(3-O-galloylgalloyl)-2,3,4-tri-O-galloyl-beta-D-glucose
-
from Saxifraga melanocentra
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.025 mM
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-phenyl-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-phenyl-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-thiophen-3-yl-pyridin-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: above 0.2 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3'-nitro-biphenyl-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.05 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3-morpholin-4-yl-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.032 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4'-methoxy-biphenyl-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: above 0.2 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4'-methoxy-biphenyl-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.035 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.025 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-bromo-phenylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.04 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-chloro-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.05 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-fluoro-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.1 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-iodo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.01 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(5-chloro-quinolin-8-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.1 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(6-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.016 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-chloro-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.002 mM
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.0008 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-trifluoromethyl-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-trifluoromethyl-quinolin-4-ylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.009 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(benzothiazol-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.02 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(benzothiazol-2-ylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.02 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: above 0.2 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.035 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(isoquinolin-1-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.008 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(isoquinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.004 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2,2-diethyl-cyclopropanecarboxylic acid
-
IC50: 0.31 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2-ethyl-cyclopropanecarboxylic acid
-
IC50: 0.0048 mM
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
IC50: 0.00063 mM
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.014 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(pyridin-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.19 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(pyridin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.17 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.005 mM
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(quinolin-8-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.25 mM
12-cyclohexyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)-methyl)aminooxalyl)butyl)amide
-
50% inhibition at 130 nM
12-tert-butyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
50% inhibition at 700 nM
12-tert-butyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)-aminooxalyl)butyl)amide
-
50% inhibition at 200 nM
1H-indole-2-carboxylic acid
-
-
2'-[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-5-(1-carboxy-cyclopropylcarbamoyl)-pyrrolidin-3-yloxy]-biphenyl-4-carboxylic acid
-
IC50: above 0.2 mM
2,2,2-trifluoro-1,1-dimethylethyl[2-[(1S,5R)-2(S)-[[[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]amino]-carbonyl]-6,6-dichloro-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxoethyl]carbamate
-
-
2,2-Dihydroxy-indan-1,3-dione
-
-
2-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid
-
IC50: above 0.1 mM
2-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid methyl ester
-
IC50: 0.054 mM
2-(3-chlorobenzoyl)benzoic acid
-
-
2-(4-Butyl-phenyl)-2-phenylsulfanyl-indan-1,3-dione
-
IC50: 0.0017 mM
2-(4-carboxybenzoyl)benzoic acid
-
-
2-(4-chlorobenzoyl)-6-(methoxycarbonyl)benzoic acid
-
-
2-(4-chlorobenzoyl)-6-[(dimethylamino)carbonyl]benzoic acid
-
-
2-(4-chlorobenzoyl)benzoic acid
-
-
2-(4-chlorobenzyl)benzoic acid
-
-
2-(4-chlorophenoxy)benzoic acid
-
-
2-(4-fluorobenzoyl)benzoic acid
-
-
2-(4-fluorophenoxy)benzoic acid
-
-
2-(4-hydroxybenzoyl)-4-methylbenzoic acid
-
-
2-(4-hydroxybenzoyl)benzoic acid
-
-
2-(4-hydroxybenzyl)benzoic acid
-
-
2-(4-methoxybenzoyl)benzoic acid
-
-
2-(4-methylbenzoyl)benzoic acid
-
-
2-(4-[3-[1-Carboxy-2-(4-hydroxy-3,5-diiodo-phenyl)-ethylcarbamoyloxy]-propoxy]-benzoyl)-benzoic acid
-
; competitive
2-(4-[3-[1-tert-Butoxycarbonyl-2-(4-hydroxy-3,5-diiodo-phenyl)-ethylcarbamoyloxy]-propoxy]-benzoyl)-benzoic acid tert-butyl ester
-
; competitive
2-(carboxymethyl)-6-(4-chlorobenzoyl)benzoic acid
-
-
2-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbonyl]-amino)-pentanoic acid
-
IC50: 0.53 MM
2-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbony]}-amino)-3-mercapto-propionic acid
-
IC50: 0.14 mM
2-Chloro-6-(4-chloro-benzoyl)-benzoic acid
-
-
2-Hydroxy-2-(1-nitro-ethyl)-indan-1,3-dione
-
-
2-Hydroxy-2-(2-nitro-cyclopentyl)-indan-1,3-dione
-
-
2-Methyl-2-phenylsulfanyl-indan-1,3-dione
-
IC50: 0.0036 mM
2-O-(4-O-galloylgalloyl)-1,3,4-tri-O-galloyl-beta-D-glucose
-
from Rhodiola kirilowii
2-Phenyl-2-phenylsulfanyl-indan-1,3-dione
-
IC50: 0.012 mM
2-Phenylsulfanyl-2-p-tolyl-indan-1,3-dione
-
IC50: 0.0031 mM
2-[1-[1-(1-Carbamoyl-3-methyl-butylcarbamoyl)-2-carboxy-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid
-
IC50: 0.015 mM, wild-type enzyme, IC50: 0.017 mM, mutant enzyme K136R, IC50: 0.027 mM, mutant enzyme K136M, IC50: 0.05 mM, mutant enzyme K136S, IC50: above 0.3 mM, mutant enzyme R109Q
2-[1-[2-Carboxy-1-(1-ethylcarbamoyl-3-methyl-butylcarbamoyl)-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl]-cyclohexanecarboxylic acid
-
IC50: 0.032 mM
2-[4-(3-carboxypropyl)benzoyl]benzoic acid
-
-
2-[4-(trifluoromethyl)benzoyl]benzoic acid
-
-
3,3'-digalloylprocyanidin B2
-
-
3,3'-digalloylproprodelphinidin B2
-
rhodisin
3,4-Dichloroisocoumarin
-
0.03 mM, 50% inhibition
3,6-di-O-galloyl-beta-D-glucose
-
from Saxifraga melanocentra
3-(2-[2-[2-(4-carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid
-
IC50: 0.0092 mM
3-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid methyl ester
-
IC50: 0.025 mM
3-(4-acetylphenoxy)propanoic acid
-
-
3-(4-hydroxy-3,5-diiodophenyl)-2-phenylpropanoic acid
-
-
3-(4-hydroxy-3,5-diiodophenyl)-3-phenylpropanoic acid
-
-
3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
-
-
3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)-henicosa-13(21),14,16(20)-triene-18-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
inhibitor adopts a donutlike conformation and has close contact to A156 methyl group of enzyme
3-[(2R,5S,8S)-8-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-5-cyclohexyl-3,6,14,18-tetraoxo-1,4,7,13-tetraazacyclooctadecan-2-yl]propanoic acid
-
-
3-[(3S,6R,17S)-17-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-3-cyclohexyl-2,5,8,11-tetraoxo-1,4,7,12-tetraazacycloheptadecan-6-yl]propanoic acid
-
-
3-[2-(2-Benzyloxycarbonylamino-3-methyl-pentanoylamino)-4-methyl-pentanoylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
-
3-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
-
3-[2-(2-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-carboxy-butyrylamino)-3-cyclohexyl-propionylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
-
3-[2-(3-tert-butyl-ureido)-2-indan-2-yl-acetyl]-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
3-[2-(3-tert-butyl-ureido)-3,3-dimethyl-butyryl]-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
3-[2-[2-(2-Acetylamino-3,3-diphenyl-propionylamino)-4-tert-butoxycarbonyl-butyrylamino]-3-cyclohexyl-propionylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
-
4-(2-aminoethyl)-benzenesulfonyl fluoride
-
0.45 mM, 50% inhibition
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-3-methyl-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
highly specific
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
reversible competitive inhibitor, highly specific
4-(2-[2-[2-(4-carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-3-chloro-benzoic acid
-
IC50: 0.0007 mM
4-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-3-chloro-benzoic acid methyl ester
-
IC50: 0.0032 mM
4-(2-[2-[2-(4-carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid
-
IC50: 0.002 mM
4-(2-[2-[2-(4-Carboxy-2-isobutoxycarbonylamino-butyrylamino)-4-methyl-pentanoylamino]-3-mercapto-propionylamino]-ethyl)-benzoic acid methyl ester
-
IC50: 0.017 mM
4-(4-hydroxy-3,5-diiodophenyl)butanoic acid
-
-
4-(amidinophenyl)-methanesulfonyl fluoride
-
1.89 mM, 50% inhibition
4-(trifluoroacetyl)benzoic acid
-
-
4-Benzyloxycarbonylamino-4-[1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
-
IC50: 0.04 mM
4-chloro-1H-indole-2-carboxylic acid
-
-
4-hydroxy-2-(4-hydroxybenzoyl)benzoic acid
-
-
4-hydroxy-3,5-diiodobenzoic acid
-
-
4-hydroxypanduratin A
-
cyclohexenyl chalcone derivative, competetive inhibitor, compound from Boesenbergia rotunda (L.) Mansf. Kulturpfl.
4-Isobutoxycarbonylamino-4-[1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
-
IC50: 0.019 mM
4-methoxy-2-(4-methoxybenzoyl)benzoic acid
-
-
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-2-mercapto-ethylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
-
IC50: 0.0065 mM
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-3,3-difluoro-propenylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
-
-
4-tert-Butoxycarbonylamino-4-[1-(1-carboxy-2-mercapto-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
-
IC50: above 0.2 mM
4-tert-Butoxycarbonylamino-4-[1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-butyric acid
-
IC50: 0.027 mM
4-[(7R,9S,12R)-9-[(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-12-yl]cyclohexanecarboxylic acid
-
-
4-[1-(1-Benzylcarbamoyl-2-mercapto-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-4-tert-butoxycarbonylamino-butyric acid
-
IC50: above 0.2 mM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-2-mercapto-ethylcarbamoyl]-2-cyclohexyl-ethylcarbamoyl)-butyric acid
-
IC50: 2 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[1-(1-benzylcarbamoyl-2-mercapto-ethylcarbamoyl)-2-cyclohexyl-ethylcarbamoyl]-butyric acid
-
IC50: 250 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-(2-mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-ethylcarbamoyl]-butyric acid
-
IC50: 7 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[1-(2-cyclohexyl-ethylcarbamoyl)-2-mercapto-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
-
IC50: 1540 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[1-(indan-2-ylcarbamoyl)-2-mercapto-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
-
IC50: 1700 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[2-mercapto-1-(2-phenyl-cyclopropylcarbamoyl)-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
-
IC50: 1500 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[2-mercapto-1-(3-phenyl-propylcarbamoyl)-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
-
IC50: 210 nM
4-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-[2-cyclohexyl-1-[2-mercapto-1-(methyl-phenethyl-carbamoyl)-ethylcarbamoyl]-ethylcarbamoyl]-butyric acid
-
IC50: 0.07 mM
4MeBu-P-norvaline-(CO)-GMSYS-NH2
-
CVS4440
-
5-bromo-1H-indole-2-carboxylic acid
-
-
5-bromo-2-(4-hydroxybenzoyl)benzoic acid
-
-
5-chloro-1-benzofuran-2-carboxylic acid
-
-
5-chloro-1H-indole-2-carboxylic acid
-
-
5-cyclohexyl-3,6-dioxo-11,16-dioxa-4,7-diazatricyclo(15.3.1.17,10)-docosa-1(21),17,19-triene-8-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
-
5-fluoro-1H-indole-2-carboxylic acid
-
-
5-methoxy-1-benzothiophene-2-carboxylic acid
-
-
5-methoxy-1H-indole-2-carboxylic acid
-
-
5-methyl-1H-indole-2-carboxylic acid
-
-
6,6-dichloro-3-[2-cyclohexyl-2-(3-cyclohexyl-ureido)-acetyl]-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
6-chloro-1H-indole-2-carboxylic acid
-
-
7-bromo-1H-indole-2-carboxylic acid
-
-
7-chloro-1H-indole-2-carboxylic acid
-
-
Ac-Asp-Glu-Leu-Ile-Cha-Cys-OH
-
-
Ac-DdIVPC-OH
-
0.04 mM, 50% inhibition
-
Ac-DvIVPC-OH
-
0.0075 mM, 50% inhibition
-
Ac-EVKKQR-NH2
-
-
Ac-FAAGRK-NH2
-
-
Ac-FASGKR-arginylaldehyde
-
competitive, 50% inhibition at about 0.001 mM
Ac-GKR-NH2
-
-
Ac-KKR-NH2
-
-
Ac-KR-NH2
-
-
Ac-RTSKKR-NH2
-
-
Ac-SKKR-NH2
-
-
Ac-TTSTRR-NH2
-
-
acetyl-3,3-diphenylalanine-beta-cyclohexylalanine-Cys-OH
-
0.3 mM, 50% inhibition
-
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
-
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
-
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
-
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
-
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
-
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
-
acetyl-Asp-D-(gamma-carboxyglutamic acid)-Leu-Ile-(beta-cyclohexylalanine)-Cys
-
-
acetyl-Asp-D-Glu-Leu-Ile-(beta-cyclohexylalanine)-Cys-(Me)Ala-Ser-His-Leu-NH2
-
IC50: 0.0006 mM, inhibitor is cleaved by NS3/4A protease
acetyl-Asp-Glu-(3,3-diphenylalanine)-Glu-(beta-cyclohexylalanine)-Cys
-
-
acetyl-Asp-Glu-(3,3-diphenylalanine)-Ile-(beta-cyclohexylalanine)-Cys
-
-
acetyl-Asp-Glu-(3,3-diphenylalanine)-Ile-(beta-cyclohexylalanine)-Cys-(Me)Ala-Ser-His-Leu-NH2
-
IC50: 0.0034 mM, inhibitor is cleaved by NS3/4A protease
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
-
acetyl-Asp-Glu-3,3-diphenylalanine-Glu-beta-cyclohexylalanine-Cys-OH
-
0.00005 mM, 50% inhibition
acetyl-Asp-Glu-3,3-diphenylalanine-Ile-beta-cyclohexylalanine-OH
-
0.046 mM, 50% inhibition
acetyl-Asp-Glu-Leu-Glu-(beta-cyclohexylalanine)-Cys
-
-
acetyl-Asp-Glu-Leu-Glu-beta-cyclohexylalanine-Cys-OH
-
0.0026 mM, 50% inhibition
acetyl-Asp-Glu-Leu-Ile-beta-cyclohexylalanine-Cys-OH
-
0.00006 mM, 50% inhibition
acetyl-Asp-Glu-Met-Glu-beta-cyclohexylalanine-Cys-OH
-
0.00035 mM, 50% inhibition
acetyl-Asp-Glu-Met-Glu-Glu-Cys
-
-
acetyl-Asp-Glu-Met-Glu-Glu-Cys-OH
-
0.001 mM, 50% inhibition
acetyl-Asp-Glu-Val-Val-Pro-boroAlg-OH
-
the inhibitor binds in an antiparrallel manner to beta-strand E2 and interacts with the unprimed sites of the substrate binding pocket. In the NS3/NS4 inhibitor complex, the inhibitor behaves like a reaction intermediate analog. In the absence of the cofactor, inhibitor binding is an order of magnitude weaker
acetyl-DEMEEC-OH
-
-
acetyl-DYPSPC-OH
-
-
acetyl-ECTTPC-OH
-
-
acetyl-EDVVCC-OH
-
-
acetyl-EEVVP-norvaline-(CO)-GMSYS-NH2
-
CVS4437
-
acetyl-EEVVP-norvaline-(CO)-phenethylamide
-
CVS4442
-
acetyl-Glu-3,3-diphenylalanine-Glu-beta-cyclohexyalanine-Cys-OH
-
0.0014 mM, 50% inhibition
acetyl-Glu-Asp-Val-Val-(alpha-aminobutyryl)-Cys-(1,2,3,4-tetrahydroisoquinoline-3-L-carboxyl)-Nle-Ser-Tyr-NH2
-
IC50: 0.0019 mM, inhibitor is cleaved by NS3/4A protease
acetyl-Glu-Asp-Val-Val-(alpha-aminobutyryl)-Cys-(Me)Ala-Nle-Ser-Tyr-NH2
-
IC50: 0.0035 mM, inhibitor is cleaved by NS3/4A protease
acetyl-Glu-Asp-Val-Val-Leu-Cys-(1,2,3,4-tetrahydroisoquinoline-3-L-carboxyl)-Nle-Ser-Tyr-NH2
-
IC50: 0.001 mM, inhibitor is cleaved by NS3/4A protease
acetyl-Glu-beta-cyclohexylalanine-Cys-OH
-
0.46 mM, 50% inhibition
acetyl-Glu-Leu-Glu-beta-cyclohexylalanine-Cys-OH
-
5 mM, 50% inhibition
acetyl-P-norvaline-(CO)-GMSYS-NH2
-
CVS4441
-
acetyl-QSVVCC-OH
-
-
acetyl-VVP-norvaline-(CO)-G-NH2
-
SCH212986
-
acetyl-VVP-norvaline-(CO)-S(Bzl)-NH2
-
SCH215426
-
alpha1-anitrypsin
-
-
-
alpinetin
-
compound from Boesenbergia rotunda (L.) Mansf. Kulturpfl.
antibody Fv fragment
-
specific for the HCV NS3 protease domain, IC50: 71.3 nM
-
Asp-Glu-Leu-Ile-L-cyclohexylalanine-aminobutyryl-(Me)Ala-Ser-His-Leu
-
IC50: 5 mM
Asp-Glu-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
IC50: 15 nM
Asp-Glu-Leu-Ile-L-cyclohexylalanine-Cys-Pro-L-cyclohexylalanine-Asp-Leu
-
IC50 below 0.2 nM
Asp-Glu-Leu-Ile-L-cyclohexylalanine-Cys-Pro-Nle-Ser-Leu
-
IC50: 10 nM
benzyl 1-([[(2S)-1-[(1R,5S)-2-[(4-amino-1-cyclopropyl-3,4-dioxobutan-2-yl)carbamoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hex-3-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl]amino)cyclohexanecarboxylate
-
-
-
benzyloxycarbonyl-L-Ile-L-Leu-L-(difluoro)aminobutyric acid
-
-
BILN 2061
P27958
significantly less active on genotype 2 and 3 enzyme
BILN 2061
-
potent inhibitor
BILN-2061
-
used in clinical trials. Potently inhibits Hepatitis C virus replication in human hepatoma cells, but causes cardiac toxicity in experimental animals
BILN-2061
-
about 90% inhibition at 40 nM
BILN-2061
-
rapidly reversible NS3 inhibitor
BILN2061
-
NS3 protease inhibitor, fully restores MAVS/IPS-1-dependent IFN-alpha promoter activity in Hepatitis C virus-infected cells
bis(4-aminophenyl)methanone
-
-
boceprevir
-
SCH 503034, slowly reversible covalent inhibitor
Bowman-Birk inhibitor
-
from mung bean
Bz-Ala-Lys-Arg-Arg-H
-
-
Bz-Ala-Lys-Arg-Arg-H
-
-
Bz-Ala-Lys-Arg-Arg-H
-
-
Bz-Arg-Arg-H
-
-
Bz-D-Nle-Lys-Arg-Arg-H
-
-
Bz-D-Nle-Lys-Arg-Arg-H
-
-
Bz-Lys-Arg-Arg-H
-
-
Bz-Lys-Arg-Arg-H
-
-
Bz-N-Me-Nle-Lys-Arg-Arg-H
-
-
Bz-N-Me-Nle-Lys-Arg-Arg-H
-
-
Bz-Nle-Ala-Arg-Arg-H
-
-
Bz-Nle-Ala-Arg-Arg-H
-
-
Bz-Nle-Ala-Arg-Arg-H
-
-
Bz-Nle-D-Lys-Arg-Arg-H
-
-
Bz-Nle-D-Lys-Arg-Arg-H
-
-
Bz-Nle-Lys-Ala-Arg-H
-
-
Bz-Nle-Lys-Ala-Arg-H
-
-
Bz-Nle-Lys-Ala-Arg-H
-
-
Bz-Nle-Lys-Arg-(p-Cl)-Phe-H
-
-
Bz-Nle-Lys-Arg-(p-Cl)Phe-H
-
-
Bz-Nle-Lys-Arg-(p-CN)-Phe-H
-
-
Bz-Nle-Lys-Arg-(p-CN)Phe-H
-
-
Bz-Nle-Lys-Arg-(p-guanidinyl)-Phe-H
-
-
Bz-Nle-Lys-Arg-(p-guanidinyl)Phe-H
-
-
Bz-Nle-Lys-Arg-(p-Me)Phe-H
-
-
Bz-Nle-Lys-Arg-(p-Ph)-Phe-H
-
-
Bz-Nle-Lys-Arg-(p-Ph)Phe-H
-
-
Bz-Nle-Lys-Arg-Ala-H
-
-
Bz-Nle-Lys-Arg-Ala-H
-
-
Bz-Nle-Lys-Arg-Ala-H
-
-
Bz-Nle-Lys-Arg-Arg(OH)-CONH-Bn
-
-
Bz-Nle-Lys-Arg-Arg-B(OH)2
-
-
Bz-Nle-Lys-Arg-Arg-benzoxazole
-
-
Bz-Nle-Lys-Arg-Arg-CF3
-
-
Bz-Nle-Lys-Arg-Arg-H
-
-
Bz-Nle-Lys-Arg-Arg-H
-
-
Bz-Nle-Lys-Arg-Arg-H
-
-
Bz-Nle-Lys-Arg-Arg-NH2
-
-
Bz-Nle-Lys-Arg-Arg-NHSO2CF3
-
-
Bz-Nle-Lys-Arg-Arg-OH
-
-
Bz-Nle-Lys-Arg-Arg-thiazole
-
-
Bz-Nle-Lys-Arg-D-Arg-H
-
-
Bz-Nle-Lys-Arg-D-Arg-H
-
-
Bz-Nle-Lys-Arg-His-H
-
-
Bz-Nle-Lys-Arg-homoPhe-H
-
-
Bz-Nle-Lys-Arg-Lys-H
-
-
Bz-Nle-Lys-Arg-Lys-H
-
-
Bz-Nle-Lys-Arg-Lys-H
-
-
Bz-Nle-Lys-Arg-Phe-H
-
-
Bz-Nle-Lys-Arg-Phe-H
-
-
Bz-Nle-Lys-Arg-Phe-H
-
-
Bz-Nle-Lys-Arg-Phg-H
-
-
Bz-Nle-Lys-Arg-Phg-H
-
-
Bz-Nle-Lys-Arg-Trp-H
-
-
Bz-Nle-Lys-Arg-Trp-H
-
-
Bz-Nle-Lys-Arg-Tyr-H
-
-
Bz-Nle-Lys-D-Arg-Arg-H
-
-
Bz-Nle-Lys-D-Arg-Arg-H
-
-
Bz-Nle-Lys-Lys(Z)-Arg-H
-
-
Bz-Nle-Lys-Lys-Arg-B(OH)2
-
-
Bz-Nle-Lys-Lys-Arg-H
-
-
Bz-Nle-Lys-Lys-Arg-H
-
-
Bz-Nle-Lys-Lys-Arg-H
-
-
Bz-Nle-Lys-N-Me-Arg-Arg-H
-
-
Bz-Nle-Lys-N-Me-Arg-Arg-H
-
-
Bz-Nle-Lys-Phe-Arg-H
-
-
Bz-Nle-Lys-Phe-Arg-H
-
-
Bz-Nle-Lys-Phe-Arg-H
-
-
Bz-Nle-Lys-Pro-Arg-H
-
-
Bz-Nle-Lys-Thr-Arg-H
-
-
Bz-Nle-Lys-Thr-Arg-NH2
-
-
Bz-Nle-Lys-Thr-Arg-OH
-
-
Bz-Nle-N-Me-Lys-Arg-Arg-H
-
-
Bz-Nle-N-Me-Lys-Arg-Arg-H
-
-
Bz-Nle-Phe-Arg-Arg-H
-
-
Bz-Nle-Phe-Arg-Arg-H
-
-
Bz-Nle-Phe-Arg-Arg-H
-
-
Bz-Nle-Pro-Arg-Arg-H
-
-
Bz-Nle-Pro-Arg-Arg-H
-
-
Bz-Phe-Lys-Arg-Arg-H
-
-
Bz-Phe-Lys-Arg-Arg-H
-
-
Bz-Phe-Lys-Arg-Arg-H
-
-
cardamonin
-
chalcone, non-competetive inhibitor, compound from Boesenbergia rotunda (L.) Mansf. Kulturpfl.
chymostatin
-
0.71 mM, 50% inhibition
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17R)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carbonyl]-amide
-
-
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17R)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-13-methyl-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carbonyl]-amide
-
high potency, lacks the P4 substituent
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17S)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0. 04,6]octadec-7-ene-4-carbonyl]-amide
-
-
cyclopropyl(4-methoxyphenyl)methanone
-
-
DDIVPC-OH
-
0.071 mM, 50% inhibition
deca-D-Arg-NH2
-
-
dodeca-D-Arg-NH2
-
-
dodeka-D-Arg-NH2
-
-
EDTA
O92972
inhibits NS2/3 auto-cleavage and NS3 protease activity
EDTA
-
0.007 mM, 50% inhibition
EDVVAbuC-OH
-
-
EGTA
-
1.6 mM, 50% inhibition
fluorescein-L-Asp-D-Glu-L-Leu-L-Ile-L-beta-cyclohexylalanine-L-Cys-L-Pro-L-beta-cyclohexylalanine-L-Asp-L-Leu-NH2
-
i.e. PepInh-1, noncleavable decapeptidyl inhibitor
GS-9132
-
an acylthiourea with in vitro activity against Hepatitis C virus genotype 1, inhibits the formation of a functional replication complex. Reversible nephrotoxicity in clinical trials
hepta-D-Arg-NH2
-
-
hexa-D-Arg-NH2
-
-
IFN-alpha
-
-
-
iodoacetamide
-
0.26 mM, 50% inhibition
ITMN-191
-
high in vitro potency and specificity
ITMN-191
-
rapidly reversible inhibitor
ITMN-C
-
active site inhibitor of the NS3-4A protease
-
L-aminobutyric acid carboxylic acid
-
non-electrophilic and acidic compound
L-aminobutyric acid pentafluoroethyl ketone
-
electrophilic and non-acidic compound
L-norvaline carboxylic acid
-
non-electrophilic and acidic compound
L-norvaline ketotetrazole
-
electrophilic and acidic compound
L-norvaline pentafluoroethyl ketone
-
electrophilic and non-acidic compound
L-Valine, N-[[[(1S)-1-[[(3'aR,6'aS)-1'-(cyclopropylcarbonyl)hexahydro-2'-oxospiro[cyclobutane-1,3'(4'H)-pyrrolo[3,2-b]pyrrol]-4'-yl]carbonyl]-2-methylpropyl]amino]carbonyl]-, 1,1-dimethylethyl ester
-
-
L-Valine, N-[[[(1S)-1-[[(3'aR,6'aS)-1'-(cyclopropylcarbonyl)hexahydro-2'-oxospiro[cyclobutane-1,3'(4'H)-pyrrolo[3,2-b]pyrrol]-4'-yl]carbonyl]-2-methylpropyl]amino]carbonyl]-, methyl ester
-
-
L-Valine, N-[[[(1S)-1-[[(3'aR,6'aS)-1'-(cyclopropylcarbonyl)hexahydro-2'-oxospiro[cyclobutane-1,3'(4'H)-pyrrolo[3,2-b]pyrrol]-4'-yl]carbonyl]-2-methylpropyl]amino]carbonyl]-, phenylmethyl ester
-
-
L-Valine, N-[[[(1S)-1-[[(3'aR,6'aS)-1'-(cyclopropylcarbonyl)hexahydro-2'-oxospiro[cyclobutane-1,3'(4'H)-pyrrolo[3,2-b]pyrrol]-4'-yl]carbonyl]-2-methylpropyl]amino]sulfonyl]-, 1,1-dimethylethyl ester
-
-
N-(cyclohexylacetyl)-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000037 mM
N-(cyclohexylcarbamoyl)-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000009 mM
N-(cyclopentylcarbamoyl)-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000005 mM
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-4-[[7-(acetylamino)-2-phenylquinolin-4-yl]oxy]-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-L-prolinamide
-
50% inhibition at 0.000029 mM
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-([2-[2-(dimethylamino)-1,3-thiazol-4-yl]pyridin-4-yl]oxy)-L-prolinamide
-
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000029 mM
N-(tert-butoxycarbonyl)-D-valyl-(4S)-N-(1-carboxy-2-ethenylcyclopropyl)-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolinamide
-
50% inhibition of processing of substrate SEAP-1 at 0.00026 mM
N-(tert-butylcarbamoyl)-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000008 mM
N-([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)-L-norvaline
-
-
N-([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)-L-norvaline
-
-
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-b-phenyl-L-phenylalanyl-L-alpha-glutamyl-N-[1-(carboxycarbonyl)-3,3-difluoropropyl]-3-cyclohexyl-L-alaninamide
-
50% inhibition of processing of substrate SEAP-1 at 0.0067 mM
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-beta-phenyl-L-phenylalanyl-L-alpha-glutamyl-3-cyclohexyl-L-alanine
-
1.17 mM, 50% inhibition
N-acetyl-L-alpha-aspartyl-N-[(1S)-2-[[(1S)-1-([(2S,4R)-2-[[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]carbamoyl]-4-[(2-phenylquinolin-4-yl)oxy]pyrrolidin-1-yl]carbonyl)-2,2-dimethylpropyl]amino]-1-cyclohexyl-2-oxoethyl]-D-alpha-glutamine
-
-
N-tosyl-Phe chloromethyl ketone
-
0.03 mM, 50% inhibition
N-tosyl-Phe chloromethyl ketone
-
-
N-[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]-L-norvaline
-
-
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000001 mM
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000013 mM, no inhibition of human leukocyte elastase, cathepsin B
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(6-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000041 mM
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7,8-dimethoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000013 mM
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000002 mM
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(8-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000005 mM
N-[(2S)-2-(acetylamino)-2-cyclohexylacetyl]-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[[2-(3-methoxyphenyl)quinolin-4-yl]oxy]-L-prolinamide
-
50% inhibition at 0.000010 mM
N-[(2S)-2-amino-2-cyclohexylacetyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000018 mM
N-[(2S)-2-cyclohexylpropanoyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000037 mM
N-[(2S)-2-[(N-acetyl-L-alpha-aspartyl-D-alpha-glutamyl)amino]-2-cyclohexylacetyl]-L-valyl-(4S)-4-(naphthalen-2-ylmethoxy)-D-prolyl-D-norvaline
-
-
N-[(cyclobutyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000024 mM
N-[(cyclohexyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000030 mM
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1R,2R)-1-[(cyclopropylsulfonyl)carbamoyl]-2-(methylideneamino)cyclopropyl]-4-hydroxy-L-prolinamide
-
-
-
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
50% inhibition at 0.000014 mM
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-phenyl-L-prolinamide
-
-
N-[(cyclopentyloxy)carbonyl]-L-leucyl-(4R)-N-[(2S,3R)-2-carboxy-3-ethenylcyclopropyl]-4-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-L-prolinamide
-
-
N-[(cyclopentyloxy)carbonyl]-L-leucyl-(4R)-N-[(2S,3S)-2-ethenyl-3-phosphonocyclopropyl]-4-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-L-prolinamide
-
-
N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide
-
HCV replication in a cellular assay (subgenomic 1b replicon) is inhibited with a half-maximal effective concentration (EC50) of 8 nM. The compound is synergistic with alpha interferon and an NS5B inhibitor in the replicon model and additive with ribavirin. In rats, the compound is extensively distributed to the liver and intestinal tract, and the absolute bioavailability is 44% after a single oral administration. Compound concentrations detected in both plasma and liver at 8 h postdosing are above the EC99 value measured in the replicon
N-{17-[8-chloro-2-(4-isopropylthiazol-2-yl)-7-methoxy-quinolin-4-yloxy]-2,14-dioxo-3,15-diazatricyclo [13.3.0.0]octadec-7-ene-4-carbonyl}-(1-methylcyclo propyl)-(1-methylcyclopropyl)sulfonamide
-
EC50 = 3.76 nM, non-cytotoxic (CC50 above 0.020 nM), and metabolically stable HCV inhibitor. Compound exhibits advantageous drug metabolism and pharmacokinetic properties in rat and dog, with a high liver exposure after oral administration, but limited heart exposure observed in rat
Nalpha-p-tosyl-Lys chloromethyl ketone
-
0.15 mM, 50% inhibition
-
Nalpha-p-tosyl-Lys chloromethyl ketone
-
-
-
nona-D-Arg-NH2
-
reduces infection in primary neurons
octa-D-Arg-NH2
-
-
panduratin A
-
cyclohexenyl chalcone derivative, competetive inhibitor, compound from Boesenbergia rotunda (L.) Mansf. Kulturpfl.
peptidyl-alpha ketoamides
-
-
-
phenylmethanesulfonyl fluoride
-
0.6 mM, 50% inhibition
pinocembrin
-
compound from Boesenbergia rotunda (L.) Mansf. Kulturpfl.
pinostrobin
-
flavanone, non-competetive inhibitor, compound from Boesenbergia rotunda (L.) Mansf. Kulturpfl.
RNA aptamer G9-I
-
noncompetitive inhibition, Arg161 as well Arg130 of the NS3 protease domain are essential for interaction with the G9-I aptamer
-
RNA aptamer G9-II
-
-
-
RNA aptamer G9-III
-
-
-
SCH-503034
-
used in clinical trials. Orally bioavailable, covalent, reversible alpha-keto amide inhibitor. Displays potent and time-dependent inhibition of the NS3-4A protease. Inhibitor dissociation constant in the low nanomolar range. Ability to effectively inhibit Hepatitis C virus RNA synthesis in the human hepatoma cells harboring the hepatitis C virus replicon
SCH6
-
active site inhibitor of the NS3-4A protease
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)-4'-[(2S)-2-[[(ethylamino)carbonyl]amino]-3-methyl-1-oxobutyl]hexahydro-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)-4'-[(2S)-2-[[[(cyclopropylmethyl)amino]carbonyl]amino]-3-methyl-1-oxobutyl]hexahydro-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)-4'-[(2S)-2-[[[[3-(dimethylamino)propyl]methylamino]carbonyl]amino]-3-methyl-1-oxobutyl]hexahydro-, (3'aR,6'aS)-
-
IC50: 0.00066 mM
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-2-[[[[(1S)-1-(hydroxymethyl)-2-methylpropyl]amino]carbonyl]amino]-3-methyl-1-oxobutyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-3-methyl-1-oxo-2-[[(2-propenylamino)carbonyl]amino]butyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-3-methyl-1-oxo-2-[[(propylamino)carbonyl]amino]butyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-3-methyl-1-oxo-2-[[[(2,2,2-trifluoroethyl)amino]carbonyl]amino]butyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-3-methyl-2-[[[(1-methylethyl)amino]carbonyl]amino]-1-oxobutyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 1'-(cyclopropylcarbonyl)hexahydro-4'-[(2S)-3-methyl-2-[[[[(1S)-2-methyl-1-[[4-(2-pyrimidinyl)-1-piperazinyl]carbonyl]propyl]amino]carbonyl]amino]-1-oxobutyl]-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4',4'''-[sulfonylbis[imino[(2S)-2-(1-methylethyl)-1-oxo-2,1-ethanediyl]]]bis[1'-(cyclopropylcarbonyl)hexahydro]-, (3'aR,3'''aR,6'aS,6'''aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4'-[(2S)-2-amino-3-methyl-1-oxobutyl]-1'-(cyclopropylcarbonyl)hexahydro-, monohydrochloride, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4'-[(2S)-2-[(aminocarbonyl)amino]-3-methyl-1-oxobutyl]-1'-(cyclopropylcarbonyl)hexahydro-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4'-[(2S)-2-[[(cyclohexylamino)carbonyl]amino]-3-methyl-1-oxobutyl]-1'-(cyclopropylcarbonyl)hexahydro-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4'-[(2S)-2-[[(cyclopentylamino)carbonyl]amino]-3-methyl-1-oxobutyl]-1'-(cyclopropylcarbonyl)hexahydro-, (3'aR,6'aS)-
-
-
Spiro[cyclobutane-1,3'(2'H)-pyrrolo[3,2-b]pyrrol]-2'-one, 4'-[(2S)-2-[[(cyclopropylamino)carbonyl]amino]-3-methyl-1-oxobutyl]-1'-(cyclopropylcarbonyl)hexahydro-, (3'aR,6'aS)-
-
-
STAT-C
-
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-COOH
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-COOH
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-NHSO2Ph
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-NHSO2Ph
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-2-aminovaleryl-NHSO2Ph
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-2-aminovaleryl-NHSO2Ph
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-aminobutyryl ((S)-2-amino-butanoyl)-C2F5
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-aminobutyryl ((S)-2-amino-butanoyl)-C2F5
-
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-Cys-OH
-
comparison with inhibitory effect on human leukocyte elastase, porcine pancreatic elastase, bovine pancreatic chymotrypsin, and cathepsin B
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-Cys-OH
-
-
telaprevir
-
VX-950
telaprevir
-
VX-950, slowly reversible covalent inhibitor
tert-butyl (1-cyclohexyl-2-[(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]pentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]-2-oxoethyl)carbamate
-
-
tert-butyl (1-[[(3R)-3-([1-(2-cyclobutylethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]carbonyl]-2,2-dimethylpropyl)carbamate
-
non-preferred name
tert-butyl (1-[[(3R)-3-([1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]carbonyl]-2,2-dimethylpropyl)carbamate
-
non-preferred name
tert-butyl (1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylate
-
-
tert-butyl (1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylate
-
-
tert-butyl (2S)-([N-[3-([[(3S,18S)-18-cyclohexyl-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinolin-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
tert-butyl (2S)-([N-[3-([[(3S,6S)-6-cyclohexyl-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-trien-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
tert-butyl (2S)-([N-[3-([[(7R,9S,12S)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
tert-butyl (2S)-[([[3-([[(6S,8S,9R,10S,13S)-13-cyclohexyl-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-trien-10-yl]carbonyl]amino)-2-oxohexanoyl]amino]acetyl)amino](phenyl)ethanoate
-
-
tert-butyl [(2R,6S,12Z,14aR,16aS)-14a-[(cyclopropylsulfonyl)carbamoyl]-2-[(6-methoxyisoquinolin-1-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,11,13a,14,14a,15,16,16a-tetradecahydro-5H-cyclopropa[e]pyrrolo[2,1-i][1,7,10]oxadiazacyclopentadecin-6-yl]carbamate
-
-
tert-butyl [1-([(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]-4-methylpentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]carbonyl)-2,2-dimethylpropyl]carbamate
-
non-preferred name
tert-butyl [1-([(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]pentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]carbonyl)-2,2-dimethylpropyl]carbamate
-
-
tert-butyl [1-cyclohexyl-2-[(3R)-3-([1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]-2-oxoethyl]carbamate
-
-
tert-butyl [2-[(3R)-3-([1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]-1-cyclohexyl-2-oxoethyl]carbamate
-
-
tert-butyloxacrybonyl-L-Glu-L-Leu-L-(difluoro)aminobutyric acid
-
-
TMC 435350
-
rapidly reversible inhibitor
TMC435
-
small-molecule reversible noncovalent inhibitor of the NS3/4A serine protease
trans-1,2-cyclohexanediamine-N,N,N',N'-tetraacetic acid
-
0.007 mM, 50% inhibition
undeca-D-Arg-NH2
-
-
vaniprevir
-
; MK-7009, i.e. (1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
-
VX-950
P27958
equally active on enzyme from all three genotypes
VX-950
-
used in clinical trials. Orally biovailable tetrapeptide alpha-ketoamide, binds slowly and reversibly to the protease, with an affinity for the genotype 1 Hepatitis C virus NS4-4A protease in the low nanomolar range and a half life of nearly an hour. Moderately potent inhibitor of Hepatitis C virus replication. Achieves a more than a 10000fold suppression of hepatitis C virus RNA in replicon cells treated for 14 days in the presence of relatively low concentrations of the compound
VX-950
-
telaprevir
[(2R,5S,8S)-8-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-5-cyclohexyl-3,6,14,18-tetraoxo-1,4,7,13-tetraazacyclooctadecan-2-yl]acetic acid
-
-
[(2R,6R,12Z,13aS,14S,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl]phosphonic acid
-
-
[(3S,6R,17S)-17-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-3-cyclohexyl-2,5,8,11-tetraoxo-1,4,7,12-tetraazacycloheptadecan-6-yl]acetic acid
-
-
[(Z)-(1R,4R,6S,15R,17R)-4-cyclopropanesulfonylaminocarbonyl-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-en-13-yl]-carbamic acid tert-butyl ester
-
-
[1-(6-Ethyl-4-methanesulfonyl-5-oxo-hexahydro-pyrrolo[3,2-b]pyrrole-1-carbonyl)-2-methyl-propyl]-carbamic acid tert-butyl ester
-
IC50: 0.0005 mM
[1-[1-(2-Mercapto-1-phenethylcarbamoyl-ethylcarbamoyl)-3-methyl-butylcarbamoyl]-2-methyl-propyl]-carbamic acid benzyl ester
-
IC50: 0.4 mM
[1-[2-(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethylcarbamoyl)-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-3-carbonyl]-2,2-dimethyl-propyl]-carbamic acid tert-butyl ester
-
is the most promising of all the inhibitors. With tert-leucine as P3 residue, extremely potent with single digit nanomolar potency in enzymatic assay. Excellent selectivity against elastase. Bioavailability above 10% in rat, monkey, and dog
[2-[2-(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethylcarbamoyl)-6,6-dichloro-3-aza-bicyclo[3.1.0]hex-3-yl]-1-indan-2-yl-2-oxo-ethyl]-carbamic acid tert-butyl ester
-
-
MK-7009
-
i.e. (1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,70.06,11]heptacosa-6,8,10-triene-24-carboxamide, potent and selective inhibitor of hepatitis C virus NS3/4A protease
additional information
-
alpha-ketoacids incorporating difluoroaminobutyric acid in the p1 position are potent slow binding inhibitors
-
additional information
-
many NS3 protease inhibitors have taken advantage of an unusual product inhibition by N-terminal products of cleavage at the polyprotein processing sites
-
additional information
-
solid-phase synthesis of peptidomimetic inhibitors
-
additional information
-
the effect of prime-site occupancy on the enzyme structure
-
additional information
-
inhibitors with electrophilic C-terminal residues are generally non-selective while compounds with non-electrophilic C-terminal residues are more selective. Compounds with P1 aminobutyric acid residues are non-selective, while 1-aminocyclopropanecarboxylic acid and norvaline-based inhibitors are generally selective. Most potent and selective inhibitors contain a non-electrophilic phenyl acyl sulfonamide C-terminal residue
-
additional information
-
the P1 and P2 positions are most important for inhibitor binding, whilst the P3 and P4 positions have much less effect
-
additional information
-
human leukocyte antigen A2restricted epitope in which substitutions at 5 of 9 residues destroy the protease
-
additional information
O92972
EGTA and zinc metalloprotease inhibitors bestatin, phosphoramidon and thiorphan have no effect on NS2/3 auto-cleavage and NS3 protease activity. No inhibitory effect of the NS4A peptide on NS2/3 auto-cleavage, additionally the NS4A peptide does not significantly affect the sensitivity of NS2/3 autocleavage to zinc chelation, but has a marked effect on NS3 protease activity, rendering this activity approximately 3fold more resistant to zinc chelation
-
additional information
-
methylated 3,3'-digalloylproprodelphinidin B2, hexanoylated (-)-epigallocatechin-3-O-gallate, (-)-epigallocatechin, (-)-epicatechin, gallic acid, luetolin, tyrosol and salidroside show no activity up to 100 micromol
-
additional information
-
two galloyl residues at 3 and 4 positions of the glucopyranose ring of the plant inhibitors interact with SER139, GLY137, ALA157, and ASP81 by hydrogen bond interaction and with ALA156 and HIE57 by hydrophobic interaction and are essential for the activities of the inhibitors
-
additional information
-
compounds with urea cappings are more potent and selective than their carbamate counterparts
-
additional information
-
protease is susceptible to feedback inhibition by the N-terminal products released from the polyprotein substrate after enzymatic cleavage
-
additional information
-
14-membered ring system is the most potent.The corresponding 13-, 15-, and 16-membered macrocyclic rings deliver less potent inhibitors. Corresponding P1 acylsulfonamides have superior potencies over the corresponding P1 carboxylic acids. Highly potent protease inhibitors lack the P4 substituent
-
additional information
-
cleavage products and their analogs do not appreciably inhibit the Dengue NS3 protease. Inhibitors with electrophilic warheads, such as aldehyde, trifluoromethyl ketone, and boronic acid, are needed to see effective inhibition of the enzyme activity. Among warheads, tetrapeptide boronic acid has the highest affinity
-
additional information
-
P2 Arg residue is more important for enzyme interactions than P1 Arg. Tri- and dipeptide aldehyde inhibitors afford low micromolar activity
-
additional information
-
macrocyclic peptidic inhibitors, are less susceptible to hydrolytic degradation by proteases, have markedly improved oral absorption, and pharmacokinetic properties compared to corresponding acyclic analogs
-
additional information
-
electrophilic compounds with a pentafluoroethyl ketone group show stronger inhibition at pH 8 than pH 6, the difference is only significant at high ionic strength. Electrophilic compounds with an acidic C-terminal group or a cyclic P1 residue show a lower inhibitory effect at pH 8 than at pH 6, inconsistent with a mechanism-based inhibition. All electrophilic compounds have a strong inhibition at pH 6, when mechanism-based inhibition is unlikely
-
additional information
-
decrease in the efficiency of expression of NS3/4A protease, as the concentration of Hepatitis C virus-infected cells increases
-
additional information
-
not inhibited by BMS-858
-
additional information
-
no inhibition by bestatin, EDTA, Mn2+, Mg2+, Ca2+, K+
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
4A cofactor peptide
-
-
-
DTT
-
required for maximal activity
NS2B
-
viral activator protein
-
NS4A
-
cofactor for efficient for efficient cleavage at four sites in the nonstructural region, biological importance of the NS4A N-terminus, in fully potentiating NS3 enzymatic activity
-
NS4A
-
enhances the activity of NS3 protease in all cleavages via the formation of an NS3/NS4A; NS4A is a 54 residue amphipathic peptide acting as a cofactor and possibly assisting the membrane-localization of NS3
-
NS4A
-
enhances the activity of NS3 protease in all cleavages via the formation of an NS3/NS4A; hydrophobic central core of NS4A corresponding to residues 21-34, kinetic value for a modified peptide modified with a KK residue at the C-terminus to enhance solubility, Km: 0.00076 mM, kcat: 9 per min
-
NS4A
-
enhances the activity of NS3 protease in all cleavages via the formation of an NS3/NS4A
-
NS4A cofactor peptide
-
NS3-NS4A interaction consists of a high-affinity and a low-affinity interaction, contributing equally to the overall binding. By immobilizing NS3 alone or together with NS4A it is shown that inhibitors have a higher affinity for NS3 in the presence of NS4A. NS4A thus has a direct effect on the binding of inhibitors to NS3 and not only on catalysis
-
NS4A peptide
-
-
-
NS4A protein
-
NS4A serves as a cofactor for NS3 protease and helicase activities
-
Pep4AK
-
cofactor, peptide spanning the central hydrophobic core of the NS4A protein, with a three-lysine tag at the N-terminus
-
SP6EVC/S
-
inhibits by slow tight binding mechanism characteristics of serpin molecules, operating as a suicide substrate inhibitor. HCV-Pep4A is required for efficient formation of SDS-stable complex between NS3 protein and SP6EVC/S
-
Triton X-100
-
required for maximal activity
additional information
O92972
both auto-cleavage and NS3 protease activity show absolute requirement for cysteine residues 1123, 1125 and 1171 within NS3. Cysteine 922 (within NS2) is only required for NS2/3 auto-cleavage activity and histidine 1175 is only required for NS3 activity. Complete NS3 protease domain (including the C-terminal alpha-helix) is required for NS2/3 auto-cleavage, the activity of the NS3 protease is not essential
-
additional information
-
presence of basic residues at the P3 and P4 positions significantly promotes reactivity
-
KM VALUE [mM]
KM VALUE [mM] Maximum
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.0658
-
2-Naph-3Pya-Lys-Arg-p-nitroanilide
-
-
0.021
-
2-Naph-Cit-Lys-Arg-p-nitroanilide
-
-
0.1007
-
2-Naph-Cit-Orn-Arg-p-nitroanilide
-
-
0.048
-
2-Naph-hArg-Lys-Arg-p-nitroanilide
-
-
2.303
-
2-Naph-Lys-AcLys-Arg-p-nitroanilide
-
-
0.0434
-
2-Naph-Lys-Arg-Arg-p-nitroanilide
-
-
3.423
-
2-Naph-Lys-Cit-Arg-p-nitroanilide
-
-
0.0267
-
2-Naph-Lys-hArg-Arg-p-nitroanilide
-
-
0.0254
-
2-Naph-Lys-Lys-Arg-p-nitroanilide
-
-
0.0977
-
2-Naph-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant V154F
0.0368
-
2-Naph-Lys-Orn-Arg-p-nitroanilide
-
-
0.038
-
2-Naph-Orn-Lys-Arg-p-nitroanilide
-
-
0.0229
-
2-Naph-Orn-Orn-Arg-p-nitroanilide
-
-
0.00076
-
7-methoxycoumarin-4-acetyl-DEMEECASHLPYK-(epsilon-NHCOCH3)
-
presence of inhibitor peptide 4Apep21-34KK
-
0.0292
-
7-methoxycoumarin-4-acetyl-DEMEECASHLPYK-(epsilon-NHCOCH3)
-
-
-
0.0436
-
7-methoxycoumarin-4-acetyl-EDASTPCSGSN-(4-nitro)Phe
-
presence of inhibitor peptide 4Apep21-34KK
-
0.053
-
9-fluorenylmethyloxycarbonyl-YQEFDEMEECASHLPYIEQG
-
-
-
0.0045
-
Abz-RRRRSAGnY-amide
-
-
0.0797
-
Ac-Aib-Lys-Lys-Arg-p-nitroanilide
-
-
0.0755
-
Ac-Aoc-Lys-Lys-Arg-p-nitroanilide
-
-
0.0227
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
-
in the presence of 0.0174% DDM
0.03
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
-
-
0.0367
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
-
operating at wavelengths 515 nm/605 nm (excitation/emission)
0.03984
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
-
operating at wavelengths 524 nm/600 nm (excitation/emission)
0.0699
-
Ac-Cha-Lys-Lys-Arg-p-nitroanilide
-
-
0.0819
-
Ac-Chg-Lys-Lys-Arg-p-nitroanilide
-
-
0.063
-
Ac-DEEMECASHLPYK-NH2
-
wild-type NS3 protease plus cofactor NS4A, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT
-
0.087
-
Ac-DEEMECASHLPYK-NH2
-
engineered single-chain protease plus cofactor NS4A, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT
-
0.088
-
Ac-DEEMECASHLPYK-NH2
-
engineered single-chain protease, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT
-
0.102
-
Ac-DEEMECASHLPYK-NH2
-
wild-type NS3 protease, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT
-
0.403
-
Ac-DEEMECASHLPYK-NH2
-
wild-type NS3 protease plus cofactor NS4A, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT, 150 mM NaCl
-
0.49
-
Ac-DEEMECASHLPYK-NH2
-
wild-type NS3 protease, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT, 150 mM NaCl
-
0.502
-
Ac-DEEMECASHLPYK-NH2
-
engineered single-chain protease plus cofactor NS4A, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT, 150 mM NaCl
-
0.519
-
Ac-DEEMECASHLPYK-NH2
-
engineered single-chain protease, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT, 150 mM NaCl
-
0.74
-
Ac-DPNRKR-4-nitroanilide
-
37C, pH 9.5
0.0012
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 3 mutant R123T, 30C, pH 6.5
0.0026
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 enzyme, 30C, pH 6.5
0.0034
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 and 3 mutant V132L, 30C, pH 6.5
0.0039
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 1b enzyme, 30C, pH 6.5
0.0042
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 3 mutant D168Q, 30C, pH 6.5
0.0044
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant S122K/V132L, 30C, pH 6.5
0.0047
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant V78A/D79E/Q80G/S122K/V321L, 30C, pH 6.5
0.0048
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant S122K, 30C, pH 6.5
0.005
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant T160A, 30C, pH 6.5; genotype 3 mutant R123T/D168Q/V132L, 30C, pH 6.5
0.0051
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 3 mutant R123T/D168Q, 30C, pH 6.5
0.0055
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant Q80G, 30C, pH 6.5
0.0058
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant D79E, 30C, pH 6.5
0.0059
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant V78A, 30C, pH 6.5
0.0072
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 3 enzyme, 30C, pH 6.5
0.0073
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant V78A/D79E/Q80G, 30C, pH 6.5
3.1
-
Ac-EMEECASHLP
-
-
-
0.45
-
Ac-FASGKR-4-nitroanilide
-
37C, pH 9.5
0.17
-
Ac-KPGLKR-4-nitroanilide
-
wild-type, pH 9.5, 37C
0.246
-
Ac-KPGLKR-4-nitroanilide
-
mutant Y150F, pH 9.5, 37C
0.357
-
Ac-KPGLKR-4-nitroanilide
-
mutant S160A, pH 9.5, 37C
0.36
-
Ac-KPGLKR-4-nitroanilide
-
mutant V115A, pH 9.5, 37C
0.561
-
Ac-KPGLKR-4-nitroanilide
-
mutant D129E, pH 9.5, 37C
0.611
-
Ac-KPGLKR-4-nitroanilide
-
mutant D129N, pH 9.5, 37C
0.821
-
Ac-KPGLKR-4-nitroanilide
-
37C, pH 9.5
2.942
-
Ac-KPGLKR-4-nitroanilide
-
mutant D129A, pH 9.5, 37C
1.1
-
Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2
-
wild-type, pH 7.8, 30C
1.3
-
Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2
-
mutant A156T, pH 7.8, 30C
2.6
-
Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2
-
mutant A156V, pH 7.8, 30C
0.0887
-
Ac-Leu-3Pya-Lys-Arg-p-nitroanilide
-
-
0.2548
-
Ac-Leu-4Pya-Lys-Arg-p-nitroanilide
-
-
0.1413
-
Ac-Leu-aPhe-Lys-Arg-p-nitroanilide
-
-
0.2086
-
Ac-Leu-Cit-Lys-Arg-p-nitroanilide
-
-
0.199
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
-
0.232
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant V166L
0.344
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant V154L
0.376
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant T111F
0.416
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant I162F
0.617
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant T111L
0.879
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant M156A
0.0625
-
Ac-Leu-hArg-Lys-Arg-p-nitroanilide
-
-
0.0546
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
-
0.096
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant V166L
0.164
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant M156A
0.169
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant T111F
0.19
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant V154L
0.207
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant I155F
0.214
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant T111L
0.221
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant A164S
0.263
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant V154F
0.268
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant I162F
0.331
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant A164V
0.432
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant D129E
0.635
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant D129A
0.2541
-
Ac-Leu-nPhe-Lys-Arg-p-nitroanilide
-
-
0.1055
-
Ac-Leu-Orn-Lys-Arg-p-nitroanilide
-
-
0.892
-
Ac-LQYTKR-4-nitroanilide
-
37C, pH 9.5
0.0807
-
Ac-Nle-Lys-Lys-Arg-p-nitroanilide
-
-
0.0673
-
Ac-Nva-Lys-Lys-Arg-p-nitroanilide
-
-
0.1342
-
Ac-Tbg-Lys-Lys-Arg-p-nitroanilide
-
-
0.15
-
Ac-YQEFDEMEECAS
-
-
-
0.11
-
Ac-YQEFDEMEECASH
-
-
-
0.12
-
Ac-YQEFDEMEECASHL
-
-
-
0.095
-
Ac-YQEFDEMEECASHLP
-
-
-
0.0028
-
acetyl-DEMEECASHLPYL-(epsilon-NHCOCH3)
-
presence of inhibitor peptide 4Apep21-34KK
0.0013
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 4a, in 1 M MES (pH 5.8), at 23C
0.0021
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 1b, in 1 M MES (pH 5.8), at 23C
0.0028
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 6a, in 1 M MES (pH 5.8), at 23C
0.0035
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 2a, in 1 M MES (pH 5.8), at 23C
0.0066
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 5a, in 1 M MES (pH 5.8), at 23C
0.0029
-
anthranilyl-DDIVPAbu[C(O)-O]AMY(3-NO2)TW-OH
-
single chain NS3 protease domain, at 23C
0.0042
-
anthranilyl-DDIVPAbu[C(O)-O]AMY(3-NO2)TW-OH
-
mutant full-length protease M485A/V524A/Q562A, at 23C
0.1422
-
Boc-Gly-Arg-Arg-AMC
-
-
0.12
-
Boc-GRR-7-amido-4-methylcoumarin
-
37C, pH 8.5
0.041
-
Boc-RVRR-7-amido-4-methylcoumarin
-
pH 8.0, 18C
0.0062
-
Bz-nKRR-7-amido-3-carbamoylmethyl-4-methylcoumarin
-
37C, pH 8.5
0.202
-
Bz-nKTR-7-amido-3-carbamoylmethyl-4-methylcoumarin
-
37C, pH 8.5
0.0146
-
Bz-norleucine-lysine-arginine-arginine-AMC
-
-
0.071
-
Bz-nTRR-7-amido-3-carbamoylmethyl-4-methylcoumarin
-
37C, pH 8.5
0.0066
-
Bz-TKRR-7-amido-3-carbamoylmethyl-4-methylcoumarin
-
37C, pH 8.5
0.36
-
Bz-TTRR-7-amido-3-carbamoylmethyl-4-methylcoumarin
-
37C, pH 8.5
10
-
DEMEECASHLPYK
-
-
0.16
-
DEMEECSQHLPYI
-
presence of cofactor
0.805
-
DEMEECSQHLPYI
-
absence of cofactor
0.019
-
DTEDVVCCSMSYTWTGK
-
protease NS4A(21-32)-GSGS-NS3(3-181)
0.02
-
DTEDVVCCSMSYTWTGK
-
protease NS3(1-631)/NS4A(1-54)
0.08
-
DTEDVVCCSMSYTWTGK
-
protease NS3(1-181)/NS4A
0.0004
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme K136M
0.0005
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme K165S; pH 7.5, wild-type enzyme
0.001
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme R161S
0.0012
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme K136M/R109Q; pH 7.5, mutant enzyme R123T; pH 7.5, mutant enzyme R155S
0.0018
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme R109Q
0.0054
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme K165S/R161S
0.0041
-
EAGDNIVPCSMSYTWTGA-OH
-
pH 7.5, wild-type enzyme
0.0038
-
EAGNDIVPCSMSYTWTGA-OH
-
pH 7.5, wild-type enzyme
0.0252
-
EAGNNIVPCSMSYTWTGA-OH
-
pH 7.5, wild-type enzyme
0.029
-
EDVV-4-aminobutyryl-CSMSY
-
mutant V36L, in the presence of cofactor peptide KKGSVVIVGRIVLSCK
0.032
-
EDVV-4-aminobutyryl-CSMSY
-
presence of cofactor
0.051
-
EDVV-4-aminobutyryl-CSMSY
-
mutant V36M, in the presence of cofactor peptide KKGSVVIVGRIVLSCK
0.053
-
EDVV-4-aminobutyryl-CSMSY
-
wild-type, genotype 1a, in the presence of cofactor peptide KKGSVVIVGRIVLSCK
0.18
-
EDVV-4-aminobutyryl-CSMSY
-
mutant V36M/R155K, in the presence of cofactor peptide KKGSVVIVGRIVLSCK
0.27
-
EDVV-4-aminobutyryl-CSMSY
-
absence of cofactor
0.29
-
EDVV-4-aminobutyryl-CSMSY
-
wild-type, genotype 1b, in the presence of cofactor peptide KKGSVVIVGRIVLSCK
0.38
-
EDVV-4-aminobutyryl-CSMSY
-
mutant V36A, in the presence of cofactor peptide KKGSVVIVGRIVLSCK
0.053
-
EDVV-Abu-CSMSY
-
wild-type
0.068
-
EDVV-Abu-CSMSY
-
mutant R155T
0.168
-
EDVV-Abu-CSMSY
-
mutant R155K
0.552
-
EDVV-Abu-CSMSY
-
mutant R155S
3.8
-
EDVVAbuCSMSY-NH2
-
-
1.01
-
Glu-Asp-Val-Val-4-aminobutyryl-Cys-p-nitroanilide
-
presence of cofactor
0.051
-
o-aminobenzoyl (Abz)-L-Asp-L-Asp-L-Ile-L-Val-L-Pro-L-Cys-L-Ser-L-Met-L-Ser-L-Tyr(3-NO2)-L-Thr-NH2
-
pH 7.3, 30C
0.043
-
Pyr-RTKR-7-amido-4-methylcoumarin
-
pH 8.0, 18C
0.146
-
Z-RR-7-amido-4-methylcoumarin
-
pH 8.0, 18C
1.08
-
Glu-Asp-Val-Val-4-aminobutyryl-Cys-p-nitroanilide
-
absence of cofactor
additional information
-
additional information
-
-
-
TURNOVER NUMBER [1/s]
TURNOVER NUMBER MAXIMUM[1/s]
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.96
-
2-Naph-3Pya-Lys-Arg-p-nitroanilide
-
-
0.32
-
2-Naph-Cit-Lys-Arg-p-nitroanilide
-
-
0.57
-
2-Naph-Cit-Orn-Arg-p-nitroanilide
-
-
0.11
-
2-Naph-hArg-Lys-Arg-p-nitroanilide
-
-
0.3
-
2-Naph-Lys-AcLys-Arg-p-nitroanilide
-
-
0.89
-
2-Naph-Lys-Arg-Arg-p-nitroanilide
-
-
0.43
-
2-Naph-Lys-Cit-Arg-p-nitroanilide
-
-
0.59
-
2-Naph-Lys-hArg-Arg-p-nitroanilide
-
-
0.0431
-
2-Naph-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant V154F
1.08
-
2-Naph-Lys-Lys-Arg-p-nitroanilide
-
-
1.58
-
2-Naph-Lys-Orn-Arg-p-nitroanilide
-
-
0.98
-
2-Naph-Orn-Lys-Arg-p-nitroanilide
-
-
0.27
-
2-Naph-Orn-Orn-Arg-p-nitroanilide
-
-
0.006
-
7-methoxycoumarin-4-acetyl-DEMEECASHLPYK-(epsilon-NHCOCH3)
-
-
-
0.15
-
7-methoxycoumarin-4-acetyl-DEMEECASHLPYK-(epsilon-NHCOCH3)
-
presence of inhibitor peptide 4Apep21-34KK
-
0.227
-
7-methoxycoumarin-4-acetyl-EDASTPCSGSN-(4-nitro)Phe
-
presence of inhibitor peptide 4Apep21-34KK
-
0.00833
-
9-fluorenylmethyloxycarbonyl-YQEFDEMEECASHLPYIEQG
-
-
-
0.005
-
Abz-AGRK-SLTnY-amide
-
-
0.001
-
Abz-AGRK-SnY-amide
-
-
0.0967
-
Abz-KKQR-SAGMnY-amide
-
-
0.0045
-
Abz-SKKR-AGVLnY-amide
-
-
0.045
-
Abz-SKKR-SAGMnY-amide
-
-
1.6
-
Ac-Aib-Lys-Lys-Arg-p-nitroanilide
-
-
2.51
-
Ac-Aoc-Lys-Lys-Arg-p-nitroanilide
-
-
0.6
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
-
-
1
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
-
operating at wavelengths 524 nm/600 nm (excitation/emission)
1.2
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
-
operating at wavelengths 515 nm/605 nm (excitation/emission)
7.2
-
Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
-
in the presence of 0.0174% DDM
2.28
-
Ac-Cha-Lys-Lys-Arg-p-nitroanilide
-
-
1.78
-
Ac-Chg-Lys-Lys-Arg-p-nitroanilide
-
-
0.00167
-
Ac-DEEMECASHLPYK-NH2
-
wild-type NS3 protease, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT
-
0.00183
-
Ac-DEEMECASHLPYK-NH2
-
wild-type NS3 protease, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT, 150 mM NaCl
-
0.0233
-
Ac-DEEMECASHLPYK-NH2
-
wild-type NS3 protease plus cofactor NS4A, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT
-
0.0253
-
Ac-DEEMECASHLPYK-NH2
-
engineered single-chain protease, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT
-
0.0255
-
Ac-DEEMECASHLPYK-NH2
-
engineered single-chain protease plus cofactor NS4A, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT
-
0.0267
-
Ac-DEEMECASHLPYK-NH2
-
wild-type or engineered single-chain protease plus cofactor NS4A, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT, 150 mM NaCl
-
0.03
-
Ac-DEEMECASHLPYK-NH2
-
engineered single-chain protease, in 50 mM HEPES buffer, pH 7.5, 0.1% 1-O-n-octyl-beta-D-glucopyranoside, 15% glycerol, 30 mM DTT, 150 mM NaCl
-
1.3
-
Ac-DPNRKR-4-nitroanilide
-
37C, pH 9.5
0.033
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 3 mutant D168Q, 30C, pH 6.5
0.095
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 and 3 mutant V132L, 30C, pH 6.5
0.13
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 3 mutant R123T, 30C, pH 6.5
0.133
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant V78A/D79E/Q80G/S122K/V321L, 30C, pH 6.5
0.16
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant V78A/D79E/Q80G, 30C, pH 6.5
0.2
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant T160A, 30C, pH 6.5
0.22
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant D79E, 30C, pH 6.5; genotype 2 mutant Q80G, 30C, pH 6.5
0.25
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant S122K/V132L, 30C, pH 6.5; genotype 3 mutant R123T/D168Q, 30C, pH 6.5
0.3
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant V78A, 30C, pH 6.5; genotype 3 mutant R123T/D168Q/V132L, 30C, pH 6.5
0.4
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 1b enzyme, 30C, pH 6.5
0.43
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 enzyme, 30C, pH 6.5
0.57
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 3 enzyme, 30C, pH 6.5
0.58
-
Ac-DTEDVVP(Nva)-O-4-phenylazophenyl ester
P27958
genotype 2 mutant S122K, 30C, pH 6.5
0.005
-
Ac-EMEECASHLP
-
-
-
1.9
-
Ac-FASGKR-4-nitroanilide
-
37C, pH 9.5
0.011
-
Ac-KPGLKR-4-nitroanilide
-
mutant D129A, pH 9.5, 37C
0.019
-
Ac-KPGLKR-4-nitroanilide
-
mutant D129E, pH 9.5, 37C
0.038
-
Ac-KPGLKR-4-nitroanilide
-
mutant D129N, pH 9.5, 37C
0.133
-
Ac-KPGLKR-4-nitroanilide
-
mutant Y150F, pH 9.5, 37C
0.394
-
Ac-KPGLKR-4-nitroanilide
-
mutant S160A, pH 9.5, 37C
0.872
-
Ac-KPGLKR-4-nitroanilide
-
mutant V115A, pH 9.5, 37C
0.965
-
Ac-KPGLKR-4-nitroanilide
-
wild-type, pH 9.5, 37C
1.5
-
Ac-KPGLKR-4-nitroanilide
-
37C, pH 9.5
6.08
-
Ac-KPGLKR-4-nitroanilide
-
mutant V115A, pH 9.5, 37C; wild-type, pH 9.5, 37C
0.2
-
Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2
-
mutant A156T, pH 7.8, 30C
0.6
-
Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2
-
mutant A156V, pH 7.8, 30C
1
-
Ac-L-Asp-L-Glu-L-Asp-(EDANS)-L-Glu-L-Glu-alpha-aminobutyric acid-PSI[COO]-L-Ala-L-Ser-L-Lys-(DABCYL)-NH2
-
wild-type, pH 7.8, 30C
0.5
-
Ac-Leu-3Pya-Lys-Arg-p-nitroanilide
-
-
0.9
-
Ac-Leu-4Pya-Lys-Arg-p-nitroanilide
-
-
0.75
-
Ac-Leu-aPhe-Lys-Arg-p-nitroanilide
-
-
1.44
-
Ac-Leu-Cit-Lys-Arg-p-nitroanilide
-
-
0.018
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant T111L
0.04
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant I162F
0.051
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant T111F
0.245
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant V154L
0.266
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
-
0.297
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant V166L
0.314
-
Ac-Leu-Gln-Tyr-Thr-Lys-Arg-p-nitroanilide
-
NS3 mutant M156A
118
-
Ac-Leu-hArg-Lys-Arg-p-nitroanilide
-
-
0.036
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant D129E
0.048
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant D129A
0.057
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant V154F
0.06
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant T111L
0.164
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant I162F
0.181
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant A164V
0.198
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant T111F
0.26
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant A164S
0.638
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant V166L
0.733
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant I155F
0.778
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant M156A
0.8
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
NS3 mutant V154L
1.64
-
Ac-Leu-Lys-Lys-Arg-p-nitroanilide
-
-
0.72
-
Ac-Leu-nPhe-Lys-Arg-p-nitroanilide
-
-
1.79
-
Ac-Leu-Orn-Lys-Arg-p-nitroanilide
-
-
1.1
-
Ac-LQYTKR-4-nitroanilide
-
37C, pH 9.5
2.35
-
Ac-Nle-Lys-Lys-Arg-p-nitroanilide
-
-
2.36
-
Ac-Nva-Lys-Lys-Arg-p-nitroanilide
-
-
1.74
-
Ac-Tbg-Lys-Lys-Arg-p-nitroanilide
-
-
0.005
-
Ac-YQEFDEMEECAS
-
-
-
0.00333
-
Ac-YQEFDEMEECASH
-
-
-
0.00667
-
Ac-YQEFDEMEECASHL, Ac-YQEFDEMEECASHLP
-
-
-
0.143
-
acetyl-DEMEECASHLPYL-(epsilon-NHCOCH3)
-
presence of inhibitor peptide 4Apep21-34KK
0.21
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 4a, in 1 M MES (pH 5.8), at 23C
0.77
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 1b, in 1 M MES (pH 5.8), at 23C
0.83
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 6a, in 1 M MES (pH 5.8), at 23C
0.85
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 2a, in 1 M MES (pH 5.8), at 23C
1.7
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 5a, in 1 M MES (pH 5.8), at 23C
0.62
-
anthranilyl-DDIVPAbu[C(O)-O]AMY(3-NO2)TW-OH
-
mutant full-length protease M485A/V524A/Q562A, at 23C
2.5
-
anthranilyl-DDIVPAbu[C(O)-O]AMY(3-NO2)TW-OH
-
single chain NS3 protease domain, at 23C
0.034
-
Boc-Gly-Arg-Arg-AMC
-
-
0.03
-
Boc-GRR-7-amido-4-methylcoumarin
-
37C, pH 8.5
0.073
-
Boc-RVRR-7-amido-4-methylcoumarin
-
pH 8.0, 18C
0.32
-
Bz-nKRR-7-amido-3-carbamoylmethyl-4-methylcoumarin
-
37C, pH 8.5
0.97
-
Bz-nKTR-7-amido-3-carbamoylmethyl-4-methylcoumarin
-
37C, pH 8.5
0.111
-
Bz-norleucine-lysine-arginine-arginine-AMC
-
-
0.28
-
Bz-nTRR-7-amido-3-carbamoylmethyl-4-methylcoumarin
-
37C, pH 8.5
0.05
-
Bz-TKRR-7-amido-3-carbamoylmethyl-4-methylcoumarin
-
37C, pH 8.5
0.21
-
Bz-TTRR-7-amido-3-carbamoylmethyl-4-methylcoumarin
-
37C, pH 8.5
0.05
-
DEMEECSQHLPYI
-
absence of cofactor
0.243
-
DEMEECSQHLPYI
-
presence of cofactor
0.05
-
DTEDVVCCSMSYTWTGK
-
protease NS3(1-181)/NS4A
0.167
-
DTEDVVCCSMSYTWTGK
-
protease NS3(1-631)/NS4A(1-54)
0.317
-
DTEDVVCCSMSYTWTGK
-
protease NS4A(21-32)-GSGS-NS3(3-181)
0.083
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme K136M/R109Q
0.167
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme K136M
0.59
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme R109Q
0.7
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, wild-type enzyme
0.72
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme K165S/R161S
0.77
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme R161S
0.78
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme R155S
0.85
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme R123T
0.95
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme K165S
6.08
-
EAGDDIVPCSMSYTWTGA-OH
-
pH 7.5, mutant enzyme K165S/R161S; pH 7.5, mutant enzyme R109Q; pH 7.5, mutant enzyme R155S; pH 7.5, mutant enzyme R161S
0.8
-
EAGDNIVPCSMSYTWTGA-OH
-
pH 7.5, wild-type enzyme
0.7
-
EAGNDIVPCSMSYTWTGA-OH
-
pH 7.5, wild-type enzyme
0.67
-
EAGNNIVPCSMSYTWTGA-OH
-
pH 7.5, wild-type enzyme
6.08
-
EAGNNIVPCSMSYTWTGA-OH
-
pH 7.5, wild-type enzyme
0.18
-
EDVV-4-aminobutyryl-CSMSY
-
absence of cofactor
0.6
-
EDVV-4-aminobutyryl-CSMSY
-
presence of cofactor
0.012
-
Glu-Asp-Val-Val-4-aminobutyryl-Cys-p-nitroanilide
-
absence of cofactor
0.0065
-
o-aminobenzoyl (Abz)-L-Asp-L-Asp-L-Ile-L-Val-L-Pro-L-Cys-L-Ser-L-Met-L-Ser-L-Tyr(3-NO2)-L-Thr-NH2
-
pH 7.3, 30C
43
-
Pyr-RTKR-7-amido-4-methylcoumarin
-
pH 8.0, 18C
0.062
-
Z-RR-7-amido-4-methylcoumarin
-
pH 8.0, 18C
0.2
-
Glu-Asp-Val-Val-4-aminobutyryl-Cys-p-nitroanilide
-
presence of cofactor
additional information
-
additional information
-
-
-
kcat/KM VALUE [1/mMs-1]
kcat/KM VALUE [1/mMs-1] Maximum
SUBSTRATE
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
160
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 4a, in 1 M MES (pH 5.8), at 23C
302592
230
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 2a, in 1 M MES (pH 5.8), at 23C
302592
260
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 5a, in 1 M MES (pH 5.8), at 23C
302592
300
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 6a, in 1 M MES (pH 5.8), at 23C
302592
370
-
anthraniloyl-DDIVP-Abu[C(O)-O] AMY(3-NO2)-TW-OH
-
enzyme from hepatitis C virus genotype 1b, in 1 M MES (pH 5.8), at 23C
302592
150
-
anthranilyl-DDIVPAbu[C(O)-O]AMY(3-NO2)TW-OH
-
mutant full-length protease M485A/V524A/Q562A, at 23C
302593
840
-
anthranilyl-DDIVPAbu[C(O)-O]AMY(3-NO2)TW-OH
-
single chain NS3 protease domain, at 23C
302593
Ki VALUE [mM]
Ki VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.00000009
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclobutane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000122
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclohexane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000009
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopentane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.0000001
-
(1'R,21'S,24'S)-21'-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3',19',22'-trioxo-2',18'-dioxa-4',20',23'-triazaspiro[cyclopropane-1,16'-tetracyclo-[21.2.1.14,7.06,11]heptacosane]-6',8',10'-triene-24'-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.0012
-
(10R,13R)-N-(1-[[(2-[[(1R)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10-cyclohexyl-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
0.00039
-
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-oxo-2,7-dioxa-8-thia-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide 8,8-dioxide
-
-
0.00032
-
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2,7-dioxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
0.00031
-
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
0.00017
-
(10S,13S)-10-cyclohexyl-N-(1-[[(2-[[(1S)-2-(methylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-8,11-dioxo-2-oxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-triene-13-carboxamide
-
-
0.00016
-
(11R,14R)-N-(1-[[(2-[[(1R)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-cyclohexyl-9,12-dioxo-2-oxa-10,13-diazabicyclo[14.3.1]icosa-1(20),16,18-triene-14-carboxamide
-
-
0.0011
-
(11S,14S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11-cyclohexyl-9,12-dioxo-1,10,13,17-tetraazabicyclo[14.2.1]nonadeca-16(19),17-diene-14-carboxamide
-
-
0.0000001
-
(1R,12E,19S,22S)-19-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,17,20-trioxo-2,16-dioxa-4,18,21-triazatetracyclo[19.2.1.14,7.06,11]pentacosa-6,8,10,12-tetraene-22-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000005
-
(1R,12E,20S,23S)-20-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000002
-
(1R,12E,20S,23S)-20-cyclohexyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000004
-
(1R,12E,20S,23S)-20-cyclopentyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000004
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000005
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.0000016
-
(1R,12E,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-4-methyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatricyclo[20.2.1.06,11]pentacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000006
-
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-(1-methylcyclohexyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000004
-
(1R,12E,20S,23S)-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-vinylcyclopropyl)-20-isopropyl-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10,12-tetraene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000003
-
(1R,12E,21S,24S)-21-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10,12-tetraene-24-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000002
-
(1R,12E,22S,25S)-22-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,20,23-trioxo-2,19-dioxa-4,21,24-triazatetracyclo[22.2.1.14,7.06,11]octacosa-6,8,10,12-tetraene-25-carboxamide
-
Ki below 0.00000002 mM, in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000045
-
(1R,20S,23S)-20-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000005
-
(1R,20S,23S)-20-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3,18,21-trioxo-2,17-dioxa-4,19,22-triazatetracyclo[20.2.1.14,7.06,11]hexacosa-6,8,10-triene-23-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.0000003
-
(1R,21S,24S)-21-(tert-butoxymethyl)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000009
-
(1R,21S,24S)-21-cyclohexyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]-heptacosa-6,8,10-triene-24-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000018
-
(1R,21S,24S)-21-tert-butyl-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-ethylcyclopropyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00000008
-
(1R,21S,24S)-N-((1R,2R)-1-[[(cyclopropylsulfonyl)amino]-carbonyl]-2-ethylcyclopropyl)-16,16-dimethyl-21-(1-methylcyclohexyl)-3,19,22-trioxo-2,18-dioxa-4,20,23-triazatetracyclo[21.2.1.14,7.06,11]heptacosa-6,8,10-triene-24-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.000016
-
(1R,2S)-1-[([(1R,2R,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopentyl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.0000013
-
(1R,2S)-1-[([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.0000011
-
(1R,2S)-1-[([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.000023
-
(1R,2S)-1-[([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.000108
-
(1R,2S)-1-[([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.0027
-
(1R,2S)-1-[[(1R,2R,4S)-2-((S)-1-cyclopentylcarbamoyl-2,2-dimethyl-propylcarbamoyl)-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
0.0069
-
(1R,2S)-1-[[(1R,2R,4S)-2-((S)-1-tert-butylcarbamoyl-2,2-dimethyl-propylcarbamoyl)-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
0.000016
-
(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyldimethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethylpropylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
0.000022
-
(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
0.01
-
(1R,2S)-1-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-methyl-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
-
0.005
-
(1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl](methyl)carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.000024
-
(1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylic acid
-
-
0.000004
-
(1R,5S)-3-(N-[[(1S)-1-cyclohexyl-2-cyclopropyl-2-oxoethyl]carbamoyl]-3-methyl-L-valyl)-N-[1-(cyclopropylamino)-1,2-dioxohept-6-yn-3-yl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
pH and temperature not specified in the publication
-
0.000007
-
(1R,5S)-3-[2(S)-[[[[1-[[[cyclobutyl(methyl)amino]sulfonyl]methyl]cyclohexyl]amino] carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000014
-
(1R,5S)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-[N-(tert-butylcarbamoyl)-3-methyl-L-valyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
pH and temperature not specified in the publication
-
0.000006
-
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyll]-butyl]-3-[2(S)-[[[[1-[[(dimethylamino)sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000002
-
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[(2S)-2-[[[[1-[1(R)-[(dimethylamino)sulfonyl]ethyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyll-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000004
-
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-(2-cyclopropyl-1,1-dioxido-5(R)-isothiazolidinyl)cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.0000028
-
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[(2-fluoro-1,1-dimethylethyl)methylamino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000006
-
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[cyclopropyl(1-methylethyl)amino]-sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000008
-
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)amino]sulfonyl]-methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000009
-
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[2(S)-[[[[1-[[[ethyl(methyl)amino]sulfonyl]methyl]-cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000008
-
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[3,3-dimethyl-2(S)-[[[[1-[(4-morpholinylsulfonyl)-methyl]cyclohexyl]amino]carbonyl]amino]-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000007
-
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-butyl]-3-[3,3-dimethyl-2(S)-[[[[1-[[[methyl(1-me5thylethyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000011
-
(1R,5S)-N-[1(S)-[2-(cyclopropylamino)-1,2-dioxoethyl]-pemtyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)amino]sulfonyl]-methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000004
-
(1R,5S)-N-[3-(cyclopropylamino)-1(S)-(2-cyclopropylethyl)-2,3-dioxopropyl]-3-[2(S)-[[[[1-[[[cycloppropyl(methyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000015
-
(1R,5S)-N-[3-(cyclopropylamino)-1(S)-(cyclopropylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[[1-[[[cyclopropyl(methyl)-amino]sulfonyl]methyl]cyclohexyl]amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]-hexane-2(S)-carboxamide
-
pH and temperature not specified in the publication
0.000014
-
(1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide
-
-
0.00011
-
(1S,3aR,6aS)-2-((S)-2-((S)-2-cyclohexyl-2-(pyrazine-2-carboxamido)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(cyclopropylamino)-1,2-dioxohexan-3-yl)octahydrocyclopenta[c]pyrrole-1-carboxamide
-
-
0.0001
-
(1S,5R)-6,6-dichloro-3-[cyclohexyl[[[(1,1-dimethylethyl)amino]carbonyl]amino]acetyl]-N-[1-[1,2-dioxo-2-(2-propenylamino)ethyl]butyl]-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide
-
-
0.000006
-
(1S,5R)-N-((S)-5-cyclopropyl-1-(cyclopropylamino)-1,2-dioxopentan-3-yl)-3-((S)-2-(3-(1-((N-cyclopropyl-N-methylsulfamoyl)methyl)cyclohexyl)ureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
pH and temperature not specified in the publication
0.00036
-
(1S,5R)-N-(1-amino-5,5-difluoro-1,2-dioxoheptan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.00023
-
(1S,5R)-N-(1-amino-5,5-difluoro-1,2-dioxohexan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.000065
-
(1S,5R)-N-(1-amino-6,6,6-trifluoro-1,2-dioxohexan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.0013
-
(1S,5R)-N-(1-amino-7,7,7-trifluoro-1,2-dioxoheptan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.00016
-
(1S,5R)-N-(4-amino-1-((1s,3S)-3-hydroxycyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.00021
-
(1S,5R)-N-(4-amino-1-(1-fluorocyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.163
-
(1S,5R)-N-(4-amino-1-(1-hydroxycyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.00005
-
(1S,5R)-N-(4-amino-1-(2,2-difluorocyclopropyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.000098
-
(1S,5R)-N-(4-amino-1-(3,3-difluorocyclobutyl)-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.000014
-
(1S,5R)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.000035
-
(1S,5R)-N-(4-amino-1-cyclobutyl-3,4-dioxobutan-2-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.00012
-
(1S,5R)-N-(5-amino-1,1,1-trifluoro-4,5-dioxopentan-3-yl)-3-((S)-2-(3-tert-butylureido)-3,3-dimethylbutanoyl)-6,6-dimethyl-3-azabicyclo[3.1.0]hexane-2-carboxamide
-
-
0.00001
-
(2-(3-((12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo-(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid
-
protease continous assay
0.000044
-
(2-(3-((12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo-(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
-
protease continous assay
0.000016
-
(2-(3-((12-cyclohexyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,-13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
-
protease continous assay
0.000015
-
(2-(3-((3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)henicosa-13(21),14,16(20)-triene-18-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid
-
continous enzyme assay
0.00026
-
(2-(3-((3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)henicosa-13(21),14,16(20)-triene-18-carbonyl)amino)-2-oxohexanoylamino)acetylamino)phenylacetic acid tert-butyl ester
-
continous enzyme assay
0.0023
-
(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2,10-dioxa-13-azatricyclo[15.2.2.13,7]docosa-1(19),3(22),4,6,17,20-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.00011
-
(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[15.2.2.13,7]docosa-1(19),3(22),4,6,17,20-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.0003
-
(2R)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[16.2.2.13,7]tricosa-1(20),3(23),4,6,18,21-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.21
-
(2R)-2-(acetylamino)-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
-
pH 6.5, 30C
0.26
-
(2R)-2-[(tert-butoxycarbonyl)amino]-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
-
pH 6.5, 30C
0.0000004
-
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-2-phenylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000001
-
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methyl-2-phenylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000002
-
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methyl-2-phenylquinazolin-4-yl)oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000003
-
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000006
-
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-2-(4-methoxyphenyl)-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000009
-
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(6-methylpyridin-2-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000028
-
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(pyridin-3-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000002
-
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[7-methoxy-8-methyl-2-(pyridin-4-yl)quinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000062
-
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-2-[[2-(morpholin-4-yl)quinazolin-4-yl]oxy]-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000004
-
(2R,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-4,14-dioxo-2-[(2-phenylquinazolin-4-yl)oxy]-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.00000062
-
(2R,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14
-
wild type enzyme, at 23C
-
0.0000016
-
(2R,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14
-
mutant enzyme M485A/V524A/Q526A, at 23C
-
0.0000064
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-([7-methoxy-2-[2-(methylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.000024
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxyquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.0000047
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[2-(1H-imidazol-1-yl)-7-methoxyquinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.0000055
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(1H-pyrazol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.0000051
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(1H-pyrrol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.000022
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(4-methyl-1H-pyrazol-1-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.000012
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[7-methoxy-2-(5-methyl-1,3,4-oxadiazol-2-yl)quinolin-4-yl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.00042
-
(2S)-([N-[3-([[(10S,13S)-10-cyclohexyl-8,11-dioxo-2,7-dioxa-9,12-diazabicyclo[13.3.1]nonadeca-1(19),15,17-trien-13-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.000015
-
(2S)-([N-[3-([[(3S,18S)-18-cyclohexyl-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinolin-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.00025
-
(2S)-([N-[3-([[(3S,6S)-6-cyclohexyl-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-trien-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.00001
-
(2S)-([N-[3-([[(7R,9S,12S)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.00016
-
(2S)-([N-[3-([[(9S,12S)-12-cyclohexyl-11,14-dioxo-2-oxa-10,13-diazatricyclo[17.2.2.13,7]tetracosa-1(21),3(24),4,6,19,22-hexaen-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoic acid
-
-
0.31
-
(2S)-2-[(tert-butoxycarbonyl)amino]-3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
-
pH 6.5, 30C
0.002
-
(2S)-2-[([(1R,4R)-2-[[(1R)-1-[[(1R)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)amino]butanoic acid
-
-
0.002
-
(2S)-2-[[(2-[[(1S)-1-(methoxycarbonyl)-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
0.00028
-
(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
0.000503
-
(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
0.000523
-
(2S)-2-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]butanoic acid
-
-
0.000038
-
(2S)-[([[3-([[(6S,8S,9R,10S,13S)-13-cyclohexyl-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-trien-10-yl]carbonyl]amino)-2-oxohexanoyl]amino]acetyl)amino](phenyl)ethanoic acid
-
-
0.0000012
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-([7-methoxy-2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinazolin-4-yl]oxy)-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000004
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(3-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000004
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000002
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxyquinazolin-4-yl]oxy]-5-methyl-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000012
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-2-[[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]oxy]-4,14-dioxo-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000008
-
(2S,3aR,10Z,11aS,12aR,14aR)-N-(cyclopropylsulfonyl)-5-methyl-4,14-dioxo-2-([2-[4-(propan-2-yl)-1,3-thiazol-2-yl]quinazolin-4-yl]oxy)-2,3,3a,4,5,6,7,8,9,11a,12,13,14,14a-tetradecahydrocyclopenta[c]cyclopropa[g][1,6]diazacyclotetradecine-12a(1H)-carboxamide
-
pH and temperature not specified in the publication
0.0000003
-
(2S,3aR,11Z,12aS,13aR,15aR)-N-(cyclopropylsulfonyl)-2-[(7-methoxy-8-methyl-2-phenylquinazolin-4-yl)oxy]-4,15-dioxo-1,2,3,3a,4,5,6,7,8,9,10,12a,13,14,15,15a-hexadecahydro-13aH-cyclopenta[c]cyclopropa[g][1,6]diazacyclopentadecine-13a-carboxamide
-
pH and temperature not specified in the publication
0.0000002
-
(2S,3aR,11Z,12aS,13aR,15aR)-N-(cyclopropylsulfonyl)-2-[[2-(4-fluorophenyl)-7-methoxy-8-methylquinazolin-4-yl]oxy]-4,15-dioxo-1,2,3,3a,4,5,6,7,8,9,10,12a,13,14,15,15a-hexadecahydro-13aH-cyclopenta[c]cyclopropa[g][1,6]diazacyclopentadecine-13a-carboxamide
-
pH and temperature not specified in the publication
0.0000014
-
(2S,4S)-1-((S)-2-((R)-2-cyclohexyl-2-(prop-1-en-2-ylamino)acetamido)-3,3-dimethylbutanoyl)-N-((1S,2R)-1-(cyclopropylsulfonylcarbamoyl)-2-vinylcyclopropyl)-4-phenylpyrrolidine-2-carboxamide
-
wild type enzyme, at 23C
0.0000028
-
(2S,4S)-1-((S)-2-((R)-2-cyclohexyl-2-(prop-1-en-2-ylamino)acetamido)-3,3-dimethylbutanoyl)-N-((1S,2R)-1-(cyclopropylsulfonylcarbamoyl)-2-vinylcyclopropyl)-4-phenylpyrrolidine-2-carboxamide
-
mutant enzyme M485A/V524A/Q526A, at 23C
0.0035
-
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,15-trioxo-1,4,10-triazacyclopentadecane-5-carboxamide
-
-
0.00066
-
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,16-trioxo-1,4,10-triazacyclohexadecane-5-carboxamide
-
-
0.00051
-
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,17-trioxo-1,4,10-triazacycloheptadecane-5-carboxamide
-
-
0.00044
-
(2S,5S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-cyclohexyl-3,11,18-trioxo-1,4,10-triazacyclooctadecane-5-carboxamide
-
-
0.000022
-
(2S,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
wild type enzyme, at 23C
0.000055
-
(2S,6S,12Z,13aS,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[4-(4-methoxyphenyl)-1H-1,2,3-triazol-1-yl]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
mutant enzyme M485A/V524A/Q526A, at 23C
0.000013
-
(3R)-2-[2-[(tert-butylcarbamoyl)amino]-3,3-dimethylbutanoyl]-N-[1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
continuous protease assay
0.00001
-
(3R)-2-[2-[(tert-butylcarbamoyl)amino]-3,3-dimethylbutanoyl]-N-[1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
continuous protease assay
0.000021
-
(3R)-2-[[(tert-butylcarbamoyl)amino](cyclohexyl)acetyl]-N-[1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
continuous protease assay
0.000019
-
(3R)-2-[[(tert-butylcarbamoyl)amino](cyclohexyl)acetyl]-N-[1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]-2-azabicyclo[2.2.1]heptane-3-carboxamide
-
continuous protease assay
0.000006
-
(3S)-3-[(7R,9S,12R)-9-[(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-12-yl]cyclohexanecarboxylic acid
-
-
0.000021
-
(3S,18S)-18-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinoline-3-carboxamide
-
-
0.00011
-
(3S,6S)-6-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-triene-3-carboxamide
-
-
0.00000015
-
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[16.6.2.14,7.022,26]heptacosa-16,18(26),19,21-tetraene-6-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.0000083
-
(4R,6S,9S,16E)-9-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-2,8,11-trioxo-3,12-dioxa-1,7,10-triazatetracyclo[20.3.1.14,7.018,23]heptacosa-16,18,20,22-tetraene-6-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.00021
-
(4S,7S,9R)-4-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2,5-dioxo-10,15-dioxa-3,6-diazatricyclo[14.3.1.16,9]henicosa-1(20),16,18-triene-7-carboxamide
-
-
0.000095
-
(5R,7S,10S)-10-cyclopentyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000071
-
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo(prop-2-en-1-ylamino)acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.00014
-
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo[(1-phenylethyl)amino]acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000176
-
(5R,7S,10S)-10-tert-butyl-3,9,12-trioxo-N-[(1S)-1-[oxo[(pyridin-2-ylmethyl)amino]acetyl]butyl]-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.00014
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclobutylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000078
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopentylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000085
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-1,6,7,9,10,11,12,14,15,16,17,18-dodecahydro-5H-2,22:5,8-dimethano-4,13,2,8,11-benzodioxatriazacycloicosine-7(3H)-carboxamide
-
-
0.000057
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[(cyclopropylamino)(oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000066
-
(5R,7S,10S)-10-tert-butyl-N-[(1S)-1-[[(1-methylpropyl)amino](oxo)acetyl]butyl]-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.000242
-
(5R,7S,10S)-N-[(1S)-1-[(benzylamino)(oxo)acetyl]butyl]-10-tert-butyl-3,9,12-trioxo-6,7,9,10,11,12,14,15,16,17,18,19-dodecahydro-1H,5H-2,23:5,8-dimethano-4,13,2,8,11-benzodioxatriazacyclohenicosine-7(3H)-carboxamide
-
-
0.00009
-
(5R,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-2-methyl-3,6-dioxo-11,15-dioxa-2,4,7-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
0.0016
-
(5R,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-11,15-dioxa-2,4,7-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
0.0002
-
(5R,8S,10R)-5-tert-butyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-2,11,15-trioxa-4,7-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-8-carboxamide
-
-
0.00068
-
(5S,8S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5-cyclohexyl-3,6,14-trioxo-4,7,13-triazabicyclo[14.2.2]icosa-1(18),16,19-triene-8-carboxamide
-
-
0.00045
-
(5S,8S)-N-(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5-cyclohexyl-3,6,14-trioxo-4,7,13-triazabicyclo[14.3.1]icosa-1(20),16,18-triene-8-carboxamide
-
-
0.000007
-
(5S,8S,10R)-5-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-3,6-dioxo-11,16-dioxa-4,7-diazatricyclo[15.3.1.17,10]docosa-1(21),17,19-triene-8-carboxamide
-
-
0.000025
-
(6R,8S,11R)-11-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[14.3.1.16,9]henicosa-1(20),16,18-triene-8-carboxamide
-
-
0.00003
-
(6R,8S,11S)-11-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[13.3.1.16,9]icosa-1(19),15,17-triene-8-carboxamide
-
-
0.00000014
-
(6R,8S,11S,18E)-11-tert-butyl-N-((1R,2S)-1-[[(cyclopropylsulfonyl)amino]carbonyl]-2-vinylcyclopropyl)-3-methyl-4,10,13-trioxo-5,14-dioxa-3,9,12-triazatricyclo[18.3.1.16,9]pentacosa-1(24),18,20,22-tetraene-8-carboxamide
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
0.000037
-
(6S,11S,20S)-11-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-10,13-dioxo-2,5-dioxa-9,12-diazatricyclo[13.3.1.16,9]icosa-1(19),15,17-triene-20-carboxamide
-
-
0.000044
-
(6S,8S,9R,10S,13S)-13-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-triene-10-carboxamide
-
-
0.00007
-
(7R,9S)-12-(2,3-dihydro-1H-inden-1-yl)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000008
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000026
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-15-methyl-11,14-dioxo-2,6-dioxa-10,13,15-triazatricyclo[15.3.1.17,10]docosa-1(21),17,19-triene-9-carboxamide
-
-
0.000032
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-18-methoxy-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00003
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-18-methyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000012
-
(7R,9S,12R)-12-cyclohexyl-N-(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-19-methyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000008
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00001
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2-oxa-6-thia-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
protease continous assay
0.00001
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2-oxa-6-thia-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000036
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-6-(phenylsulfonyl)-2-oxa-6,10,13-triazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000006
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00006
-
(7R,9S,12S)-12-cyclohexyl-N-(1-[[(2-[[(1S)-2-hydroxy-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00006
-
(7R,9S,12S)-12-cyclohexyl-N-[(1S)-1-[[(2-[[(1S)-2-hydroxy-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
protease continous assay
0.000008
-
(7R,9S,12S)-12-cyclohexyl-N-[(1S)-1-[[[4-(dimethylamino)-2,4-dioxo-3-phenylbutyl]amino](oxo)acetyl]butyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
protease continous assay
0.000017
-
(7R,9S,12S)-12-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000019
-
(7R,9S,12S)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-12-(1-methylethyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00004
-
(7R,9S,12S)-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-5,5-dimethyl-12-(2-methylpropyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.00031
-
(7R,9S,12S)-N-(1-[[(2-[[(S)-cyano(phenyl)methyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-9-carboxamide
-
-
0.000015
-
(7S,12S,21S)-12-tert-butyl-N-(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-triene-21-carboxamide
-
-
0.000071
-
(R)-4-((S)-2-acetamido-3-carboxypropanamido)-5-((2S,3S)-1-((S)-1-((2S,4R)-4-(benzyloxy)-2-(2-butyl-2-((S)-1-phenylethylcarbamoyl)hydrazinecarbonyl)pyrrolidin-1-yl)-3-methyl-1-oxobutan-2-ylamino)-3-methyl-1-oxopentan-2-ylamino)-5-oxopentanoic acid
-
wild type enzyme, at 23C
-
0.00011
-
(R)-4-((S)-2-acetamido-3-carboxypropanamido)-5-((2S,3S)-1-((S)-1-((2S,4R)-4-(benzyloxy)-2-(2-butyl-2-((S)-1-phenylethylcarbamoyl)hydrazinecarbonyl)pyrrolidin-1-yl)-3-methyl-1-oxobutan-2-ylamino)-3-methyl-1-oxopentan-2-ylamino)-5-oxopentanoic acid
-
mutant enzyme M485A/V524A/Q526A, at 23C
-
0.0012
-
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
0.0023
-
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
0.0017
-
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
0.0066
-
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexyl-methylcarbamoyl-methyl)-carbamoyl]-2-methyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-pentanoic acid
-
-
0.00056
-
(S)-2-[[(1R,2R,4S)-2-[(S)-1-[((S)-cyclohexylmethylcarbamoyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopentanecarbonyl]-amino]-4,4-difluoro-butyric acid
-
-
0.00003
-
(S)-2-[[(1R,4R)-2-[(R)-1-[((S)-cyclohexyl-methoxycarbonyl-methyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopent-2-enecarbonyl]-amino]-pentanoic acid
-
-
0.002
-
(S)-2-[[(1S,4S)-2-[(R)-1-[((S)-cyclohexyl-methoxycarbonylmethyl)-carbamoyl]-2,2-dimethyl-propylcarbamoyl]-4-(7-methoxy-2-phenyl-quinolin-4-yloxy)-cyclopent-2-enecarbonyl]-amino]-pentanoic acid
-
-
0.00013
-
(Z)-(1R,4R,6S,14R,16R)-12-tert-butoxycarbonylamino-16-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,13-dioxo-3,12-diaza-tricyclo[12.3.0. 04, 6]heptadec-7-ene-4-carboxylic acid
-
-
0.000006
-
(Z)-(1R,4R,6S,15R,17R)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
0.000031
-
(Z)-(1R,4R,6S,15R,17R)-13-tert-butoxycarbonylamino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
0.000044
-
(Z)-(1R,4R,6S,15R,17R)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-13-methyl-2,14-dioxo-3,13-diazatricyclo[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
0.00026
-
(Z)-(1R,4R,6S,15R,17S)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo-[13.3.0.04,6]octadec-7-ene-4-carboxylic acid
-
-
0.00012
-
(Z)-(1R,4R,6S,16R,18R)-14-amino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diazatricyclo[14.3.0.04,6]nonadec-7-ene-4-carboxylic acid
-
-
0.00071
-
(Z)-(1R,4R,6S,16R,18R)-14-tert-butoxycarbonylamino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diaza-tricyclo[14.3.0.04,6]nonadec-7-ene-4-carboxylic acid
-
-
0.000015
-
(Z)-(1R,4R,6S,17R) and (1S,4R,6S,17S)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadeca-7,15-diene-4-carboxylic acid
-
-
0.01
-
(Z)-(1R,4R,6S,17R,19R)-15-amino-19-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,16-dioxo-3,15-diaza-tricyclo[15.3.0.04,6]icos-7-ene-4-carboxylic acid
-
-
0.01
-
(Z)-(1R,4R,6S,17R,19R)-15-tert-butoxycarbonylamino-19-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,16-dioxo-3,15-diaza-tricyclo[15.3.0.04,6]icos-7-ene-4-carboxylic acid
-
-
0.00011
-
(Z)-(1R,4R,6S,18R) and (1S,4R,6S,18S)-14-amino-18-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,15-dioxo-3,14-diaza-tricyclo[14.3.0.04,6]nonadeca-7,16-diene-4-carboxylic acid
-
-
0.00009
-
1,1-dimethylethyl [1-cyclohexyl-2-[(1S,5R)-6,6-dichloro-2(S)-[[[1-[1,2-dioxo-2-(2-propenylamino) ethyl]butyl]-amino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-2-oxoethyl]carbamate
-
-
0.00002
-
1,1-dimethylethyl [2-[(1S,5R)-2(S)-[[[1-(2-amino-1,2-dioxoethyl)butyl]amino]carbonyl]-6,6-dichloro-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxoethyl]-carbamate
-
-
0.000015
-
1,1-dimethylethyl[1-cyclohexyl-2-[(1S,5R)-6,6-dichloro-2(S)-[[[1-[2-[[2-[[2-(dimethylamino)-2-oxo-1(S)-phenylethyl]amino]-2-oxoethyl]amino]-1,2-dioxoethyl]-butyl]amino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-2-oxoethyl]carbamate
-
-
0.000007
-
1,1-dimethylethyl[2-[(1S,5R)-6,6-dichloro-2(S)-[[ [1-(cyclopropyl-methyl)-3-[[2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl]amino]-2,3-dioxopropyl]-amino]carbonyl]-3-azabicyclo[3.1.0]-hexan-3-yl]-1-cyclohexyl-2-oxoethyl]carbamate
-
-
0.000009
-
1,1-dimethylethyl[2-[(1S,5R)-6,6-dichloro-2(S)-[[1-(cyclobutylmethyl)-3-[[2-[[2-(dimethylamino)-2-oxo-1(S)-phenylethyl]amino]-2-oxomethyl]amino]-2,3-dioxopropylamino]carbonyl]-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxomethyl]carbamate
-
-
0.26
-
1,10-phenanthroline
-
-
0.0002
-
1-([1-[(1,2-diphenylhydrazino)carbonyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
with Ac-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide as substrate
0.0003
-
1-([1-[(1,2-diphenylhydrazino)carbonyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-D-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
with Ac-Asp-Glu-Glu(EDANS)-Glu-Glu-AlgPSI[COO]-Ala-Ser-Lys(DABCYL)-amide as substrate
0.000052
-
1-aminocyclopropane-1-carboxylic acid ketoacid
-
at pH 6.0
0.00019
-
1-aminocyclopropane-1-carboxylic acid ketoacid
-
at pH 6.0 and 100 mM NaCl
0.00182
-
1-aminocyclopropane-1-carboxylic acid ketoacid
-
at pH 8.0 and 100 mM NaCl
0.00377
-
1-aminocyclopropane-1-carboxylic acid ketoacid
-
at pH 8.0
0.00037
-
1-aminocyclopropane-1-carboxylic acid ketotetrazole
-
at pH 6.0
0.00107
-
1-aminocyclopropane-1-carboxylic acid ketotetrazole
-
at pH 6.0 and 100 mM NaCl
0.00227
-
1-aminocyclopropane-1-carboxylic acid ketotetrazole
-
at pH 8.0 and 100 mM NaCl
0.00562
-
1-aminocyclopropane-1-carboxylic acid ketotetrazole
-
at pH 8.0
0.00149
-
1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone
-
at pH 6.0
0.00168
-
1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone
-
at pH 8.0 and 100 mM NaCl
0.0032
-
1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone
-
at pH 6.0 and 100 mM NaCl
0.0041
-
1-aminocyclopropane-1-carboxylic acid pentafluoroethyl ketone
-
at pH 8.0
0.0000062
-
1-aminocyclopropanecarboxylic acid
-
at pH 6.0
0.000025
-
1-aminocyclopropanecarboxylic acid
-
at pH 6.0 and 100 mM NaCl
0.0002
-
1-aminocyclopropanecarboxylic acid
-
at pH 8.0 and 100 mM NaCl
0.00032
-
1-aminocyclopropanecarboxylic acid
-
at pH 8.0
0.000006
-
12-cyclohexyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)-methyl)aminooxalyl)butyl)amide
-
protease continous assay
0.000015
-
12-tert-butyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
protease continous assay
0.000017
-
12-tert-butyl-5,5-dimethyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo(14.3.1.17,10)henicosa-1(19),16(20),17-triene-9-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)-aminooxalyl)butyl)amide
-
protease continous assay
0.000065
-
2,2,2-trifluoro-1,1-dimethylethyl[2-[(1S,5R)-2(S)-[[[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]amino]-carbonyl]-6,6-dichloro-3-azabicyclo[3.1.0]hexan-3-yl]-1(S)-cyclohexyl-2-oxoethyl]carbamate
-
-
0.0008
-
2-(4-[3-[1-Carboxy-2-(4-hydroxy-3,5-diiodo-phenyl)-ethylcarbamoyloxy]-propoxy]-benzoyl)-benzoic acid
-
pH 6.5, 30C
0.001
-
2-(4-[3-[1-tert-Butoxycarbonyl-2-(4-hydroxy-3,5-diiodo-phenyl)-ethylcarbamoyloxy]-propoxy]-benzoyl)-benzoic acid tert-butyl ester
-
pH 6.5, 30C
0.03
-
3,4-Dichloroisocoumarin
-
-
0.14
-
3-(4-hydroxy-3,5-diiodophenyl)-2-phenylpropanoic acid
-
pH 6.5, 30C
0.1
-
3-(4-hydroxy-3,5-diiodophenyl)-3-phenylpropanoic acid
-
pH 6.5, 30C
0.08
-
3-(4-hydroxy-3,5-diiodophenyl)propanoic acid
-
pH 6.5, 30C
0.000021
-
3-cyclohexyl-2,5-dioxo-12-oxa-1,4-diazatricyclo(11.5.3.016,20)-henicosa-13(21),14,16(20)-triene-18-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
continous enzyme assay
0.0034
-
3-[(2R,5S,8S)-8-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-5-cyclohexyl-3,6,14,18-tetraoxo-1,4,7,13-tetraazacyclooctadecan-2-yl]propanoic acid
-
-
0.0043
-
3-[(3S,6R,17S)-17-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-3-cyclohexyl-2,5,8,11-tetraoxo-1,4,7,12-tetraazacycloheptadecan-6-yl]propanoic acid
-
-
0.0185
-
3-[2-(2-Benzyloxycarbonylamino-3-methyl-pentanoylamino)-4-methyl-pentanoylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
pH 7.5
0.017
-
3-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
pH 7.5
0.000004
-
3-[2-(2-[2-[2-(2-Acetylamino-3-carboxy-propionylamino)-4-carboxy-butyrylamino]-3,3-diphenyl-propionylamino]-4-carboxy-butyrylamino)-3-cyclohexyl-propionylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
pH 7.5
0.00003
-
3-[2-(3-tert-butyl-ureido)-2-indan-2-yl-acetyl]-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
0.000007
-
3-[2-(3-tert-butyl-ureido)-3,3-dimethyl-butyryl]-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
0.0046
-
3-[2-[2-(2-Acetylamino-3,3-diphenyl-propionylamino)-4-tert-butoxycarbonyl-butyrylamino]-3-cyclohexyl-propionylamino]-5,5-difluoro-2-oxo-pentanoic acid
-
pH 7.5
0.45
-
4-(2-aminoethyl)-benzenesulfonyl fluoride
-
-
0.0021
-
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-3-methyl-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
wild-type enzyme
0.0023
-
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-3-methyl-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
mutant enzyme K136R
0.004
-
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-3-methyl-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
mutant enzyme K136M
0.0006
-
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
wild-type enzyme
0.0009
-
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
mutant enzyme K136R
0.0013
-
4-(2-[2-[2-(2-tert-Butoxycarbonylamino-4-carboxy-butyrylamino)-4-methyl-pentanoylamino]-4,4-difluoro-but-2-enoylamino]-ethyl)-3-chloro-benzoic acid
-
mutant enzyme K136M
0.18
-
4-(4-hydroxy-3,5-diiodophenyl)butanoic acid
-
pH 6.5, 30C
1.89
-
4-(amidinophenyl)-methanesulfonyl fluoride
-
-
0.6
-
4-hydroxy-3,5-diiodobenzoic acid
-
pH 6.5, 30C
0.021
-
4-hydroxypanduratin A
-
-
0.0073
-
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-3,3-difluoro-propenylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
-
wild-type enzyme
0.0083
-
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-3,3-difluoro-propenylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
-
mutant enzyme K136R
0.0135
-
4-tert-Butoxycarbonylamino-4-(1-[1-[2-(2-chloro-phenyl)-ethylcarbamoyl]-3,3-difluoro-propenylcarbamoyl]-3-methyl-butylcarbamoyl)-butyric acid
-
mutant enzyme K136M
0.000019
-
4-[(7R,9S,12R)-9-[(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-12-yl]cyclohexanecarboxylic acid
-
-
0.00003
-
4-[(7R,9S,12R)-9-[(1-[[(2-[[2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-12-yl]cyclohexanecarboxylic acid
-
-
0.06
-
4MeBu-P-norvaline-(CO)-GMSYS-NH2
-
pH 6.5, 30C
-
0.000007
-
5-cyclohexyl-3,6-dioxo-11,16-dioxa-4,7-diazatricyclo(15.3.1.17,10)-docosa-1(21),17,19-triene-8-carboxylic acid ((((1-(dimethylcarbamoylphenylmethyl)carbamoyl)methyl)aminooxalyl)butyl)amide
-
protease continous assay
0.000015
-
6,6-dichloro-3-[2-cyclohexyl-2-(3-cyclohexyl-ureido)-acetyl]-3-aza-bicyclo[3.1.0]hexane-2-carboxylic acid(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethyl)-amide
-
-
0.0038
-
Ac-Asp-Glu-Leu-Ile-Cha-Cys-OH
-
for Ac-Asp-Glu-Glu(EDANS)-Glu-Glu-AlgPSI[COO]-Ala-Ser-Lys(DABCYL)-amide
0.004
-
Ac-Asp-Glu-Leu-Ile-Cha-Cys-OH
-
for AAc-Asp-Glu-Lys(TAMRA)-Glu-Glu-AbuPSI[COO]-Ala-Ser-Lys(QSY-7)-amide
0.04
-
Ac-DdIVPC-OH
-
-
-
0.0075
-
Ac-DvIVPC-OH
-
-
-
0.0667
-
Ac-EVKKQR-NH2
-
pH 9.0, 37C
0.0259
-
Ac-FAAGRK-NH2
-
pH 9.0, 37C
0.1523
-
Ac-GKR-NH2
-
pH 9.0, 37C
0.0223
-
Ac-KKR-NH2
-
pH 9.0, 37C
0.1215
-
Ac-KR-NH2
-
pH 9.0, 37C
0.0121
-
Ac-RTSKKR-NH2
-
pH 9.0, 37C
0.1876
-
Ac-SKKR-NH2
-
pH 9.0, 37C
0.046
-
Ac-TTSTRR-NH2
-
pH 9.0, 37C
0.3
-
acetyl-3,3-diphenylalanine-beta-cyclohexylalanine-Cys-OH
-
-
-
0.009
-
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 1a
0.01
-
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme D168Q; pH 6.5, 30C, strain 1b; pH 6.5, 30C, strain 3a, mutant enzyme T123R/Q168D
0.013
-
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme T123R
0.04
-
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 3a
0.045
-
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme Q168D
0.05
-
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme R123T
0.055
-
acetyl-Asp-(D-Glu)-(allyloxycarbonyl-L-lysine)-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme R123T/D168Q
0.0028
-
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme T123R/Q168D
0.0032
-
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme T123R
0.0045
-
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a
0.005
-
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme D168Q
0.0052
-
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1b
0.02
-
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme R123T; pH 6.5, 30C, strain 3a, mutant enzyme Q168D
0.025
-
acetyl-Asp-(D-Glu)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme R123T/D168Q; pH 6.5, 30C, strain 3a
0.0018
-
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a
0.0027
-
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1b
0.0029
-
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme T123R
0.0033
-
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme D168Q
0.004
-
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme T123R/Q168D
0.01
-
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 3a
0.013
-
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme Q168D
0.015
-
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme R123T
0.018
-
acetyl-Asp-(D-Glu)-Tyr-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme R123T/D168Q
0.016
-
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a
0.02
-
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1b; pH 6.5, 30C, strain 3a, mutant enzyme Q168D
0.021
-
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme D168Q; pH 6.5, 30C, strain 1a, mutant enzyme R123T
0.023
-
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme R123T/D168Q; pH 6.5, 30C, strain 3a
0.024
-
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme T12 3R
0.025
-
acetyl-Asp-(D-glutamine)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme T123R/Q168D
0.0012
-
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys
-
pH 6.5, 30C, strain 1a
0.0011
-
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1b
0.0022
-
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme D168Q
0.0026
-
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme T123R/Q168D
0.0032
-
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme T123R
0.024
-
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme Q168D
0.025
-
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme R123T
0.03
-
acetyl-Asp-(D-homoglutamate)-Leu-Ile-L-cyclohexylalanine-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme R123T/D168Q; pH 6.5, 30C, strain 3a
0.018
-
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme R123T; pH 6.5, 30C, strain 3a, mutant enzyme Q168D
0.019
-
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 1a; pH 6.5, 30C, strain 3a, mutant enzyme T123R
0.02
-
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme R123T/D168Q
0.021
-
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 3a
0.022
-
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 3a, mutant enzyme T123R/Q168D
0.023
-
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 1b
0.024
-
acetyl-Asp-(D-homoleucine)-Leu-Ile-(L-cyclohexylalanine)-Cys-OH
-
pH 6.5, 30C, strain 1a, mutant enzyme D168Q
0.000012
-
acetyl-Asp-D-(gamma-carboxyglutamic acid)-Leu-Ile-(beta-cyclohexylalanine)-Cys
-
pH 7.5, 30C
0.000041
-
acetyl-Asp-Glu-(3,3-diphenylalanine)-Glu-(beta-cyclohexylalanine)-Cys
-
pH 7.5, 30C
0.00022
-
acetyl-Asp-Glu-(3,3-diphenylalanine)-Ile-(beta-cyclohexylalanine)-Cys
-
pH 7.5, 30C
0.000055
-
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme R161S
0.00006
-
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme R123T
0.0000615
-
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme K165S
0.000079
-
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme R109Q
0.000129
-
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme R155S
0.000179
-
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme K165S/R1161S
0.00031
-
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme K136M/R109Q
0.000313
-
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, mutant enzyme K136M
0.04
-
acetyl-Asp-Glu-(diaminopropionyl)-(N-beta-dansyl)-Glu-(beta-cyclohexylalanine)-Cys-OH
-
pH 7.5, wild-type enzyme
0.00005
-
acetyl-Asp-Glu-3,3-diphenylalanine-Glu-beta-cyclohexylalanine-Cys-OH
-
-
0.046
-
acetyl-Asp-Glu-3,3-diphenylalanine-Ile-beta-cyclohexylalanine-OH
-
-
0.00049
-
acetyl-Asp-Glu-Leu-Glu-(beta-cyclohexylalanine)-Cys
-
pH 7.5, 30C
0.0026
-
acetyl-Asp-Glu-Leu-Glu-beta-cyclohexylalanine-Cys-OH
-
-
0.00006
-
acetyl-Asp-Glu-Leu-Ile-beta-cyclohexylalanine-Cys-OH
-
-
0.00035
-
acetyl-Asp-Glu-Met-Glu-beta-cyclohexylalanine-Cys-OH
-
-
0.00036
-
acetyl-Asp-Glu-Met-Glu-Glu-Cys
-
pH 7.5, 30C
0.001
-
acetyl-Asp-Glu-Met-Glu-Glu-Cys-OH
-
-
0.000013
-
acetyl-Asp-Glu-Val-Val-Pro-boroAlg-OH
-
-
0.17
-
acetyl-DEMEEC-OH
-
pH 6.5, 30C, strain 1b
0.2
-
acetyl-DEMEEC-OH
-
pH 6.5, 30C, strain 1a
0.21
-
acetyl-DEMEEC-OH
-
pH 6.5, 30C, strain 3a
0.4
-
acetyl-DYPSPC-OH
-
pH 6.5, 30C, strain 1b
0.43
-
acetyl-DYPSPC-OH
-
pH 6.5, 30C, strain 3a
0.45
-
acetyl-DYPSPC-OH
-
pH 6.5, 30C, strain 1a
0.46
-
acetyl-ECTTPC-OH
-
pH 6.5, 30C, strain 1b
0.5
-
acetyl-ECTTPC-OH
-
pH 6.5, 30C, strain 1a
0.51
-
acetyl-ECTTPC-OH
-
pH 6.5, 30C, strain 3a
0.1
-
acetyl-EDVVCC-OH
-
pH 6.5, 30C, strain 3a
0.13
-
acetyl-EDVVCC-OH
-
pH 6.5, 30C, strain 1a
0.15
-
acetyl-EDVVCC-OH
-
pH 6.5, 30C, strain 1b
0.000096
-
acetyl-EEVVP-norvaline-(CO)-GMSYS-NH2
-
pH 6.5, 30C
-
0.0016
-
acetyl-EEVVP-norvaline-(CO)-phenethylamide
-
pH 6.5, 30C
-
0.0014
-
acetyl-Glu-3,3-diphenylalanine-Glu-beta-cyclohexyalanine-Cys-OH
-
-
0.46
-
acetyl-Glu-beta-cyclohexylalanine-Cys-OH
-
-
5
-
acetyl-Glu-Leu-Glu-beta-cyclohexylalanine-Cys-OH
-
-
0.08
-
acetyl-P-norvaline-(CO)-GMSYS-NH2
-
pH 6.5, 30C
-
0.04
-
acetyl-QSVVCC-OH
-
pH 6.5, 30C, strain 1a; pH 6.5, 30C, strain 3a
0.05
-
acetyl-QSVVCC-OH
-
pH 6.5, 30C, strain 1b
0.00059
-
Alpha1-antitrypsin
-
pH 8.0, 18C
-
0.00001761
-
Aprotinin
-
-
0.000026
-
Aprotinin
-
pH 8.0, 18C
0.000049
-
benzyl 1-([[(2S)-1-[(1R,5S)-2-[(4-amino-1-cyclopropyl-3,4-dioxobutan-2-yl)carbamoyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hex-3-yl]-3,3-dimethyl-1-oxobutan-2-yl]carbamoyl]amino)cyclohexanecarboxylate
-
pH and temperature not specified in the publication
-
0.000001
-
BILN 2061
-
enzyme from hepatitis C virus genotype 4a, in 1 M MES (pH 5.8), at 23C
0.0000014
-
BILN 2061
-
enzyme from hepatitis C virus genotype 1b, in 1 M MES (pH 5.8), at 23C
0.000003
-
BILN 2061
-
enzyme from hepatitis C virus genotype 5a, in 1 M MES (pH 5.8), at 23C
0.0000037
-
BILN 2061
-
enzyme from hepatitis C virus genotype 6a, in 1 M MES (pH 5.8), at 23C
0.000015
-
BILN 2061
-
enzyme from hepatitis C virus genotype 2a, in 1 M MES (pH 5.8), at 23C
0.000019
-
BILN 2061
-
wild-type, pH 7.8, 30C
0.0012
-
BILN 2061
-
or above, mutant A156T, pH 7.8, 30C; or above, mutant A156V, pH 7.8, 30C
0.00000038
-
BILN-2061
-
-
0.000003
-
BILN-2061
-
NS3/4A genotype 1b
0.0000081
-
BILN-2061
-
NS3/4A genotype 1a
0.00007
-
BILN-2061
-
NS3/4A genotype 2a
0.00061
-
BILN-2061
-
NS3/4A genotype 2b
0.00075
-
Bz-Ala-Lys-Arg-Arg-H
-
-
0.0053
-
Bz-Ala-Lys-Arg-Arg-H
-
-
0.00085
-
Bz-Arg-Arg-H
-
-
0.012
-
Bz-Arg-Arg-H
-
-
0.0094
-
Bz-D-Nle-Lys-Arg-Arg-H
-
-
0.0004
-
Bz-Lys-Arg-Arg-H
-
-
0.0015
-
Bz-Lys-Arg-Arg-H
-
-
0.0437
-
Bz-N-Me-Nle-Lys-Arg-Arg-H
-
-
0.0009
-
Bz-Nle-Ala-Arg-Arg-H
-
-
0.0221
-
Bz-Nle-Ala-Arg-Arg-H
-
-
0.0286
-
Bz-Nle-D-Lys-Arg-Arg-H
-
-
0.125
-
Bz-Nle-Lys-Ala-Arg-H
-
-
0.5
-
Bz-Nle-Lys-Ala-Arg-H
-
-
0.138
-
Bz-Nle-Lys-Arg-(p-Cl)Phe-H
-
-
0.0186
-
Bz-Nle-Lys-Arg-(p-CN)Phe-H
-
-
0.0028
-
Bz-Nle-Lys-Arg-(p-guanidinyl)Phe-H
-
-
0.006
-
Bz-Nle-Lys-Arg-(p-Me)Phe-H
-
-
0.0116
-
Bz-Nle-Lys-Arg-(p-Ph)Phe-H
-
-
0.03315
-
Bz-Nle-Lys-Arg-Ala-H
-
-
0.193
-
Bz-Nle-Lys-Arg-Ala-H
-
-
0.178
-
Bz-Nle-Lys-Arg-Arg(OH)-CONH-Bn
-
-
0.000043
-
Bz-Nle-Lys-Arg-Arg-B(OH)2
-
-
0.0829
-
Bz-Nle-Lys-Arg-Arg-benzoxazole
-
-
0.00085
-
Bz-Nle-Lys-Arg-Arg-CF3
-
-
0.0004
-
Bz-Nle-Lys-Arg-Arg-H
-
-
0.0058
-
Bz-Nle-Lys-Arg-Arg-H
-
-
0.1275
-
Bz-Nle-Lys-Arg-Arg-NH2
-
-
0.5
-
Bz-Nle-Lys-Arg-Arg-NHSO2CF3
-
-
0.5
-
Bz-Nle-Lys-Arg-Arg-OH
-
-
0.0428
-
Bz-Nle-Lys-Arg-Arg-thiazole
-
-
0.051
-
Bz-Nle-Lys-Arg-D-Arg-H
-
-
0.5
-
Bz-Nle-Lys-Arg-homoPhe-H
-
-
0.0112
-
Bz-Nle-Lys-Arg-Lys-H
-
-
0.0205
-
Bz-Nle-Lys-Arg-Lys-H
-
-
0.0159
-
Bz-Nle-Lys-Arg-Phe-H
-
-
0.062
-
Bz-Nle-Lys-Arg-Phe-H
-
-
0.033
-
Bz-Nle-Lys-Arg-Phg-H
-
-
0.0075
-
Bz-Nle-Lys-Arg-Trp-H
-
-
0.115
-
Bz-Nle-Lys-D-Arg-Arg-H
-
-
0.00005
-
Bz-Nle-Lys-Lys-Arg-B(OH)2
-
-
0.0012
-
Bz-Nle-Lys-Lys-Arg-H
-
-
0.0413
-
Bz-Nle-Lys-Lys-Arg-H
-
-
0.0474
-
Bz-Nle-Lys-N-Me-Arg-Arg-H
-
-
0.0156
-
Bz-Nle-Lys-Phe-Arg-H
-
-
0.0407
-
Bz-Nle-Lys-Phe-Arg-H
-
-
0.109
-
Bz-Nle-Lys-Pro-Arg-H
-
-
0.5
-
Bz-Nle-Lys-Thr-Arg-H
-
-
0.5
-
Bz-Nle-Lys-Thr-Arg-NH2
-
-
0.5
-
Bz-Nle-Lys-Thr-Arg-OH
-
-
0.1133
-
Bz-Nle-N-Me-Lys-Arg-Arg-H
-
-
0.0015
-
Bz-Nle-Phe-Arg-Arg-H
-
-
0.0158
-
Bz-Nle-Phe-Arg-Arg-H
-
-
0.0614
-
Bz-Nle-Pro-Arg-Arg-H
-
-
0.00025
-
Bz-Phe-Lys-Arg-Arg-H
-
-
0.0068
-
Bz-Phe-Lys-Arg-Arg-H
-
-
0.377
-
cardamonin
-
-
0.71
-
chymostatin
-
-
0.00000019
-
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17R)-13-amino-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carbonyl]-amide
-
-
0.0000000091
-
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17R)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-13-methyl-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-ene-4-carbonyl]-amide
-
-
0.0000044
-
cyclopropanesulfonic acid [(Z)-(1R,4R,6S,15R,17S)-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0. 04,6]octadec-7-ene-4-carbonyl]-amide
-
-
0.071
-
DDIVPC-OH
-
-
0.000002
-
deca-D-Arg-NH2
-
pH 8.0, 18C
0.000001
-
dodeka-D-Arg-NH2
-
pH 8.0, 18C
0.007
-
EDTA
-
-
0.000124
-
fluorescein-L-Asp-D-Glu-L-Leu-L-Ile-L-beta-cyclohexylalanine-L-Cys-L-Pro-L-beta-cyclohexylalanine-L-Asp-L-Leu-NH2
-
pH 7.3, 30C
0.000041
-
hepta-D-Arg-NH2
-
pH 8.0, 18C
0.000478
-
hexa-D-Arg-NH2
-
pH 8.0, 18C
0.26
-
iodoacetamide
-
-
0.000098
-
L-aminobutyric acid carboxylic acid
-
at pH 6.0
0.00025
-
L-aminobutyric acid carboxylic acid
-
at pH 6.0 and 100 mM NaCl
0.00125
-
L-aminobutyric acid carboxylic acid
-
at pH 8.0 and 100 mM NaCl
0.00275
-
L-aminobutyric acid carboxylic acid
-
at pH 8.0
0.000051
-
L-aminobutyric acid pentafluoroethyl ketone
-
at pH 8.0 and 100 mM NaCl
0.000084
-
L-aminobutyric acid pentafluoroethyl ketone
-
at pH 6.0
0.00015
-
L-aminobutyric acid pentafluoroethyl ketone
-
at pH 6.0 and 100 mM NaCl
0.00082
-
L-aminobutyric acid pentafluoroethyl ketone
-
at pH 8.0
0.000016
-
L-norvaline carboxylic acid
-
at pH 6.0
0.000031
-
L-norvaline carboxylic acid
-
at pH 6.0 and 100 mM NaCl
0.000245
-
L-norvaline carboxylic acid
-
at pH 8.0 and 100 mM NaCl
0.00045
-
L-norvaline carboxylic acid
-
at pH 8.0
0.000134
-
L-norvaline ketotetrazole
-
at pH 6.0
0.00046
-
L-norvaline ketotetrazole
-
at pH 6.0 and 100 mM NaCl
0.00174
-
L-norvaline ketotetrazole
-
at pH 8.0
0.00188
-
L-norvaline ketotetrazole
-
at pH 8.0 and 100 mM NaCl
0.000117
-
L-norvaline pentafluoroethyl ketone
-
at pH 8.0 and 100 mM NaCl
0.000145
-
L-norvaline pentafluoroethyl ketone
-
at pH 8.0
0.00015
-
L-norvaline pentafluoroethyl ketone
-
at pH 6.0
0.00035
-
L-norvaline pentafluoroethyl ketone
-
at pH 6.0 and 100 mM NaCl
0.00000006
-
MK-7009
-
NS3/4A genotype 1b
0.00000007
-
MK-7009
-
NS3/4A genotype 1a
0.000001
-
MK-7009
-
NS3/4A genotype 2a
0.000041
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-([2-[2-(dimethylamino)-1,3-thiazol-4-yl]pyridin-4-yl]oxy)-L-prolinamide
-
wild type enzyme, at 23C
0.000078
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-([2-[2-(dimethylamino)-1,3-thiazol-4-yl]pyridin-4-yl]oxy)-L-prolinamide
-
mutant enzyme M485A/V524A/Q526A, at 23C
0.0000095
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
wild type enzyme, at 23C
0.000015
-
N-(tert-butoxycarbonyl)-3-methyl-L-valyl-(4R)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolinamide
-
mutant enzyme M485A/V524A/Q526A, at 23C
0.000102
-
N-([(1R,4R)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)-L-norvaline
-
-
0.00256
-
N-([(1S,4S)-2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2-methylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl]carbonyl)-L-norvaline
-
-
1.17
-
N-acetyl-L-alpha-aspartyl-L-alpha-glutamyl-beta-phenyl-L-phenylalanyl-L-alpha-glutamyl-3-cyclohexyl-L-alanine
-
-
0.00000074
-
N-acetyl-L-alpha-aspartyl-N-[(1S)-2-[[(1S)-1-([(2S,4R)-2-[[(1S,2R)-1-carboxy-2-ethenylcyclopropyl]carbamoyl]-4-[(2-phenylquinolin-4-yl)oxy]pyrrolidin-1-yl]carbonyl)-2,2-dimethylpropyl]amino]-1-cyclohexyl-2-oxoethyl]-D-alpha-glutamine
-
-
0.03
-
N-tosyl-Phe chloromethyl ketone
-
-
0.000067
-
N-[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]-L-norvaline
-
-
0.000003
-
N-[(2S)-2-[(N-acetyl-L-alpha-aspartyl-D-alpha-glutamyl)amino]-2-cyclohexylacetyl]-L-valyl-(4S)-4-(naphthalen-2-ylmethoxy)-D-prolyl-D-norvaline
-
-
0.00025
-
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1R,2R)-1-[(cyclopropylsulfonyl)carbamoyl]-2-(methylideneamino)cyclopropyl]-4-hydroxy-L-prolinamide
-
wild type enzyme, at 23C
-
0.00041
-
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4R)-N-[(1R,2R)-1-[(cyclopropylsulfonyl)carbamoyl]-2-(methylideneamino)cyclopropyl]-4-hydroxy-L-prolinamide
-
mutant enzyme M485A/V524A/Q526A, at 23C
-
0.002
-
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-phenyl-L-prolinamide
-
wild type enzyme, at 23C
0.0036
-
N-[(cyclopentyloxy)carbonyl]-3-methyl-L-valyl-(4S)-N-[(1R,2S)-1-carboxy-2-ethenylcyclopropyl]-4-phenyl-L-prolinamide
-
mutant enzyme M485A/V524A/Q526A, at 23C
0.0000004
-
N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide
-
-
0.0000005
-
N-[17-[2-(4-isopropylthiazole-2-yl)-7-methoxy-8-methylquinolin-4-yloxy]-13-methyl-2,14-dioxo-3,13-diazatricyclo [13.3.0.0(4,6)]octadec-7-ene-4-carbonyl](cyclopropyl)sulfonamide
-
-
0.0000002
-
N-[17-[8-chloro-2-(4-isopropylthiazol-2-yl)-7-methoxy-quinolin-4-yloxy]-2,14-dioxo-3,15-diazatricyclo [13.3.0.0]octadec-7-ene-4-carbonyl]-(1-methylcyclo propyl)-(1-methylcyclopropyl)sulfonamide
-
-
0.15
-
Nalpha-p-tosyl-Lys chloromethyl ketone
-
-
-
0.000006
-
nona-D-Arg-NH2
-
pH 8.0, 18C
0.000017
-
octa-D-Arg-NH2
-
pH 8.0, 18C
0.025
-
panduratin A
-
-
0.6
-
phenylmethanesulfonyl fluoride
-
-
0.345
-
pinostrobin
-
-
0.000014
-
SCH 503034
-
-
0.000021
-
SCH-503034
-
NS3/4A genotype 1a; NS3/4A genotype 2b
0.000025
-
SCH-503034
-
NS3/4A genotype 2a
0.000028
-
SCH-503034
-
NS3/4A genotype 1b
0.02
-
SCH217135
-
pH 6.5, 30C
0.048
-
SCH217142
-
pH 6.5, 30C
0.06
-
SCH217942
-
pH 6.5, 30C
0.000091
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid
-
pH 7.5, 30C
0.000098
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-COOH
-
pH 7.5, 30C
0.0000038
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-1-aminocyclopropane-1-carboxylic acid-NHSO2Ph
-
pH 7.5, 30C
0.0000136
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-2-aminovaleryl-NHSO2Ph
-
pH 7.5, 30C
0.000081
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-aminobutyryl ((S)-2-amino-butanoyl)-C2F5
-
pH 7.5, 30C
0.000028
-
Suc-L-Asp-D-Glu-L-Leu-L-Ile-L-(cyclohexyl)Ala-L-Cys-OH
-
pH 7.5, 30C
0.000041
-
tert-butyl (1-cyclohexyl-2-[(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]pentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]-2-oxoethyl)carbamate
-
continuous protease assay
0.000027
-
tert-butyl (1-[[(3R)-3-([1-(2-cyclobutylethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]carbonyl]-2,2-dimethylpropyl)carbamate
-
continuous protease assay
0.000019
-
tert-butyl (1-[[(3R)-3-([1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]carbonyl]-2,2-dimethylpropyl)carbamate
-
continuous protease assay
0.002
-
tert-butyl (1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-(methylamino)-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylate
-
-
0.002
-
tert-butyl (1R,2S)-1-[[(2-[[(1S)-1-[[(1S)-1-cyclohexyl-2-methoxy-2-oxoethyl]carbamoyl]-2,2-dimethylpropyl]carbamoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]cyclopent-2-en-1-yl)carbonyl]amino]-2-ethenylcyclopropanecarboxylate
-
-
0.00026
-
tert-butyl (2S)-([N-[3-([[(3S,18S)-18-cyclohexyl-16,19-dioxo-3,4-dihydro-1H-7,2-(epoxyheptanoiminoethano)isoquinolin-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
0.0023
-
tert-butyl (2S)-([N-[3-([[(3S,6S)-6-cyclohexyl-5,8-dioxo-4,7-diazabicyclo[14.3.1]icosa-1(20),16,18-trien-3-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
0.000044
-
tert-butyl (2S)-([N-[3-([[(7R,9S,12S)-12-cyclohexyl-11,14-dioxo-2,6-dioxa-10,13-diazatricyclo[14.3.1.17,10]henicosa-1(20),16,18-trien-9-yl]carbonyl]amino)-2-oxohexanoyl]glycyl]amino)(phenyl)ethanoate
-
-
0.000038
-
tert-butyl (2S)-[([[3-([[(6S,8S,9R,10S,13S)-13-cyclohexyl-12,15-dioxo-2,7,23-trioxa-11,14-diazatetracyclo[15.3.1.16,9.18,11]tricosa-1(21),17,19-trien-10-yl]carbonyl]amino)-2-oxohexanoyl]amino]acetyl)amino](phenyl)ethanoate
-
-
0.00004
-
tert-butyl [1-([(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]-4-methylpentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]carbonyl)-2,2-dimethylpropyl]carbamate
-
continuous protease assay
0.000081
-
tert-butyl [1-([(3R)-3-[(1-[[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]pentyl)carbamoyl]-2-azabicyclo[2.2.1]hept-2-yl]carbonyl)-2,2-dimethylpropyl]carbamate
-
continuous protease assay
0.00002
-
tert-butyl [1-cyclohexyl-2-[(3R)-3-([1-(cyclopropylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]-2-oxoethyl]carbamate
-
continuous protease assay
0.000051
-
tert-butyl [2-[(3R)-3-([1-(cyclobutylmethyl)-3-[(2-[[(1S)-2-(dimethylamino)-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino]-2,3-dioxopropyl]carbamoyl)-2-azabicyclo[2.2.1]hept-2-yl]-1-cyclohexyl-2-oxoethyl]carbamate
-
continuous protease assay
0.007
-
trans-1,2-cyclohexanediamine-N,N,N',N'-tetraacetic acid
-
-
0.000001
-
undeca-D-Arg-NH2
-
pH 8.0, 18C
0.00000005
-
vaniprevir
-
in 50 mM HEPES, pH 7.5, 150 mM NaCl, 15% (v/v) glycerol, 0.15% (w/v) Triton X-100, 10 mM dithiothreitol, and 0.1% (w/v) PEG 8000
-
0.000042
-
VX-950
-
NS3/4A genotype 2b
0.000044
-
VX-950
-
-
0.000054
-
VX-950
-
NS3/4A genotype 2a
0.000093
-
VX-950
-
NS3/4A genotype 1b
0.0001
-
VX-950
-
wild-type, pH 7.8, 30C
0.00013
-
VX-950
-
NS3/4A genotype 1a
0.0099
-
VX-950
-
mutant A156T, pH 7.8, 30C
0.033
-
VX-950
-
mutant A156V, pH 7.8, 30C
0.0039
-
[(2R,5S,8S)-8-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-5-cyclohexyl-3,6,14,18-tetraoxo-1,4,7,13-tetraazacyclooctadecan-2-yl]acetic acid
-
-
0.005
-
[(3S,6R,17S)-17-[(1-[[(2-[[(1S)-2-amino-2-oxo-1-phenylethyl]amino]-2-oxoethyl)amino](oxo)acetyl]butyl)carbamoyl]-3-cyclohexyl-2,5,8,11-tetraoxo-1,4,7,12-tetraazacycloheptadecan-6-yl]acetic acid
-
-
0.00000007
-
[(Z)-(1R,4R,6S,15R,17R)-4-cyclopropanesulfonylaminocarbonyl-17-(7-methoxy-2-phenyl-quinolin-4-yloxy)-2,14-dioxo-3,13-diaza-tricyclo[13.3.0.04,6]octadec-7-en-13-yl]-carbamic acid tert-butyl ester
-
-
0.000009
-
[1-[2-(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethylcarbamoyl)-6,6-dichloro-3-aza-bicyclo[3.1.0]hexane-3-carbonyl]-2,2-dimethyl-propyl]-carbamic acid tert-butyl ester
-
-
0.00006
-
[2-[2-(2-carbamoyl-1-cyclobutylmethyl-2-oxo-ethylcarbamoyl)-6,6-dichloro-3-aza-bicyclo[3.1.0]hex-3-yl]-1-indan-2-yl-2-oxo-ethyl]-carbamic acid tert-butyl ester
-
-
0.0000014
-
MK-7009
-
NS3/4A genotype 2b
additional information
-
additional information
-
peptidyl-alphe ketoamides with Ki-values ranging from 0.17 nM to 5.6 mM
-
IC50 VALUE [mM]
IC50 VALUE [mM] Maximum
INHIBITOR
ORGANISM
UNIPROT ACCESSION NO.
COMMENTARY
LITERATURE
IMAGE
0.000008
-
((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(ethyl)phosphinic acid
-
pH and temperature not specified in the publication
0.000006
-
((1R,2S)-1-((2S,4S)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(methyl)phosphinic acid
-
pH and temperature not specified in the publication
0.01855
-
(-)-epicatechin-3-O-gallate
-
-
0.07006
-
(-)-epicatechin-3-O-gallate
-
methylation of the inhibitor
0.00851
-
(-)-epigallocatechin-3-O-gallate
-
-
0.04455
-
(-)-epigallocatechin-3-O-gallate
-
acetylation of the inhibitor
0.05647
-
(-)-epigallocatechin-3-O-gallate
-
methylation of the inhibitor
0.0004
-
(1R)-1-([(4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]heptanoyl]-4-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-L-prolyl]amino)-2-ethenylcyclopropanecarboxylic acid
-
-
0.13
-
(1R)-2-but-3-en-1-yl-1-[[(4R)-1-[(2S)-2-[(tert-butoxycarbonyl)amino]hept-6-enoyl]-4-(quinolin-4-yloxy)-L-prolyl]amino]cyclopropanecarboxylic acid
-
-
0.000001
-
(2R,6R,12Z,13aR,14S,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-([7-methoxy-2-[2-(propan-2-ylamino)-1,3-thiazol-4-yl]quinolin-4-yl]oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14-carboxylic acid
-
pH and temperature not specified in the publication
0.000077
-
(2R,6S,10E,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.004
-
(2R,6S,10E,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-5,16-dioxo-2-(quinolin-4-yloxy)-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.00024
-
(2R,6S,10Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,12,13,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.0001
-
(2R,6S,12Z,14aR,16aS)-2-[(8-chloro-2-ethoxyquinolin-4-yl)oxy]-6-[[(cyclopentyloxy)carbonyl]amino]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.000011
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.0001
-
(2R,6S,12Z,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[[(4-fluoro-1,3-dihydro-2H-isoindol-2-yl)carbonyl]oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.0001
-
(2R,6S,12Z,14aR,16aS)-6-[[(cyclopentyloxy)carbonyl]amino]-2-[(5-ethoxythieno[3,2-b]pyridin-7-yl)oxy]-5,16-dioxo-1,2,3,6,7,8,9,10,11,13a,14,15,16,16a-tetradecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.000028
-
(2R,6S,14aR,16aS)-6-[(tert-butoxycarbonyl)amino]-2-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-5,16-dioxohexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecine-14a(5H)-carboxylic acid
-
-
0.053
-
(3R,12S,16R,17aS)-12-[(tert-butoxycarbonyl)amino]-16-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-1,13-dioxohexadecahydro-1H-pyrrolo[1,2-a][1,4]diazacyclopentadecine-3-carboxylic acid
-
-
0.0075
-
(3S,12S,16R,17aS)-12-[(tert-butoxycarbonyl)amino]-16-[(7-methoxy-2-phenylquinolin-4-yl)oxy]-1,13-dioxohexadecahydro-1H-pyrrolo[1,2-a][1,4]diazacyclopentadecine-3-carboxylic acid
-
-
0.000006
-
(R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(4-methoxybenzyl)phosphinic acid
-
pH and temperature not specified in the publication
0.000086
-
(R)-((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(isopropyl)phosphinic acid
-
pH and temperature not specified in the publication
0.000044
-
(R)-((1S,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)(phenyl)phosphinic acid
-
pH and temperature not specified in the publication
0.000006
-
(R)-(4-chlorobenzyl)((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
pH and temperature not specified in the publication
0.000009
-
(R)-benzyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
pH and temperature not specified in the publication
0.000008
-
(R)-butyl((1R,2S)-1-((2S,4R)-1-((S)-2-(((cyclopentyloxy)carbonyl)amino)-3,3-dimethylbutanoyl)-4-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)pyrrolidine-2-carboxamido)-2-vinylcyclopropyl)phosphinic acid
-
pH and temperature not specified in the publication
0.000003
-
(S)-((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)(2-methoxybenzyl)phosphinic acid
-
pH and temperature not specified in the publication
0.000003
-
(S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
pH and temperature not specified in the publication
0.000001
-
(S)-(2-chlorobenzyl)((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
pH and temperature not specified in the publication
0.000006
-
(S)-benzyl((2R,6R,13aS,14S,16aS)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxooctadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
pH and temperature not specified in the publication
0.000003
-
(S)-benzyl((2R,6R,13aS,14S,16aS,Z)-6-(((cyclopentyloxy)carbonyl)amino)-2-((2-(2-(isopropylamino)thiazol-4-yl)-7-methoxyquinolin-4-yl)oxy)-5,16-dioxo-1,2,3,5,6,7,8,9,10,11,13a,14,14a,15,16,16a-hexadecahydrocyclopropa[e]pyrrolo[1,2-a][1,4]diazacyclopentadecin-14-yl)phosphinic acid
-
pH and temperature not specified in the publication
0.78
-
1,10-phenanthroline
O92972
inhibition of NS2/3 auto-cleavage of mutant H1175A in the absence of NS4A peptide
0.79
-
1,10-phenanthroline
O92972
inhibition of NS2/3 auto-cleavage of the wild-type in the absence of NS4A peptide
0.89
-
1,10-phenanthroline
O92972
inhibition of NS2/3 auto-cleavage of the wild-type in the presence of NS4A peptide
1.56
-
1,10-phenanthroline
O92972
inhibition of mutant H1175A NS3 protease activity in the absence of NS4A peptide
1.9
-
1,10-phenanthroline
O92972
inhibition of wild-type NS3 protease activity in the absence of NS4A peptide
2.1
-
1,10-phenanthroline
O92972
inhibition of mutant H1175A NS3 protease activity in the presence of NS4A peptide
5.9
-
1,10-phenanthroline
O92972
inhibition of wild-type NS3 protease activity in the presence of NS4A peptide
0.00064
-
1,3,4-tri-O-galloyl-beta-D-glucose
-
-
0.00642
-
1,3,6-tri-O-galloyl-beta-D-glucose
-
-
0.0097
-
1-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbonyl]-amino)-2-vinyl-cyclopropanecarboxylic acid
-
IC50: 0.0097 mM
0.33
-
1-([1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-benzyloxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
-
IC50: 0.33 mM
1
-
1-([1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-hydroxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
-
IC50: above 1 mM
0.08
-
1-([1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-phenoxy-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
-
IC50: above 0.08 mM
0.006
-
1-([4-(3'-Acetylamino-biphenyl-3-yloxy)-1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-pyrrolidine-2-carbonyl]-amino)-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
0.00064
-
1-O-(3-O-galloylgalloyl)-2,3,4-tri-O-galloyl-beta-D-glucose
-
-
0.025
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.025 mM
0.2
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(2-thiophen-3-yl-pyridin-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: above 0.2 mM
0.006
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3'-nitro-biphenyl-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
0.05
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.05 mM
0.032
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(3-morpholin-4-yl-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.032 mM
0.2
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4'-methoxy-biphenyl-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: above 0.2 mM
0.035
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4'-methoxy-biphenyl-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.035 mM
0.025
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-bromo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.025 mM
0.04
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-bromo-phenylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.04 mM
0.05
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-chloro-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.05 mM
0.1
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-fluoro-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.1 mM
0.01
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(4-iodo-phenoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.01 mM
0.1
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(5-chloro-quinolin-8-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.1 mM
0.016
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(6-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.016 mM
0.002
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-chloro-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.002 mM
0.0008
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-methoxy-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.0008 mM
0.006
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-trifluoromethyl-quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
0.009
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(7-trifluoromethyl-quinolin-4-ylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.009 mM
0.02
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(benzothiazol-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.02 mM
0.02
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(benzothiazol-2-ylsulfanyl)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.02 mM
0.2
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-2-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: above 0.2 mM
0.006
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.006 mM
0.035
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(biphenyl-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.035 mM
0.008
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(isoquinolin-1-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.008 mM
0.004
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(isoquinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.004 mM
0.31
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2,2-diethyl-cyclopropanecarboxylic acid
-
IC50: 0.31 mM
0.0048
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2-ethyl-cyclopropanecarboxylic acid
-
IC50: 0.0048 mM
0.00063
-
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-2-vinyl-cyclopropanecarboxylic acid
-
IC50: 0.00063 mM
0.014
-
1-[[1-[2-(2-acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(naphthalen-1-ylmethoxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.014 mM
0.19
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(pyridin-3-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.19 mM
0.17
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(pyridin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.17 mM
0.005
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(quinolin-4-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.005 mM
0.25
-
1-[[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-4-(quinolin-8-yloxy)-pyrrolidine-2-carbonyl]-amino]-cyclopropanecarboxylic acid
-
IC50: 0.25 mM
0.2
-
2'-[1-[2-(2-Acetylamino-2-cyclohexyl-acetylamino)-3-methyl-butyryl]-5-(1-carboxy-cyclopropylcarbamoyl)-pyrrolidin-3-yloxy]-biphenyl-4-carboxylic acid
-
IC50: above 0.2 mM