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Literature summary for 3.4.24.83 extracted from

  • Goldberg, A.B.; Turk, B.E.
    Inhibitors of the metalloproteinase anthrax lethal factor (2016), Curr. Top. Med. Chem., 16, 2350-2358 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(2R)-2-[(4-fluoro-3-methylbenzene-1-sulfonyl)amino]-N-hydroxy-2-(oxan-4-yl)acetamide i.e. L915 Bacillus anthracis
(2S)-2-(3,4-dichlorophenyl)-N-hydroxy-3-(3-methylphenyl)propanamide
-
Bacillus anthracis
(2S)-2-(4-fluoro-3,5-dimethylbenzyl)-6-[[1-(4-fluorophenyl)propyl]amino]-N-hydroxyhexanamide i.e. PT-8541 Bacillus anthracis
(2S)-2-[(2R)-2-(4-fluorophenyl)-2-methoxyethyl]-6-[[1-(4-fluorophenyl)propyl]amino]-N-hydroxyhexanamide i.e. PT-8420 Bacillus anthracis
(2S)-6-[(4-fluorobenzyl)amino]-2-[(2R)-2-(4-fluorophenyl)-2-methoxyethyl]-N-hydroxyhexanamide i.e. LFI4 Bacillus anthracis
(D-Arg)9-Trp-Leu-Met-CONHOH
-
Bacillus anthracis
(D-Arg)9-Val-Leu-Arg-CONHOH
-
Bacillus anthracis
1,4-dihydroxy-10-methoxy-5,8-dimethyl-3,7-dioxo-1,3-dihydro-7H-2,6,12-trioxabenzo[5,6]cyclohepta[1,2-e]indene-11-carbaldehyde i.e. stictic acid Bacillus anthracis
1-[([1,1'-biphenyl]-4-yl)methyl]-3-hydroxy-2-methylpyridine-4(1H)-thione i.e. 94G5 Bacillus anthracis
2-[[benzyl(ethyl)amino]methyl]-4,6-diiodophenol
-
Bacillus anthracis
2-[[benzyl(ethyl)amino]methyl]-4-bromophenol
-
Bacillus anthracis
2-[[benzyl(ethyl)amino]methyl]-4-chlorophenol
-
Bacillus anthracis
3,5-diphenyl-2,6-bis(sulfanyl)-4H-thiopyran-4-one
-
Bacillus anthracis
3-(benzyloxy)-1-(3,4-dichlorobenzene-1-sulfonyl)-N-hydroxypyrrolidine-2-carboxamide
-
Bacillus anthracis
4-methyl-N-[(1R)-1-[5-(naphthalen-1-yl)-2-(prop-2-en-1-yl)tetrahydrofuran-3-yl]ethyl]benzenesulfonamide i.e. SM157, non-competitive inhibition Bacillus anthracis
5-[4-[(E)-2-[(2R,3R,3'R)-3'-(3,5-dihydroxyphenyl)-6'-hydroxy-2,2'-bis(4-hydroxyphenyl)-2,2',3,3'-tetrahydro-3,4'-bi-1-benzofuran-5-yl]ethenyl]-6-hydroxy-2-(3-hydroxyphenyl)-2,3-dihydro-1-benzofuran-3-yl]benzene-1,3-diol
-
Bacillus anthracis
N,N'-bis(4-amino-2-methylquinolin-6-yl)urea i.e. NSC12155, competitive inhibition Bacillus anthracis
N-(4-amino-2-methylquinolin-6-yl)-3-(2-methoxyphenyl)propanamide
-
Bacillus anthracis
N-(4-amino-2-methylquinolin-6-yl)-4-(quinolin-6-yl)benzamide
-
Bacillus anthracis
N-[([1,1'-biphenyl]-4-yl)methyl]-3-hydroxy-4-sulfanylidene-4H-pyran-2-carbothioamide
-
Bacillus anthracis
N-[([1,1'-biphenyl]-4-yl)methyl]-3-hydroxy-6-methyl-4-sulfanylidene-4H-pyran-2-carboxamide i.e. AM-2S Bacillus anthracis
N-[3-(1,3-benzothiazol-2-yl)-4-methylthiophen-2-yl]-4-chlorobenzene-1-sulfonamide
-
Bacillus anthracis
N-[3-(1,3-benzothiazol-2-yl)thiophen-2-yl]-4'-methoxy[1,1'-biphenyl]-4-sulfonamide
-
Bacillus anthracis

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
mitogen-activated protein kinase kinase 1 + H2O Bacillus anthracis
-
?
-
?

Organism

Organism UniProt Comment Textmining
Bacillus anthracis P15917
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
mitogen-activated protein kinase kinase 1 + H2O
-
Bacillus anthracis ?
-
?

Subunits

Subunits Comment Organism
? x * 90000, SDS-PAGE Bacillus anthracis

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0000003
-
(D-Arg)9-Trp-Leu-Met-CONHOH pH and temperature not specified in the publication Bacillus anthracis
0.001
-
N-[3-(1,3-benzothiazol-2-yl)thiophen-2-yl]-4'-methoxy[1,1'-biphenyl]-4-sulfonamide pH and temperature not specified in the publication Bacillus anthracis
0.0092
-
4-methyl-N-[(1R)-1-[5-(naphthalen-1-yl)-2-(prop-2-en-1-yl)tetrahydrofuran-3-yl]ethyl]benzenesulfonamide pH and temperature not specified in the publication Bacillus anthracis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0015
-
pH and temperature not specified in the publication Bacillus anthracis N-(4-amino-2-methylquinolin-6-yl)-3-(2-methoxyphenyl)propanamide
0.003
-
pH and temperature not specified in the publication Bacillus anthracis N-(4-amino-2-methylquinolin-6-yl)-4-(quinolin-6-yl)benzamide
0.039
-
pH and temperature not specified in the publication Bacillus anthracis 5-[4-[(E)-2-[(2R,3R,3'R)-3'-(3,5-dihydroxyphenyl)-6'-hydroxy-2,2'-bis(4-hydroxyphenyl)-2,2',3,3'-tetrahydro-3,4'-bi-1-benzofuran-5-yl]ethenyl]-6-hydroxy-2-(3-hydroxyphenyl)-2,3-dihydro-1-benzofuran-3-yl]benzene-1,3-diol