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0.0082
(13alpha,17alpha,20S,24Z)-3-hydroxylanosta-7,24-dien-26-oic acid
Homo sapiens
-
at pH 5.5 and 37°C
0.0091
(13alpha,17alpha,20S,24Z)-3-oxolanosta-7,24-dien-26-oic acid
Homo sapiens
-
at pH 5.5 and 37°C
0.01
(2-fluorobenzophenone) thiosemicarbazone
Homo sapiens
above, pH 6.0, 37°C
0.000574
(2E)-2-(6-bromo-1,1-dioxido-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
Homo sapiens
pH 6.0, 37°C
0.000152
(2E)-2-(6-bromo-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
Homo sapiens
pH 6.0, 37°C
0.000164
(2E)-2-(6-bromo-2,3-dihydroquinolin-4(1H)-ylidene)hydrazinecarbothioamide
Homo sapiens
pH 6.0, 37°C
0.000068
(2E)-2-(6-nitro-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
Homo sapiens
pH 6.0, 37°C
0.00246
(2E)-2-[(2-fluorophenyl)(4-fluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000118
(2E)-2-[(3-bromophenyl)(3,4,5-trifluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000415
(2E)-2-[(3-bromophenyl)(3,5-dichlorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000594
(2E)-2-[(3-bromophenyl)(3,5-difluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000131
(2E)-2-[(3-bromophenyl)(3-chlorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00025
(2E)-2-[(3-bromophenyl)(3-fluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000224
(2E)-2-[(3-bromophenyl)(3-methylphenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01
(2E)-2-[(3-bromophenyl)(4-bromophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.000327
(2E)-2-[(3-bromophenyl)(4-chlorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000796
(2E)-2-[(3-bromophenyl)(4-fluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00216
(2E)-2-[(3-bromophenyl)(4-methylphenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000465
(2E)-2-[(3-bromophenyl)[3-(trifluoromethyl)phenyl]methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000521
(2E)-2-[(3-bromophenyl)[4-(trifluoromethyl)phenyl]methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01
(2E)-2-[(4-bromophenyl)(4-chlorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.00332
(2E)-2-[(4-bromophenyl)(4-fluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00457
(2E)-2-[(4-bromophenyl)(4-methylphenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01
(2E)-2-[(4-bromophenyl)[4-(trifluoromethyl)phenyl]methylidene]hydrazinecarbothioamide
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.01
(2E)-2-[6-(propan-2-yloxy)-2,3-dihydro-4H-thiochromen-4-ylidene]hydrazinecarbothioamide
Homo sapiens
above, pH 6.0, 37°C
0.000096
(2E)-2-[[3,5-bis(trifluoromethyl)phenyl](3-bromophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.5
(2E)-[(3E)-28-methoxy-28-oxours-12-en-3-ylidene]acetic acid
Homo sapiens
-
IC50 above 0.5 mM, at pH 5.5 and 37°C
0.0000019 - 0.00022
(2S,3S)-oxirane-2,3-dicarboxylic acid 2-[((S)-1-benzylcarbamoyl-2-phenyl-ethyl)-amide] 3-[[2-(4-hydroxy-phenyl)-ethyl]-amide]
0.0026
(2Z)-2-[(2-bromophenyl)(3-bromophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01
(2Z)-2-[(2-bromophenyl)(4-bromophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.01
(2Z)-2-[(2-fluorophenyl)(phenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.000233
(2Z)-2-[(3-bromo-2-fluorophenyl)(3-bromophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.000114
(2Z)-2-[(3-bromo-4-fluorophenyl)(3-bromophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000632
(2Z)-2-[(3-bromophenyl)(2,3,4,5-tetrafluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000838
(2Z)-2-[(3-bromophenyl)(2,3-difluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00061
(2Z)-2-[(3-bromophenyl)(2,6-difluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.00161
(2Z)-2-[(3-bromophenyl)(2-chlorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000305
(2Z)-2-[(3-bromophenyl)(2-fluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01
(2Z)-2-[(3-bromophenyl)(2-methylphenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.00222
(2Z)-2-[(4-bromophenyl)(2-fluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.0000305
(3-bromo-2'-fluoro-3'-hydroxybenzophenone) thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.0001314
(3-bromo-3'-hydroxybenzophenone) thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.01
(3-hydroxybenzophenone) thiosemicarbazone
Homo sapiens
above, pH 6.0, 37°C
0.0097
(3E)-3-(carboxymethylidene)olean-12-en-28-oic acid
Homo sapiens
-
at pH 5.5 and 37°C
0.0123
(3E)-3-(carboxymethylidene)urs-12-en-28-oic acid
Homo sapiens
-
at pH 5.5 and 37°C
0.00222
(4-bromo-2'-fluoro-3'-hydroxybenzophenone) thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.000056
1,3,5-trisbenzoylbenzene thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.0000081
1,3-bis(2-fluorobenzoyl)-5-bromobenzene thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.01035
1,3-bis(3-bromobenzoyl)-5-bromobenzene thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.01
1,3-bis(3-bromobenzoyl)-5-hydroxybenzene thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.0000716
1,3-bis(3-hydroxybenzoyl)-5-bromobenzene thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.000654
1,3-bis(3-methylbenzoyl)benzene thisosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.01
1,3-bis(4-bromobenzoyl)benzene bis-thiosemicarbazone
Homo sapiens
above, pH 6.0, 37°C
0.001522
1,3-bis(4-bromobenzoyl)benzene thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.0000144
1,3-bis(4-fluorobenzoyl)benzene thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.00034
1,3-bis(4-hydroxybenzoyl)benzene thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.01
1,3-bis(4-isopropoxybenzoyl)benzene thiosemicarbazone
Homo sapiens
above, pH 6.0, 37°C
0.005117
1,3-bis(4-methoxybenzoyl)benzene thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.00045
1,3-dihydro-pyrrolo[3,4-b]quinoline-2-carbonitrile
Homo sapiens
-
IC50: 0.00045 mM
0.00001
1-cyano-3-azetidinyl cyclohexylmethyl ether
Homo sapiens
-
IC50: 0.00001 mM
0.00043
1-cyanoazetidine
Homo sapiens
-
IC50: 0.00043 mM
0.004
1-cyanopyrrolidine
Homo sapiens
-
IC50: 0.004 mM
0.00236 - 0.109
2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol
0.02 - 0.087
2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
0.01293 - 0.0808
2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
0.000007
2-(3,4-dihydroquinolin-1(2H)-yl)-2-oxoethyl 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarboxylate
Homo sapiens
-
-
0.00241 - 0.0863
2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
0.02 - 0.074
2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
0.01475 - 0.0818
2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
0.01932 - 0.0927
2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide
0.02 - 0.0402
2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
0.0012
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.0011
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.00078
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.000426
2-cyano-4-[(1,4-dioxaspiro[4.5]dec-8-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.0004
2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.002
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.00001
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.0003
2-cyano-4-[[1-(2-hydroxyethyl)piperidin-4-yl]methoxy]-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00051
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.00046
2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00036
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000276
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[4.5]dec-8-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00139
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00012
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
0.00044
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00033
2-cyano-N-methyl-4-[[1-(1-methylethyl)piperidin-4-yl]methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.0007
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.00048
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.00084
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.000044
2-furancarbonyl-leucyl-leucyl-leucinal
Rattus norvegicus
-
pH 5.0, 37°C
0.000007
2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarboxylic 3,4-dihydroquinoline-1(2H)-carboxylic anhydride
Homo sapiens
in 1 mM EDTA, 5 mM cysteine at pH 5.5
0.01
2-[bis(3-bromophenyl)methylidene]-N-ethylhydrazinecarbothioamide
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.01
2-[bis(3-bromophenyl)methylidene]-N-phenylhydrazinecarbothioamide
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.00487
2-[bis(3-fluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
pH and temperature not specified in the publication
0.01
2-[bis(4-bromophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.01
2-[bis(4-fluorophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.00893
2-[cyclohexyl(methyl)amino]-4H-3,1-benzothiazin-4-one
Homo sapiens
-
37°C, pH 6.0
0.00001
3-(benzyloxy)-1-cyanoazetidine
Homo sapiens
-
IC50: 0.00001 mM
0.0026
3-(hydroxyimino)masticadienoic acid
Homo sapiens
-
at pH 5.5 and 37°C
0.0024
3-(hydroxyimino)oleanolic acid
Homo sapiens
-
at pH 5.5 and 37°C
0.0000238
3-benzoylbenzhydrol thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.0065
3-epiursolic acid
Homo sapiens
-
at pH 5.5 and 37°C
0.0072
3-hydroxyolean-12-en-28-oic acid
Homo sapiens
-
at pH 5.5 and 37°C
0.0395
3-hydroxyurs-12-en-28-oic acid
Homo sapiens
-
at pH 5.5 and 37°C
0.00378
3-oxo-urs-12-en-28-oic acid
Leishmania mexicana
pH 6.5, 25°C
0.0147
3-oxoolean-12-en-28-oic acid
Homo sapiens
-
at pH 5.5 and 37°C
0.0083
3-oxours-12-en-28-oic acid
Homo sapiens
-
at pH 5.5 and 37°C
0.00015
3-[(benzyloxy)methyl]-1-cyanopyrrolidine
Homo sapiens
-
IC50: 0.00015 mM
0.00089 - 0.0847
4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline
0.02 - 0.0865
4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid
0.00056 - 0.0621
4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol
0.00215 - 0.0834
4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide
0.0025
4-[(1-acetylpiperidin-4-yl)methoxy]-2-cyano-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00178 - 0.0922
4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide
0.00087
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.00981 - 0.08835
4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol
0.00047 - 0.00193
4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline
0.01749 - 0.0997
4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
0.02 - 0.0655
4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole)
0.00028
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.00338 - 0.0981
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole
0.01706 - 0.0888
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole
0.000096
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00084
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00032
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00026
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000023
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000018
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00037
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00004
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000086
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.0068
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.0052
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.0023
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.0062
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
0.00079
7-(2-cyclohexylethyl)-6-[(pyridin-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
inhibition profiles are determined by a fluorometric assay with recombinant CAT K employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.000057
acetyl-prolyl-leucyl-leucyl-leucinal
Rattus norvegicus
-
pH 5.0, 37°C
0.000019
acetyl-prolyl-prolyl-leucyl-leucyl-leucinal
Rattus norvegicus
-
pH 5.0, 37°C
0.00043
agathisflavone
Leishmania mexicana
pH 6.5, 25°C
0.01
benzophenone thiosemicarbazone
Homo sapiens
above, pH 6.0, 37°C
0.0000099
benzoylbenzophenone thiosemicarbazone
Homo sapiens
pH 6.0, 37°C
0.000054
benzyl 1-cyano-3-pyrrolidinylcarbamate
Homo sapiens
-
IC50: 0.000054 mM
0.000163
benzyloxycarbonyl-leucyl-leucyl-leucinal
Rattus norvegicus
-
pH 5.0, 37°C
0.0011 - 0.0972
bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone
0.000056
cathepsin L inhibitor 1
Homo sapiens
thiocarbazate cathepsin L inhibitor, 20 mM sodium acetate, 1 mM EDTA, 5 mM cysteine at pH 5.5
0.000056
CID 16725315
Homo sapiens
-
pH and temperature not specified in the publication
0.0000069
CID 23631927
Homo sapiens
-
pH and temperature not specified in the publication
0.1
diethyl-cyanamide
Homo sapiens
-
IC50 is above 0.1 mM
0.00003
E-64
Homo sapiens
-
at pH 5.5 and 37°C
0.00002
isonicotinyl-leucyl-leucyl-leucinal
Rattus norvegicus
-
pH 5.0, 37°C
0.1
L-3-trans-propylcarbamoyloxirane-2-carbonyl-L-isoleucyl-L-proline
Trypanosoma brucei
-
IC50 above 0.1 mM, at pH 5.0 and 22°C
0.0008
LFLTR-NH2
Homo sapiens
-
IC50: 0.0008 mM
0.0005
LLLTR-NH2
Homo sapiens
-
IC50: 0.0005 mM
0.25
methyl (13alpha,17alpha,20S,24Z)-3-hydroxylanosta-7,24-dien-26-oate
Homo sapiens
-
IC50 above 0.25 mM, at pH 5.5 and 37°C
0.5
methyl (3Z,13alpha,17alpha,20S,24Z)-3-(hydroxyimino)lanosta-7,24-dien-26-oate
Homo sapiens
-
IC50 above 0.5 mM, at pH 5.5 and 37°C
0.0386
methyl 5-acetyloxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
Homo sapiens
-
pH 5.5, 22°C
0.0616
methyl 5-hydroxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
Homo sapiens
-
pH 5.5, 22°C
0.000048
morpholinylsuccinyl-leucyl-leucyl-leucinal
Rattus norvegicus
-
pH 5.0, 37°C
0.00175
N-(1-cyano-3-pyrrolidinyl)benzamide
Homo sapiens
-
IC50: 0.00175 mM
0.00008
N-(1-cyano-3-pyrrolidinyl)benzenesulfonamide
Homo sapiens
-
IC50: 0.00008 mM
0.00085
N-(1-cyano-3-pyrrolidinyl)[1,1'-biphenyl]-4-carboxamide
Homo sapiens
-
IC50: 0.00085 mM
0.00018
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.000064
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.0001
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.00027
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.01
N-benzyl-2-[bis(3-bromophenyl)methylidene]hydrazinecarbothioamide
Homo sapiens
-
IC50 above 0.01 mM, pH and temperature not specified in the publication
0.023
N-[(1-cyano-2-pyrrolidinyl)methyl]benzamide
Homo sapiens
-
IC50: 0.023 mM
0.0115
N-[(1-cyano-2-pyrrolidinyl)methyl]benzenesulfonamide
Homo sapiens
-
IC50: 0.0115 mM
0.00065
N-[(1-cyano-3-azetidinyl)methyl]benzamide
Homo sapiens
-
IC50: 0.00065 mM
0.00005
N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide
Homo sapiens
-
IC50: 0.00005 mM
0.000006
N-[(1-cyano-3-azetidinyl)methyl]cyclohexanecarboxamide
Homo sapiens
-
IC50: 0.000006 mM
0.00035
N-[(1-cyano-3-pyrrolidinyl)methyl]benzenesulfonamide
Homo sapiens
-
IC50: 0.00035 mM
0.00015
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.00084
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.0015
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.00304 - 0.0625
N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide
0.00283 - 0.0862
N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide
0.000027
nicotinyl-leucyl-leucyl-leucinal
Rattus norvegicus
-
pH 5.0, 37°C
0.01803
quercetin
Leishmania mexicana
pH 6.5, 25°C
0.0006
RKLLW-NH2
Homo sapiens
-
IC50: 0.0006 mM
0.014
RKLWD-NH2
Homo sapiens
-
IC50: 0.014 mM
0.0008
RKLWL-NH2
Homo sapiens
-
IC50: 0.0008 mM
0.00011
S-(2-oxo-1-phenylpyrrolidin-3-yl) 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
Homo sapiens
-
-
0.000041
S-[2-(3,4-dihydroquinolin-1(2H)-yl)-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
Homo sapiens
-
-
0.000001 - 0.000056
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
0.000115
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-phenylpropanoyl]hydrazinecarbothioate
Homo sapiens
-
-
0.033
S-{2-[(2-ethylphenyl)amino]-2-oxoethyl} 2-[(2R)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
Homo sapiens
thiocarbazate cathepsin L inhibitor, 1 mM EDTA, 5 mM cysteine at pH 5.5
0.0022
tetrahydrorobustaflavone
Leishmania mexicana
pH 6.5, 25°C
additional information
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetic acid
0.0000019
(2S,3S)-oxirane-2,3-dicarboxylic acid 2-[((S)-1-benzylcarbamoyl-2-phenyl-ethyl)-amide] 3-[[2-(4-hydroxy-phenyl)-ethyl]-amide]
Rattus norvegicus
-
-
0.00022
(2S,3S)-oxirane-2,3-dicarboxylic acid 2-[((S)-1-benzylcarbamoyl-2-phenyl-ethyl)-amide] 3-[[2-(4-hydroxy-phenyl)-ethyl]-amide]
Trypanosoma brucei
-
at pH 5.0 and 22°C
0.00236
2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol
Trypanosoma brucei brucei
above, pH 7.4, 37°C
0.109
2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol
Homo sapiens
pH 7.4, 37°C
0.02
2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
Trypanosoma brucei brucei
above, pH 7.4, 37°C
0.02
2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.087
2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
Homo sapiens
pH 7.4, 37°C
0.01293
2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Trypanosoma brucei brucei
pH 7.4, 37°C
0.02
2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.0808
2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Homo sapiens
pH 7.4, 37°C
0.00241
2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02002
2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Trypanosoma brucei brucei
pH 7.4, 37°C
0.0863
2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Homo sapiens
pH 7.4, 37°C
0.02
2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
Trypanosoma brucei brucei
above, pH 7.4, 37°C
0.02
2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.074
2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
Homo sapiens
pH 7.4, 37°C
0.01475
2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Trypanosoma brucei brucei
pH 7.4, 37°C
0.02
2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.0818
2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
Homo sapiens
pH 7.4, 37°C
0.01932
2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide
Trypanosoma brucei brucei
pH 7.4, 37°C
0.02
2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.0927
2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide
Homo sapiens
pH 7.4, 37°C
0.02
2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
Trypanosoma brucei brucei
above, pH 7.4, 37°C
0.02
2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.0402
2-(furan-2-yl)-4-[8-[2-(furan-2-yl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
Homo sapiens
pH 7.4, 37°C
0.00012
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
0.00012
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
inhibition are determined by a fluorometric assay with recombinant Cat L
0.00089
4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.0058
4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline
Trypanosoma brucei brucei
pH 7.4, 37°C
0.0847
4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline
Homo sapiens
pH 7.4, 37°C
0.02
4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid
Trypanosoma brucei brucei
above, pH 7.4, 37°C
0.02
4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.0865
4-(4-[8-[2-(4-carboxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)benzoic acid
Homo sapiens
pH 7.4, 37°C
0.00056
4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.01179
4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol
Trypanosoma brucei brucei
pH 7.4, 37°C
0.0621
4-(4-[8-[2-(4-hydroxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazol-2-yl)phenol
Homo sapiens
pH 7.4, 37°C
0.00215
4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide
Trypanosoma brucei brucei
above, pH 7.4, 37°C
0.0834
4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide
Homo sapiens
pH 7.4, 37°C
0.00178
4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide
Trypanosoma brucei brucei
above, pH 7.4, 37°C
0.0922
4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide
Homo sapiens
pH 7.4, 37°C
0.00981
4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol
Trypanosoma brucei brucei
pH 7.4, 37°C
0.02
4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.08835
4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol
Homo sapiens
pH 7.4, 37°C
0.00047
4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.00193
4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline
Trypanosoma brucei brucei
pH 7.4, 37°C
0.01749
4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
Trypanosoma brucei brucei
pH 7.4, 37°C
0.02
4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.0997
4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
Homo sapiens
pH 7.4, 37°C
0.02
4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole)
Trypanosoma brucei brucei
above, pH 7.4, 37°C
0.02
4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole)
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.0655
4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole)
Homo sapiens
pH 7.4, 37°C
0.00338
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.01831
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole
Trypanosoma brucei brucei
pH 7.4, 37°C
0.0981
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole
Homo sapiens
pH 7.4, 37°C
0.01706
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole
Trypanosoma brucei brucei
pH 7.4, 37°C
0.02
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.0888
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole
Homo sapiens
pH 7.4, 37°C
0.0011
bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone
Trypanosoma brucei brucei
above, pH 7.4, 37°C
0.0972
bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone
Homo sapiens
pH 7.4, 37°C
0.00304
N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide
Trypanosoma brucei rhodesiense
pH 5.5, 25°C
0.02
N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide
Trypanosoma brucei brucei
above, pH 7.4, 37°C
0.0625
N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide
Homo sapiens
pH 7.4, 37°C
0.00283
N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide
Trypanosoma brucei brucei
pH 7.4, 37°C
0.02
N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide
Trypanosoma brucei rhodesiense
above, pH 5.5, 25°C
0.0862
N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide
Homo sapiens
pH 7.4, 37°C
0.000001
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
Homo sapiens
-
pH 5.5, preincubation with enzyme 4 h before substrate addition
0.0000075
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
Homo sapiens
-
pH 5.5, preincubation with enzyme 1 h before substrate addition
0.000056
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
Homo sapiens
-
-
0.000056
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
Homo sapiens
-
pH 5.5
additional information
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetic acid
Homo sapiens
-
KI value is above 5 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.001 mM, determined by a fluorometric assay with recombinant catL employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.002 mM, inhibition are determined by a fluorometric assay with recombinant Cat L
additional information
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.003 mM, inhibition are determined by a fluorometric assay with recombinant Cat L
additional information
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.003 mM inhibition are determined by a fluorometric assay with recombinant Cat L
additional information
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.003 mM inhibition are determined by a fluorometric assay with recombinant Cat L
additional information
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
Homo sapiens
IC50 is above 0.003 mM inhibition are determined by a fluorometric assay with recombinant Cat L
additional information
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzoic acid
Homo sapiens
-
KI value is above 2 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(2-piperidin-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 4 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(4-acetyl-1,4-diazepan-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 is above 1 M, with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
IC50 is above 0.01 mM, Z-Phe-Arg-7-amino-4-methylcumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)-3-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 is above 1 M, with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 is above 2 M, with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
IC50 is above 0.01 mM, Z-Phe-Arg-7-amino-4-methylcumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 4 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Rattus norvegicus
-
IC50 is above 0.01 mM, Z-Phe-Arg-7-amino-4-methylcumarin as substrate
additional information
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
IC50 is above 1 M, with Z-Phe-Arg-7-amido-4-methylcoumarin as substrate
additional information
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
7-(2-cyclohexylethyl)-6-[(pyridin-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
CLIK-148
Homo sapiens
IC50 value is below 0.0001 mM, in 1 mM EDTA, 5 mM cysteine at pH 5.5
additional information
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate
additional information
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)propanamide
Homo sapiens
-
KI value is above 1 microM, inhibition profiles are determined by a fluorometric assay with recombinant CAT L employing Z-Phe-Arg-7-amido-4-methylcoumarin as synthetic substrate