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(((2S,3S)-epoxysuccinyl-(S)-leucyl)amino)-4-guanidinobutane
-
-
(13alpha,17alpha,20S,24Z)-3-hydroxylanosta-7,24-dien-26-oic acid
-
competitive inhibition
(13alpha,17alpha,20S,24Z)-3-oxolanosta-7,24-dien-26-oic acid
-
competitive inhibition
(2-fluorobenzophenone) thiosemicarbazone
-
(2E)-1,3-diphenylprop-2-en-1-one
33% inhibition of FhCL1; 4% inhibition of FhCL3
(2E)-1-(2-hydroxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one
26% inhibition of FhCL1; 37% inhibition of FhCL3
(2E)-1-(2-hydroxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
3% inhibition of FhCL3; 48% inhibition of FhCL1
(2E)-1-(2-hydroxyphenyl)-3-(4-phenoxyphenyl)prop-2-en-1-one
16% inhibition of FhCL3; 8% inhibition of FhCL1
(2E)-1-(2-hydroxyphenyl)-3-(pyridin-2-yl)prop-2-en-1-one
20% inhibition of FhCL19; 54% inhibition of FhCL1
(2E)-1-(2-hydroxyphenyl)-3-(thiophen-2-yl)prop-2-en-1-one
52% inhibition of FhCL1; 9% inhibition of FhCL3
(2E)-1-(2-hydroxyphenyl)-3-phenylprop-2-en-1-one
16% inhibition of FhCL2
(2E)-1-(2-hydroxyphenyl)-3-[4-(methylsulfanyl)phenyl]prop-2-en-1-one
19% inhibition of FhCL3
(2E)-1-(7-hydroxynaphthalen-1-yl)-3-(naphthalen-1-yl)prop-2-en-1-one
a slow-reversible inhibitor that interacts with the Cys-His catalytic dyad and key S2 and S3 pocket residues, causing 65% inhibition of FhCL3, enzyme binding structure by molecular docking, overview. Analysis of fasciolicide activity of C34 on vitro cultu; a slow-reversible inhibitor that interacts with the Cys-His catalytic dyad and key S2 and S3 pocket residues, causing 75% inhibition of FhCL1, enzyme binding structure by molecular docking, overview. Analysis of fasciolicide activity of C34 on vitro cultu
(2E)-1-(7-hydroxynaphthalen-1-yl)-3-(naphthalen-2-yl)prop-2-en-1-one
44% inhibition of FhCL3; 67% inhibition of FhCL1
(2E)-1-(8-hydroxynaphthalen-2-yl)-3-(naphthalen-2-yl)prop-2-en-1-one
29% inhibition of FhCL3; 65% inhibition of FhCL1
(2E)-1-(naphthalen-2-yl)-3-phenylprop-2-en-1-one
13% inhibition of FhCL3; 65% inhibition of FhCL1
(2E)-1-phenyl-3-(pyridin-2-yl)prop-2-en-1-one
4% inhibition of FhCL3; 8% inhibition of FhCL1
(2E)-2-(6-bromo-1,1-dioxido-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
-
(2E)-2-(6-bromo-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
-
(2E)-2-(6-bromo-2,3-dihydroquinolin-4(1H)-ylidene)hydrazinecarbothioamide
-
(2E)-2-(6-nitro-2,3-dihydro-4H-thiochromen-4-ylidene)hydrazinecarbothioamide
-
(2E)-2-(7-bromo-3,4-dihydronaphthalen-1(2H)-ylidene)hydrazinecarbothioamide
-
-
(2E)-2-[(2-fluorophenyl)(4-fluorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)(3,4,5-trifluorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)(3,5-dichlorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)(3,5-difluorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)(3-chlorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)(3-fluorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)(3-methylphenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)(4-bromophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)(4-chlorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)(4-fluorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)(4-methylphenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)[3-(trifluoromethyl)phenyl]methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(3-bromophenyl)[4-(trifluoromethyl)phenyl]methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(4-bromophenyl)(4-chlorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(4-bromophenyl)(4-fluorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(4-bromophenyl)(4-methylphenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[(4-bromophenyl)[4-(trifluoromethyl)phenyl]methylidene]hydrazinecarbothioamide
-
-
(2E)-2-[6-(propan-2-yloxy)-2,3-dihydro-4H-thiochromen-4-ylidene]hydrazinecarbothioamide
-
(2E)-2-[[3,5-bis(trifluoromethyl)phenyl](3-bromophenyl)methylidene]hydrazinecarbothioamide
-
-
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one
11% inhibition of FhCL1; 19% inhibition of FhCL3
(2E)-3-(2-bromophenyl)-1-(2-hydroxyphenyl)prop-2-en-1-one
29% inhibition of FhCL1; 33% inhibition of FhCL3
(2E)-3-(3,4-dimethoxyphenyl)-1-phenylprop-2-en-1-one
2% inhibition of FhCL3; 35% inhibition of FhCL1
(2E)-3-(4-aminophenyl)-1-phenylprop-2-en-1-one
2% inhibition of FhCL3; 4% inhibition of FhCL1
(2E)-3-(4-bromophenyl)-1-(2-hydroxyphenyl)prop-2-en-1-one
12% inhibition of FhCL3; 19% inhibition of FhCL1
(2E)-3-(4-bromophenyl)-1-phenylprop-2-en-1-one
12% inhibition of FhCL3; 52% inhibition of FhCL1
(2E)-3-(4-chlorophenyl)-1-(2-hydroxyphenyl)prop-2-en-1-one
23% inhibition of FhCL3; 63% inhibition of FhCL1
(2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-one
25% inhibition of FhCL1; 6% inhibition of FhCL43
(2E)-3-(4-methoxyphenyl)-1-phenylprop-2-en-1-one
48% inhibition of FhCL1; 4% inhibition of FhCL3
(2E)-3-(furan-2-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one
4% inhibition of FhCL3; 57% inhibition of FhCL1
(2E)-3-(naphthalen-1-yl)-1-phenylprop-2-en-1-one
17% inhibition of FhCL1; 27% inhibition of FhCL3
(2E)-3-[4-(dimethylamino)phenyl]-1-(2-hydroxyphenyl)prop-2-en-1-one
20% inhibition of FhCL3; 34% inhibition of FhCL1
(2E)-3-[4-(methylsulfanyl)phenyl]-1-phenylprop-2-en-1-one
26% inhibition of FhCL3; 8% inhibition of FhCL1
(2E)-N'-(2-[(naphthalen-1-ylmethyl)sulfanyl]acetyl)-3-phenylprop-2-enehydrazide
-
(2E)-[(3E)-28-methoxy-28-oxours-12-en-3-ylidene]acetic acid
-
competitive inhibition
(2R,3R)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-prolyl]-aziridine-2,3-dicarboxylate
-
-
(2R,3R)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(R)-azetidine-2-carbonyl]aziridine-2,3-dicarboxylate
-
-
(2R,3R)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(R)-nipecotyl]aziridine-2,3-dicarboxylate
-
-
(2R,3R)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-azetidine-2-carbonyl]aziridine-2,3-dicarboxylate
-
-
(2R,3R)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-nipecotyl]aziridine-2,3-dicarboxylate
-
-
(2R,3R)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-isonipecotyl]-aziridine-2,3-dicarboxylate
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-(R)-leucyl-(S)-nipecotyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-(R)-phenylalanyl-(R)-alanyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-(R)-phenylalanyl-(S)-alanyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(R)-nipecotyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-nipecotyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-prolyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-isonipecotyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-(S)-phenylalanyl-(R)-alanyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-(S)-phenylalanyl-(S)-alanyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-glycyl-(R)-nipecotyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-glycyl-(R)-prolyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-glycyl-(S)-nipecotyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-1-[N-(tert-butoxycarbonyl)-glycyl-(S)-prolyl]aziridine-2,3-dicarboxylic acid
-
-
(2S,3S)-3-([(2S)-1-[(8-carbamimidamidooctyl)amino]-4-methyl-1-oxopentan-2-yl]carbamoyl)oxirane-2-carboxylic acid
-
-
(2S,3S)-dibenzyl-1-[1-[N-(tert-butoxycarbonyl)-(R)-leucyl]-(S)-aziridine-2-carbonyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[1-[N-(tert-butoxycarbonyl)-(S)-leucyl]-(S)-aziridine-2-carbonyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[biotinyl-6-aminohexanoyl]-aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(R)-leucyl-(R)-nipecotyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(R)-leucyl-(R)-prolyl]-aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(R)-leucyl-(S)-nipecotyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(R)-leucyl-(S)-prolyl]-aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(R)-phenylalanyl-(R)-alanyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(R)-phenylalanyl-(S)-alanyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(R)-azetidine-2-carbonyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(R)-nipecotyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(R)-prolyl]-aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-azetidine-2-carbonyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-nipecotyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(S)-phenylalanyl-(R)-alanyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(S)-phenylalanyl-(S)-alanyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-glycyl-(R)-nipecotyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-glycyl-(R)-prolyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-glycyl-(R+S)-nipecotyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-glycyl-(S)-pipecolyl]-aziridine-2,3-dicarboxylate
-
-
(2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-glycyl-(S)-prolyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(R)-nipecotyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-nipecotyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-prolyl]aziridine-2,3-dicarboxylate
-
-
(2S,3S)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-isonipecotyl]-aziridine-2,3-dicarboxylate
-
-
(2S,3S)-oxirane-2,3-dicarboxylic acid 2-[((S)-1-benzylcarbamoyl-2-phenyl-ethyl)-amide] 3-[[2-(4-hydroxy-phenyl)-ethyl]-amide]
(2S,3S)-trans-epoxysuccinyl-L-leucylamido-3-methylbutane ethyl ester
0.1 mM
(2S,3S+2R,3R)-dibenzyl-1-[desthiobiotinyl-6-aminohexanoyl]-aziridine-2,3-dicarboxylate
-
-
(2Z)-1-[(12R)-22-amino-12-[(1S)-2-(4-benzoylphenyl)-1-[[(benzyloxy)carbonyl]amino]ethyl]-6,13,22-trioxo-17,20-dioxa-7,14-diazadocos-1-yl]-2-[(2E)-3-(1-ethyl-3,3-dimethyl-5-sulfo-2,3-dihydro-1H-indol-2-yl)prop-2-en-1-ylidene]-3,3-dimethyl-2,3-dihydro-1H-indole-5-sulfonic acid
-
(2Z)-2-[(2-bromophenyl)(3-bromophenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[(2-bromophenyl)(4-bromophenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[(2-fluorophenyl)(phenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[(3-bromo-2-fluorophenyl)(3-bromophenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[(3-bromo-4-fluorophenyl)(3-bromophenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[(3-bromophenyl)(2,3,4,5-tetrafluorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[(3-bromophenyl)(2,3-difluorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[(3-bromophenyl)(2,6-difluorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[(3-bromophenyl)(2-chlorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[(3-bromophenyl)(2-fluorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[(3-bromophenyl)(2-methylphenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[(4-bromophenyl)(2-fluorophenyl)methylidene]hydrazinecarbothioamide
-
-
(2Z)-2-[[3,5-bis(trifluoromethyl)phenyl](4-methylphenyl)methylidene]hydrazinecarbothioamide
-
-
(3-bromo-2'-fluoro-3'-hydroxybenzophenone) thiosemicarbazone
-
(3-bromo-3'-hydroxybenzophenone) thiosemicarbazone
a slowly reversible inhibitor of cathepsin L
(3-hydroxybenzophenone) thiosemicarbazone
-
(3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
(3E)-3-(carboxymethylidene)olean-12-en-28-oic acid
-
competitive inhibition
(3E)-3-(carboxymethylidene)urs-12-en-28-oic acid
-
competitive inhibition
(4-bromo-2'-fluoro-3'-hydroxybenzophenone) thiosemicarbazone
-
(E)N-[(S)1-[(S)2-cyano-1-pyrrolidinecarbonyl]-3-methylbutyl]-2,3-diphenylacrylamide
-
selective towards cathepsin L over cathepsin B
(L-3-trans-carboxyoxirane-2-carbonyl)-L-leucine(3-methylbutyl)-amide
-
0.01 mg/ml
(L-3-trans-propylcarbamoyloxirane-2-carbonyl)-L-isoleucyl-L-proline methyl ester
-
CA-074Me, more than 99% inhibition at 0.1 mM
(N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide)
(R)-S-2-(2-ethylphenylamino)-2-oxoethyl 2-(2-(tert-butoxycarbonylamino)-3-(1H-indol-3-yl)propanoyl)hydrazinecarbothioate
R-enantiomer, thiol ester containing a diacyl hydrazine functionality and one stereogenic center
(S)-2-(3,4-dihydroquinolin-1(2H)-yl)-2-oxoethyl 2-(2-(tert-butoxycarbonylamino)-3-(1H-indol-3-yl)propanoyl)hydrazinecarboxylate
-
(S)-S-2-(2-ethylphenylamino)-2-oxoethyl 2-(2-(tert-butoxycarbonylamino)-3-(1H-indol-3-yl)propanoyl)hydrazinecarbothioate
S-enantiomer, thiol ester containing a diacyl hydrazine functionality and one stereogenic center
1,3,5-trisbenzoylbenzene thiosemicarbazone
-
1,3-bis(2-fluorobenzoyl)-5-bromobenzene thiosemicarbazone
molecular docking in the active site
1,3-bis(3-bromobenzoyl)-5-bromobenzene thiosemicarbazone
-
1,3-bis(3-bromobenzoyl)-5-hydroxybenzene thiosemicarbazone
-
1,3-bis(3-hydroxybenzoyl)-5-bromobenzene thiosemicarbazone
-
1,3-bis(3-methylbenzoyl)benzene thisosemicarbazone
-
1,3-bis(4-bromobenzoyl)benzene bis-thiosemicarbazone
-
1,3-bis(4-bromobenzoyl)benzene thiosemicarbazone
-
1,3-bis(4-fluorobenzoyl)benzene thiosemicarbazone
-
1,3-bis(4-hydroxybenzoyl)benzene thiosemicarbazone
-
1,3-bis(4-isopropoxybenzoyl)benzene thiosemicarbazone
-
1,3-bis(4-methoxybenzoyl)benzene thiosemicarbazone
-
1,3-dihydro-pyrrolo[3,4-b]quinoline-2-carbonitrile
-
IC50: 0.00045 mM
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([2-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-methyl-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([3-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-3-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(pyridin-4-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[(thiophen-2-ylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([4-[methyl(methylsulfonyl)amino]phenyl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(methylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-([(2S)-3-(1-methylcyclopentyl)-2-[([6-[(phenylsulfonyl)amino]pyridin-3-yl]carbonyl)amino]propanoyl]amino)-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-([[4-([[(dimethylamino)methyl]sulfonyl]amino)phenyl]carbonyl]amino)-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([2-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-fluoro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([3-methoxy-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[([4-[(ethylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2,4-dimethyl-1,3-thiazol-5-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(2-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(3-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-fluorophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-2-[[(4-[[(4-methoxyphenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-(methylsulfamoyl)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-([[4-([[4-(1-methylethyl)-1,3-thiazol-2-yl]sulfonyl]amino)phenyl]carbonyl]amino)propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-sulfamoylphenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methyl-1H-imidazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(1-methylethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2,2,2-trifluoroethyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(2-methylphenyl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(4-methylpyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[(2S)-3-(1-methylcyclopentyl)-2-[[(4-[[(5-methyl-1,3-thiazol-2-yl)sulfonyl]amino]phenyl)carbonyl]amino]propanoyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3,5,6-trideoxy-3-[[4-methyl-N-(thiophen-3-ylcarbonyl)-L-leucyl]amino]-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([3-chloro-4-[(phenylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(benzylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(butylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[([4-[(cyclopropylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-chloropyridin-3-yl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(2-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(3-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(4-cyanophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1,4-anhydro-3-[[(2S)-2-[[(4-[[(cyclohexylmethyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
1- (L-trans-epoxysuccinyl-leucylamino)-4-guanidinobutane
-
i.e. E-64, 0.1 mM, complete loss of activity
1-cyano-3-azetidinyl cyclohexylmethyl ether
-
IC50: 0.00001 mM
1-cyanoazetidine
-
IC50: 0.00043 mM
1-cyanopyrrolidine
-
IC50: 0.004 mM
1-hydroxy-6-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]-2,1,3-benzoxadiazol-1-ium
21% inhibition of FhCL1; 26% inhibition of FhCL3
1-N-[3,5-bis (trifluoromethyl) phenyl]-2-N-(1-ethynylcyclohexyl) benzene-1,2-dicarboxamide
-
1-naphthalenesulfonyl-Ile-Trp-aldehyde
1-naphthalenesulfonyl-Ile-Trp-CHO
-
reversible inhibitor of cathepsin L
1-nathalenesulfonyl-Ile-Trp-CHO
-
treatment of cells results in suppression of cellular proliferation and the induction of a cell death with no detecable caspase-3 activation or DNA fragmentation. Cell death is associated with increased accumulation of cathepsin D, cellular vacuolization, expression of the mannose 6-phosphate recepto, and the autophagy marker LC-II
1-[(1E)-3-phenylprop-1-en-1-yl]naphthalene
38% inhibition of FhCL1; 39% inhibition of FhCL3
2,3,7,8-tetrachlorodibenzodioxin
-
treatment of cells results in resistance to apoptosis, increased expression of the tumor marker cathepsin L, and a high degree of invasiveness
2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol
2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
2-(3,4-dihydroquinolin-1(2H)-yl)-2-oxoethyl 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarboxylate
-
unreactive to transesterification by cysteine and dithiothreitol nucleophiles. Inhibitor remains intact for greater than 24 h when incubated with cathepsin L under stoichiometric conditions, and in the presence of assay buffer
2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
2-(4-bromophenyl)-4H-chromen-4-one
19% inhibition of FhCL3; 21% inhibition of FhCL1
2-(4-chlorophenyl)-4H-chromen-4-one
17% inhibition of FhCL3
2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide
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
2-([4-benzyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl]sulfanyl)-1-(1,2,3,4-tetrahydroquinolin-1-yl)ethan-1-one
-
2-cyano-4-(2-hydroxyethoxy)-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-4-(cyclohexylamino)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-(cyclohexylmethoxy)-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(1,4-dioxaspiro[4.5]dec-8-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
-
2-cyano-4-[(2-cyclopentylethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
-
2-cyano-4-[(6,8-dioxaspiro[3.5]non-7-ylmethyl)amino]-N-methyl-6-[(1-methylpiperidin-4-yl)methoxy]pyrimidine-5-carboxamide
-
2-cyano-4-[(cyclohexylmethyl)(methyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[(cyclohexylmethyl)amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-N-(2-phenylethyl)-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-difluorocyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[[(4,4-dimethylcyclohexyl)methyl]amino]-N-(2-phenylethyl)pyrimidine-5-carboxamide
-
2-cyano-4-[[1-(2-hydroxyethyl)piperidin-4-yl]methoxy]-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(1-methyl-4-phenylpiperidin-4-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(2-phenylethyl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-(4,5-dimethoxybiphenyl-2-yl)-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-(piperidin-4-ylmethoxy)-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[4.5]dec-8-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-[(spiro[3.5]non-7-ylmethyl)amino]-6-[(2,2,6,6-tetramethylpiperidin-4-yl)oxy]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-methyl-4-[[1-(1-methylethyl)piperidin-4-yl]methoxy]-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[(1-methyl-4-phenylpiperidin-4-yl)methyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[(1R)-2-pyridin-2-yl-1-(pyrrolidin-1-ylmethyl)ethyl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-cyano-N-[5-[(1-methylpiperidin-4-yl)oxy]biphenyl-2-yl]-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
2-furancarbonyl-leucyl-leucyl-leucinal
-
-
2-hydroxy-4-[(1E)-3-(2-hydroxyphenyl)-3-oxoprop-1-en-1-yl]-1,2,5-oxadiazol-2-ium
14% inhibition of FhCL3; 48% inhibition of FhCL1
2-mercaptoethanol
-
50% activity at 2 mM
2-phenyl-4H-chromen-4-one
5% inhibition of FhCL1; 8% inhibition of FhCL3
2-[(1E)-3-phenylprop-1-en-1-yl]naphthalene
38% inhibition of FhCL3; 62% inhibition of FhCL1
2-[(2E)-3-(naphthalen-1-yl)prop-2-en-1-yl]phenol
32% inhibition of FhCL3; 42% inhibition of FhCL1
2-[(2E)-3-(naphthalen-2-yl)prop-2-en-1-yl]phenol
41% inhibition of FhCL3; 61% inhibition of FhCL1
2-[bis(3-bromophenyl)methylidene]-N-ethylhydrazinecarbothioamide
-
-
2-[bis(3-bromophenyl)methylidene]-N-phenylhydrazinecarbothioamide
-
-
2-[bis(3-fluorophenyl)methylidene]hydrazinecarbothioamide
-
-
2-[bis(4-bromophenyl)methylidene]hydrazinecarbothioamide
-
-
2-[bis(4-fluorophenyl)methylidene]hydrazinecarbothioamide
-
-
2-[cyclohexyl(methyl)amino]-4H-3,1-benzothiazin-4-one
-
selective towards cathepsin L over cathepsin G, chymotrypsin, trypsin, human angiotensin-converting enzyme, human leukocyte elastase, acetylcholinesterase
2RS,3RS)-2-benzyl-3-ethyl-1-[N-(benzyloxycarbonyl)-glycyl-(S)-prolyl]aziridine-2,3-dicarboxylate
-
-
3-(benzyloxy)-1-cyanoazetidine
-
IC50: 0.00001 mM
3-(hydroxyimino)masticadienoic acid
-
competitive inhibition
3-(hydroxyimino)oleanolic acid
-
competitive inhibition
3-benzoylbenzhydrol thiosemicarbazone
-
3-chloro-N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]benzamide
-
pH and temperature not specified in the publication
3-epiursolic acid
-
competitive inhibition
3-hydroxyolean-12-en-28-oic acid
-
competitive inhibition
3-hydroxyurs-12-en-28-oic acid
-
competitive inhibition
3-oxo-urs-12-en-28-oic acid
noncompetitive inhibitor
3-oxoolean-12-en-28-oic acid
-
competitive inhibition
3-oxours-12-en-28-oic acid
-
competitive inhibition
3-[(benzyloxy)methyl]-1-cyanopyrrolidine
-
IC50: 0.00015 mM
3-[(E)-(4-[[4-([2-[([[3-cyclohexyl-N-(morpholin-4-ylcarbonyl)-L-alanyl]amino][(6-[(2Z)-2-[(2E,4E,6Z)-7-(1-ethyl-3,3-dimethyl-5-sulfo-2,3-dihydro-1H-indol-2-yl)hepta-2,4,6-trien-1-ylidene]-3,3-dimethyl-5-sulfo-2,3-dihydro-1H-indol-1-yl]hexanoyl)amino]acetyl)amino]ethyl]amino)-4-oxobutyl](methyl)amino]phenyl)diazenyl]-7-(diethylamino)-5-phenylphenazin-5-ium
-
3-[[(2S)-2-[([3-acetyl-4-[(methylsulfonyl)amino]phenyl]carbonyl)amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[(2S)-2-[[(4-[[(4-aminophenyl)sulfonyl]amino]phenyl)carbonyl]amino]-3-(1-methylcyclopentyl)propanoyl]amino]-1,4-anhydro-3,5,6-trideoxy-L-glycero-hex-2-ulose
-
-
3-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline
4-(2,5-dimethyl-1H-pyrrol-1-yl)-N'-(5-methyl-3-phenyl-1,2-oxazole-4-carbonyl)benzohydrazide
-
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
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
4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide
4-bromophenyl (1E,3S)-3-([N-[(benzyloxy)carbonyl]-L-phenylalanyl]amino)-5-methylhex-1-ene-1-sulfonate
i.e. KD-1
4-bromophenyl (S,E)-3-((S)-2-((((4-ethynylbenzyl)oxy)carbonyl)amino)-3-phenylpropanamido)-5-methylhex-1-ene-1-sulfonate
i.e. KDP-1, in vivo inhibition of cathepsin L. Inhibition of cathepsin L compared to other cathepsins, overview
4-[(1-acetylpiperidin-4-yl)methoxy]-2-cyano-N-methyl-6-[(spiro[3.5]non-7-ylmethyl)amino]pyrimidine-5-carboxamide
-
4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide
4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol
4-[4-(benzyloxy)phenyl]-3-([(4-methylphenyl)methyl]sulfanyl)-4,5-dihydro-1H-1,2,4-triazol-5-one
-
4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline
4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole)
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]benzoic acid
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
5,5'-dithiobis(2-nitrobenzoic acid)
5-bromo-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-2-carbonitrile
-
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole
6-(4-chlorobenzyl)-7-(2,2-dimethylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclooctylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(2-piperidin-1-ylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3,3-dimethylbutyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(3-cyclohexylpropyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(4,4-dimethylpentyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(3-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-(4-chlorobenzyl)-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P2 moieties
6-[[4-(1-acetyl-1,2,3,6-tetrahydropyridin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(1-acetylpiperidin-4-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(4-acetyl-1,4-diazepan-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)-3-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cycloheptylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclopentylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4-chlorophenyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
7-(2-cyclohexylethyl)-6-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(cyclohexylmethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-(phenoxymethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(phenylamino)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridin-2-yloxy)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[(pyridin-2-ylsulfanyl)methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
7-(2-cyclohexylethyl)-6-[[methyl(phenyl)amino]methyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
acetyl-Leu-Leu-Tyr-CHN2
-
-
acetyl-prolyl-leucyl-leucyl-leucinal
-
-
acetyl-prolyl-prolyl-leucyl-leucyl-leucinal
-
-
agathisflavone
noncompetitive inhibitor
alpha2 cysteine-proteinase inhibitor
-
-
-
Aprotinin
55.22% inhibition at 0.1 mM
Azodicarboxylic acid alpha-morpholide
-
-
benzamidine
17% inhibition at 5 mM
benzofuran-2-carboxylic acid ((S)-1-[3-oxo-1-(pyridine-2-sulfonyl)azepan-4-ylcarbamoyl]-2-naphthylen-2-yl)amide
-
-
benzofuran-2-carboxylic acid ((S)-1-[3-oxo-1-(pyridine-2-sulfonyl)azepan-4-ylcarbamoyl]-2-phenyl-ethyl)amide
-
-
benzophenone thiosemicarbazone
-
benzoylbenzophenone thiosemicarbazone
molecular docking in the active site
benzyl 1-cyano-3-pyrrolidinylcarbamate
-
IC50: 0.000054 mM
benzyl [(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxo-3-(1,1':4',1''-terphenyl-4-yl)propan-2-yl]carbamate
-
-
benzyl [(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-3-(2'-methylbiphenyl-4-yl)-1-oxopropan-2-yl]carbamate
-
-
benzyl [(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-3-(3'-methylbiphenyl-4-yl)-1-oxopropan-2-yl]carbamate
-
-
benzyl [(2S)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-3-(4'-methylbiphenyl-4-yl)-1-oxopropan-2-yl]carbamate
-
-
benzyl [(2S)-3-(3'-aminobiphenyl-4-yl)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]carbamate
-
-
benzyl [(2S)-3-(3'-chlorobiphenyl-4-yl)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]carbamate
-
-
benzyl [(2S)-3-(biphenyl-4-yl)-1-[[(2S)-1,6-diamino-1-oxohexan-2-yl]amino]-1-oxopropan-2-yl]carbamate
-
-
benzyloxycarbonyl-FF-fluoromethylketone
-
cathepsin L-specific inhibitor
benzyloxycarbonyl-iodophenylalanine-Ala-CHN2
-
-
benzyloxycarbonyl-iodotyrosine-Ala-CHN2
-
-
benzyloxycarbonyl-L-Phe-L-Phe-fluoromethylketone
benzyloxycarbonyl-Leu-homophenylalanine-CHN2
-
-
benzyloxycarbonyl-Leu-Leu-Phe-CHN2
-
-
benzyloxycarbonyl-Leu-Leu-Tyr-CHN2
-
-
benzyloxycarbonyl-Leu-Met-CHN2
-
-
benzyloxycarbonyl-Leu-Trp-CHN2
-
-
benzyloxycarbonyl-Leu-Tyr-CHN2
-
-
benzyloxycarbonyl-leucyl-leucyl-leucinal
-
-
Benzyloxycarbonyl-Phe-Ala-CHN2
-
-
benzyloxycarbonyl-Phe-Ala-CNH2
benzyloxycarbonyl-Phe-Arg-diazomethyl ketone
-
more than 99% inhibition at 0.1 mM
benzyloxycarbonyl-Phe-Phe fluoromethylketone
-
cell-permeable irreversible cathepsin inhibitor
Benzyloxycarbonyl-Phe-Phe-CHN2
benzyloxycarbonyl-Phe-Phe-fluoromethyl ketone
-
benzyloxycarbonyl-Phe-Phe-fluoromethylketone
-
-
benzyloxycarbonyl-Phe-Tyr-(tert-butyl)-diazomethylketone
benzyloxycarbonyl-Phe-Tyr-CHO
benzyloxycarbonyl-Phe-X-CHN2
-
-
benzyloxycarbonyl-PheTyr-[tert-butyl]-diazomethylketone
-
specific inhibitor
benzyloxycarbonyl-Tyr-Ala-CHN2
-
-
biphenyl-4-yl-acetylasparagine-D-Arg-Phe-Phe-NH2
-
biphenyl-4-yl-acetylcysteine-D-Arg-Abu-N-(2-phenylethyl)amide
-
biphenyl-4-yl-acetylcysteine-D-Arg-Arg-N-(2-phenylethyl)amide
-
biphenyl-4-yl-acetylcysteine-D-Arg-N-(2-phenylethyl)amide
-
biphenyl-4-yl-acetylcysteine-D-Arg-Phe-N-(2-phenylethyl)amide
-
biphenyl-4-yl-acetylcysteine-D-Arg-Phe-Phe-NH2
-
biphenyl-4-yl-acetylcysteine-D-Arg-Trp-N-(2-phenylethyl)amide
-
biphenyl-4-yl-acetylcysteine-D-Arg-Tyr-N-(2-phenylethyl)amide
-
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Leu-N-(2-phenylethyl)amide
-
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Met-N-(2-phenylethyl)amide
-
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-N-(2-phenylethyl)amide
the inhibitor shows a 310fold and 210fold selectivity for cathepsin L over cathepsin K and B, respectively
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-N-(3-phenylpropyl)amide
-
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-N-(benzyl)amide
-
biphenyl-4-yl-acetylmethylcysteine-D-Arg-Phe-Phe-NH2
-
biphenyl-4-yl-acetylmethylcysteine-D-Orn-Phe-N-(2-phenylethyl)amide
-
biphenyl-4-yl-acetylmethylcysteine-Gly-Phe-Phe-NH2
-
biphenyl-4-yl-acetylnorvaline-D-Arg-Phe-N-(2-phenylethyl)amide
-
biphenyl-4-yl-acetylserine-D-Arg-Phe-Phe-NH2
-
biphenylacetyl-(N6-biphenylacetyl)-Lys-D-Arg-Tyr-N-phenylethyl
-
biphenylacetyl-(N6-biphenylacetyl)Lys-D-Arg-Phe-N-phenylethyl
-
biphenylacetyl-MCys-D-Arg-Phe-N-phenylethyl
-
bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone
CA-074
i.e. N-(L-3-trans-propylcarbamoyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline, about 25% residual activity at 0.02 mM; i.e. N-(L-3-trans-propylcarbamoyl-oxirane-2-carbonyl)-L-isoleucyl-L-proline, about 75% residual activity at 0.02 mM
Ca2+
-
51% residual activity at 1 mM
CAA0225
-
i.e. (2S,3S)-oxirane-2,3-dicarboxylic acid 2-[((S)-1-benzylcarbamoyl-2-phenyl-ethyl)-amide]3-[[2-(4-hydroxy-phenyl)-ethyl]-amide], a cathepsin L-specific inhibitor
cathepsin K propeptide
-
-
-
cathepsin L inhibitor 1
-
cathepsin L inhibitor I
-
0.05 mM
cathepsin L inhibitor III
-
0.01 mM
cathepsin L propeptide
-
-
-
cathepsin S propeptide
-
-
-
chagasin mutant delta T31-T32
-
-
-
chagasin mutant P30A
-
-
-
chagasin mutant T31A
-
-
-
chagasin mutant T31A/T32A
-
-
-
chagasin mutant T31S
-
-
-
chagasin mutant T31V
-
-
-
chagasin mutant T31Y
-
-
-
chagasin mutant T32A
-
-
-
chagasin mutant T32S
-
-
-
chagasin mutant T32V
-
-
-
chagasin mutant T32Y
-
-
-
chagasin mutant W93A
-
-
-
Chloroquine
-
chloroquine inhibits the infection with live Nipah virus and Hendra virus at a concentration of 1 microM in vitro. The mechanism for the antiviral action likely is the inhibition of cathepsin L, which is essential for the processing of the viral fusion glycoprotein and the maturation of newly budding virions
CID 16725315
-
2% inhibition at 0.025 mM
CID 23631927
-
38% inhibition at 0.025 mM, sub-nanomolar slow-binding, reversible inhibitor of human cathepsin L with cathepsin L/B selectivity of above 700fold that blocks SARS-CoV and Ebola pseudotype virus entry in human cells
CLIK-181
cathepsin L-specific inhibitor
CLIK195
-
complete inhibition at 0.01 mM
cystatin alpha
-
0.05 mg/ml
-
diazinedicarboxylic acid bisdimethylamide
-
-
diazomethanes
-
irreversible inhibition of hydrolysis of leucine enkephalin
-
diethyl-cyanamide
-
IC50 is above 0.1 mM
EGTA
40.55% inhibition at 0.1 mM
endopin 2C
-
endopin 2C inactivaties cathepsin L by binding to the enzyme, after dissociation from cathepsin L its activity is recovered within 60 min
-
Fe2+
-
5% residual activity at 1 mM
Fe3+
-
complete inhibition at 1 mM
fragment p41 of major histocompatibility complex class II-associated invariant chain
-
glucose
-
high concentrations
iodoacetate
-
complete inhibition at 1 mM
isonicotinyl-leucyl-leucyl-leucinal
-
-
JPM-565
-
cathepsin L irreversible binding
JPM-OEt
-
cathepsin L irreversible binding
KAPR-acetyl-K-QLATKAARKSAPA
-
KAPRKQLAT-acetyl-K-AARKSAPA
-
KAPRKQLATKAAR-dimethyl-K-SAPA
-
L-1-tosyl-2-phenylethylchloromethylketone
-
-
L-3-carboxy-trans-2,3-epoxypropionyl-leucylamido-(3-methyl)butane
-
-
L-3-trans-propylcarbamoyloxirane-2-carbonyl-L-isoleucyl-L-proline
-
-
L-Phe-L-Arg-7-amido-4-methylcoumarin
-
the susceptibility of recombinant enzyme to substrate inhibition at 25°C is partially reversible, i.e., it is absent at 37°C and is displayed when the same enzyme sample is assayed again at 25°C
L-trans-epoxy-succinyl-leucylamido-(4-guanidino)-butane
-
complete inhibition at 0.1 mM
L-trans-epoxysuccinyl-leucylamido(3-methyl)butane
-
-
L-trans-epoxysuccinyl-leucylamido-(4-guanidino)butane
E-64
L-trans-epoxysuccinylleucylamido-(4-guanidino)butane
i.e. E-64, complete inhibition at 0.26 mM
LFLRL
-
0.05 mM, 78% inhibition
LFLTR-NH2
-
IC50: 0.0008 mM
LKFTF
-
0.05 mM, 24% inhibition; 0.05 mM, 32% inhibition
LKFTR
-
0.05 mM, 78% inhibition
LKLFF
-
0.05 mM, 42% inhibition
LKLFW
-
0.05 mM, 22% inhibition
LKLLW
-
0.05 mM, 75% inhibition
LLFLW
-
0.05 mM, 52% inhibition
LLFRW
-
0.05 mM, 52% inhibition
LLLLR
-
0.05 mM, 62% inhibition
LLLLW
-
0.05 mM, 37% inhibition
LLLRW
-
0.05 mM, 83% inhibition
LLLTB
-
0.05 mM, 58% inhibition
LLLTL
-
0.05 mM, 67% inhibition
LLLTR-NH2
-
IC50: 0.0005 mM
LLLTW
-
0.05 mM, 62% inhibition
LLYLW
-
0.05 mM, 47% inhibition
LLYTB
-
0.05 mM, 25% inhibition
LLYTR
-
0.05 mM, 62% inhibition
LLYTW
-
0.05 mM, 30% inhibition
low-MW cysteine proteinase inhibitor
-
-
-
LRFTF
-
0.05 mM, 25% inhibition
LRLLW
-
0.05 mM, 73% inhibition
LWFFW
-
0.05 mM, 61% inhibition
LWFRQ
-
0.05 mM, 20% inhibition
LWFRW
-
0.05 mM, 20% inhibition
LWLFL
-
0.05 mM, 73% inhibition
LWLFW
-
0.05 mM, 31% inhibition
LWLLW
-
0.05 mM, 52% inhibition
MENT
-
potent and very specific irreversible cathepsin L inhibitor
-
methyl (13alpha,17alpha,20S,24Z)-3-hydroxylanosta-7,24-dien-26-oate
-
competitive inhibition
methyl (3Z,13alpha,17alpha,20S,24Z)-3-(hydroxyimino)lanosta-7,24-dien-26-oate
-
competitive inhibition
methyl 5-acetyloxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
furanquinone from Paulownia tomentosa stem, inhibitory to both cathepsin L and cathepsin K
methyl 5-hydroxy-dinaphtho[1,2-2'3']furan-7,12-dione-6-carboxylate
-
furanquinone from Paulownia tomentosa stem, inhibitory to both cathepsin L and cathepsin K
methylphenylazoformate
-
-
Mg2+
-
66% residual activity at 1 mM
morpholinurea-leucyl-homophenyl-vinyl sulfone phenyl
moderate inhibitor
morpholinylsuccinyl-leucyl-leucyl-leucinal
-
-
N-(1-cyano-3-pyrrolidinyl)benzamide
-
IC50: 0.00175 mM
N-(1-cyano-3-pyrrolidinyl)benzenesulfonamide
-
IC50: 0.00008 mM
N-(1-cyano-3-pyrrolidinyl)[1,1'-biphenyl]-4-carboxamide
-
IC50: 0.00085 mM
N-(1-cyanopyrrolidin-3-yl)benzenesulfonamide
-
-
N-(2,6-dimethylbenzoyl)-L-phenylalanyl-L-lysinamide
-
-
N-(2-chloro-5-nitrobenzoyl)-L-phenylalanyl-L-lysinamide
-
-
N-(3-phenylpropanoyl)-L-phenylalanyl-L-lysinamide
-
-
N-(4-benzyl-1-methylpiperidin-4-yl)-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-(4-biphenylacetyl)-S-methylcysteine-(D)-Arg-Phe-beta-phenethylamide
-
also called Cat L inhibitor 7, specific inhibitor
N-(4-bromobenzoyl)-L-phenylalanyl-L-lysinamide
-
-
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)acetamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(4-[[2-cyano-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidin-6-yl]methoxy]phenyl)propanamide
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
N-(biphenyl-4-ylcarbonyl)-L-phenylalanyl-L-lysinamide
-
-
N-(cyclopent-1-en-1-ylcarbonyl)-L-phenylalanyl-L-lysinamide
-
-
N-(naphthalen-2-ylcarbonyl)-L-phenylalanyl-L-lysinamide
-
-
N-(pentafluorobenzoyl)-L-phenylalanyl-L-lysinamide
-
-
N-(piperidin-2-ylcarbonyl)-L-phenylalanyl-L-lysinamide
-
-
N-(pyridin-2-ylcarbonyl)-L-phenylalanyl-L-lysinamide
-
-
N-acetyl-Leu-Leumethional
inhibition of gelatinolytic activity
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)methoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[(1-methylpiperidin-4-yl)oxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-cyano-4-[2-(1-methylpiperidin-4-yl)ethoxy]-6-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-benzyl-2-[bis(3-bromophenyl)methylidene]hydrazinecarbothioamide
-
-
N-benzyloxycarbonyl-Phe-Phe-fluoromethylketone
-
-
N-benzyloxycarbonyl-phenylalanyl-phenylalanine-fluoromethyl ketone
an irreversible cathepsin inhibitor
N-ethylmaleimide
10 mM, less than 10% residual activity
N-[(1-cyano-2-pyrrolidinyl)methyl]benzamide
-
IC50: 0.023 mM
N-[(1-cyano-2-pyrrolidinyl)methyl]benzenesulfonamide
-
IC50: 0.0115 mM
N-[(1-cyano-3-azetidinyl)methyl]benzamide
-
IC50: 0.00065 mM
N-[(1-cyano-3-azetidinyl)methyl]benzenesulfonamide
-
IC50: 0.00005 mM
N-[(1-cyano-3-azetidinyl)methyl]cyclohexanecarboxamide
-
IC50: 0.000006 mM
N-[(1-cyano-3-pyrrolidinyl)methyl]benzenesulfonamide
-
IC50: 0.00035 mM
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1R)-1-benzyl-2-pyrrolidin-1-ylpropyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(1S)-1-benzyl-2-pyrrolidin-1-ylethyl]-2-cyano-4-[(spiro[2.5]oct-6-ylmethyl)amino]pyrimidine-5-carboxamide
-
N-[(2R)-2-[(2-amino-2-oxoethyl)amino]-2-[[(benzyloxy)carbonyl]amino]acetyl]-L-phenylalanyl-L-lysinamide
-
-
N-[(2R)-2-[(3-aminopropyl)amino]-2-[[(benzyloxy)carbonyl]amino]acetyl]-L-phenylalanyl-L-lysinamide
-
-
N-[(2R)-2-[[(benzyloxy)carbonyl]amino]-2-(3a,7a-dihydro-1H-indol-3-ylamino)acetyl]-L-phenylalanyl-L-lysinamide
-
-
N-[(2R)-2-[[(benzyloxy)carbonyl]amino]-2-(propan-2-ylamino)acetyl]-L-phenylalanyl-L-lysinamide
-
-
N-[(2R)-2-[[(benzyloxy)carbonyl]amino]-2-[(2-carbamimidamidoethyl)amino]acetyl]-L-phenylalanyl-L-lysinamide
-
-
N-[(2S)-1-(1H-indol-3-yl)-3-oxopropan-2-yl]-N2-(naphthalen-1-ylsulfonyl)-L-isoleucinamide
-
-
N-[(2S)-1-(3-chlorophenyl)-3-[(cyanomethyl)amino]but-3-en-2-yl]benzamide
-
-
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-1,3-dimethyl-1H-pyrazole-4-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-1,3-dimethyl-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-1-methyl-3-(propan-2-yl)-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-2,3-dimethylbenzamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-2,4-dimethyl-1,3-thiazole-5-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-2,5-dimethyl-1,3-oxazole-4-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-2,5-dimethylbenzamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-2,5-dimethylthiophene-3-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-2-methylbenzamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-3,5-dimethylbenzamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-3,7-dimethylnaphthalene-1-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-3-ethyl-1-methyl-1H-pyrazole-5-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-3-methylbenzamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-4-methylbenzamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]-5,6,7,8-tetrahydronaphthalene-1-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]benzamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]cycloheptanecarboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]cyclohex-1-ene-1-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]cyclohexanecarboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]naphthalene-1-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-3-(3-chlorophenyl)-1-[(cyanomethyl)amino]-1-oxopropan-2-yl]quinoline-4-carboxamide
-
pH and temperature not specified in the publication
N-[(2S)-4-methyl-1-oxo-1-[[(4S)-3-oxo-1-(pyridin-2-ylsulfonyl)azepan-4-yl]amino]pentan-2-yl]-1-benzofuran-2-carboxamide
-
-
N-[(4'-carboxy-2,2'-bipyridin-4-yl)carbonyl]-L-phenylalanyl-L-lysinamide
-
-
N-[(6-aminopyridin-3-yl)carbonyl]-L-phenylalanyl-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-3-(1H-indazol-1-yl)-L-alanyl-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-3-(1H-indol-1-yl)-L-alanyl-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-4-(thiophen-2-yl)-L-phenylalanyl-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-L-leucyl-N-[(3S)-7-amino-1-[(2,6-dimethylbenzoyl)oxy]-2-oxoheptan-3-yl]-L-phenylalaninamide
-
irreversible inhibitor
N-[(benzyloxy)carbonyl]-L-phenylalanyl-3-(1H-imidazol-1-yl)-L-alaninamide
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-4-amino-L-phenylalaninamide
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-6-hydroxy-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-L-alaninamide
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-L-argininamide
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-L-leucinamide
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-L-methioninamide
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-L-ornithinamide
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-L-valinamide
-
-
N-[(benzyloxy)carbonyl]-L-phenylalanyl-N6-methyl-L-lysinamide
-
-
N-[(benzyloxy)carbonyl]-L-tryptophyl-N-[(3S)-7-amino-1-[(2,6-dimethylbenzoyl)oxy]-2-oxoheptan-3-yl]-L-phenylalaninamide
-
irreversible inhibitor
N-[(benzyloxy)carbonyl]-L-tyrosyl-L-lysinamide
-
-
N-[3-(4-hydroxyphenyl)propanoyl]-L-phenylalanyl-L-lysinamide
-
-
N-[3-(acetyloxy)benzoyl]-L-phenylalanyl-L-lysinamide
-
-
N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide
N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide
N-[4-(acetyloxy)benzoyl]-L-phenylalanyl-L-lysinamide
-
-
N-[4-(dimethylamino)benzoyl]-L-phenylalanyl-L-lysinamide
-
-
N-[4-(trifluoromethyl)benzoyl]-L-phenylalanyl-L-lysinamide
-
-
N-[4-[(1E)-3-(2-hydroxyphenyl)-3-oxoprop-1-en-1-yl]phenyl]acetamide
32% inhibition of FhCL3; 6% inhibition of FhCL1
N-[4-[(1E)-3-oxo-3-phenylprop-1-en-1-yl]phenyl]acetamide
12% inhibition of FhCL3; 14% inhibition of FhCL1
N-[4-[(1Z)-3-(2-hydroxyphenyl)-3-oxoprop-1-en-1-yl]phenyl]acetamide
13% inhibition of FhCL3
N-[6-[(6-[3,3-dimethyl-2-[(1E,3E,5E)-5-(1,3,3-trimethyl-1,3-dihydro-2H-indol-2-ylidene)penta-1,3-dien-1-yl]-3H-indolium-1-yl]hexanoyl)amino]hexanoyl]-L-histidyl-L-threonyl-N-[(2R)-1-(benzylsulfanyl)-4-[(2,6-dimethylbenzoyl)oxy]-3-oxobutan-2-yl]-2,3,4,5,6-pentafluoro-L-phenylalaninamide
-
N2-acetyl-L-arginyl-L-lysyl-L-leucyl-L-leucyl-L-tryptophanamide
-
potent inhibitor
N2-[(benzyloxy)carbonyl]-L-arginyl-N-[(3S)-7-amino-1-[(2,6-dimethylbenzoyl)oxy]-2-oxoheptan-3-yl]-L-phenylalaninamide
-
irreversible inhibitor
N2-[(benzyloxy)carbonyl]-L-lysyl-N-[4-([[(5-methyl-7-oxo-7,8-dihydronaphthalen-2-yl)carbamoyl]oxy]methyl)phenyl]-L-lysinamide
-
N2-[(benzyloxy)carbonyl]-L-ornithyl-N-[(3S)-7-amino-1-[(2,6-dimethylbenzoyl)oxy]-2-oxoheptan-3-yl]-L-phenylalaninamide
-
irreversible inhibitor
N2-[(benzyloxy)carbonyl]-N-[(3S)-1-cyanopyrrolidin-3-yl]-L-leucinamide
-
-
Nalpha-[(3-tert-butyl-1-methyl-1H-pyrazol-5-yl)carbonyl]-3-chloro-N-(cyanomethyl)-L-phenylalaninamide
-
pH and temperature not specified in the publication
Nalpha-[(3-tert-butyl-1-methyl-1H-pyrazol-5-yl)carbonyl]-N-(cyanomethyl)-3-methyl-L-phenylalaninamide
-
pH and temperature not specified in the publication
Nalpha-[(benzyloxy)carbonyl]-N-[(1R)-1,2-diamino-2-oxoethyl]-L-phenylalaninamide
-
-
Nalpha-[(benzyloxy)carbonyl]-N-[(3S)-7-[(6-[(2Z)-3,3-dimethyl-5-sulfo-2-[(2E,4E)-5-(1,3,3-trimethyl-5-sulfo-2,3-dihydro-1H-indol-2-yl)penta-2,4-dien-1-ylidene]-2,3-dihydro-1H-indol-1-yl]hexanoyl)amino]-2-oxo-1-(2,3,5,6-tetrafluoro-4-[[2-([[1-(2-[(3E)-3-(5-sulfo-2,3-dihydro-1H-indolium-1-ylidene)-6-(5-sulfo-2,3-dihydro-1H-indol-1-yl)-3H-xanthen-9-yl]benzene-1-sulfonyl)piperidin-4-yl]carbonyl]amino)ethyl]carbamoyl]phenoxy)heptan-3-yl]-L-phenylalaninamide
-
naphthalene-2-carboxylic acid ((S)-2-naphthalen-2-yl-1-[(S)-3-oxo-1-(pyridine-2-sulfonyl)azepan-4-ylcarbamoyl]ethyl)amide
-
-
naphthoic-1-carboxylic acid ((S)-1-[3-oxo-1-(pyridine-2-sulfonyl)azepan-4-ylcarbamoyl]-3-methyl-butyl)amide
-
-
Ni2+
-
complete inhibition at 1 mM
nicotinyl-leucyl-leucyl-leucinal
-
-
OC-1DELTAD86
-
0.002 mM
-
ortho-aminobenzoic acid-LFEKQ-N-[2,4-dinitrophenyl]ethylenediamine
-
-
ortho-aminobenzoic acid-VLFEKKQ-N-[2,4-dinitrophenyl]ethylenediamine
-
-
ortho-aminobenzoic acid-VLFEKKVYLQ-N-[2,4-dinitrophenyl]ethylenediamine
-
efficient cathepsin L inhibitor
ortho-aminobenzoic acid-VLFEKQ-N-[2,4-dinitrophenyl]ethylenediamine
-
-
p-hydroxymercuribenzoate
-
-
p41-fragment-mouse
64 residues present in the p41 form of the murine major histocompatibility complex II (MHCII)-associated invariant chain
-
P41icf
-
synthesis and NMR structure of the potent inhibitor
-
pepstatin A
21.54% inhibition at 0.1 mM
Phe-Tyr-(OBut)-COCHO
potent, reversible, synthetic peptidyl inhibitor of cathepsin L
Phe-Tyr-(tert-Bu)-diazomethylketone
irreversible inhibitor that can inactivate cathepsin L at micromolar concentrations
Phenylbutazone
-
noncompetitive inhibitor
phenylmethanesulfonyl fluoride
-
-
phenylmethylsulfonyl fluoride
Protein C inhibitor
-
inhibits cathepsin L with an inhibition rate (k2) of 30000 0 M-1 s-1
-
quinoline-2-carboxylic acid ((S)-1-[3-oxo-1-(pyridine-2-sulfonyl)azepan-4-ylcarbamoyl]-3-methyl-butyl)amide
-
-
quinoline-8-carboxylic acid ((S)-1-[3-oxo-1-(pyridine-2-sulfonyl)azepan-4-ylcarbamoyl]-3-methyl-butyl)amide
-
-
RFLRW
-
0.05 mM, 21% inhibition
RFLYR
-
0.05 mM, 64% inhibition
RKLFL
-
0.05 mM, 79% inhibition
RKLLW-NH2
-
IC50: 0.0006 mM
RKLWD-NH2
-
IC50: 0.014 mM
RKLWF
-
0.05 mM, 52% inhibition
RKLWL-NH2
-
IC50: 0.0008 mM
RKLWV
-
0.05 mM, 41% inhibition
RLLLW
-
0.05 mM, 75% inhibition
RLLYW
-
0.05 mM, 29% inhibition
RRFYV
-
0.05 mM, 24% inhibition
RRLTW
-
0.05 mM, 38% inhibition
RRYLB
-
0.05 mM, 33% inhibition
RWLTL
-
0.05 mM, 61% inhibition
RWLYL
-
0.05 mM, 65% inhibition
S-(2-oxo-1-phenylpyrrolidin-3-yl) 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
-
-
S-[2-(3,4-dihydroquinolin-1(2H)-yl)-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
-
-
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-phenylpropanoyl]hydrazinecarbothioate
-
-
salicylic acid
-
and its m-analogs and p-analogs
SDS
6.53% residual activity at 0.05% (w/v)
serpin B3
-
about 35% inhibition at 7.5 nM, the presence of heparin accelerates inhibition of cathepsin L by serpin B3 (4.1fold increase in rate of inhibition)
-
serpin B4
-
about 70% inhibition at 100 nM, the presence of 50 nM heparin accelerates inhibition of cathepsin L by serpin B4 (4.1fold increase in rate of inhibition)
-
soluble type I collagen
inhibitory against cathepsin L, Ki is 0.36 mg/ml, collagen is also a substrate for the enzyme
-
Soybean trypsin inhibitor
-
63.12% residual activity at 0.05 mg/ml
-
Stefin B
a potent cathepsin L inhibitor, colorectal carcinoma cells reveal only very faint amounts of immunolabeled stefin B within their nuclei, while it is prominently present within the cytoplasm of Caco-2 and SW-620 cells, and mostly associated with the cytoplasmic face of vesicles in HCT-116 cells
-
tert-butyloxycarbonyl-Lys(epsilon-9-fluorenylmethoxycarbonyl)-Leu-Tyr-CHN2
-
-
tert-butyloxycarbonyl-Lys-Leu-Tyr-CHN2
-
-
tert-butyloxycarbonyl-Val-Lys(epsilon-benzyloxycarbonyl)-Leu-Tyr-CHN2
-
-
testican-1
-
strong competitive inhibitor, inhibition is independent of its chondroitin sulfate chains and is effective at both pH 5.5 and pH 7.2, does not inhibit the structurally related lysosomal cysteine protease cathepsin B
-
tetrahydrorobustaflavone
uncompetitive inhibitor
Tg1 domain of testican-1
-
-
-
thyroglobulin type-1 domain
-
-
-
TLCK
10 mM, less than 10% residual activity
tosyl phenylalanyl chloromethylketone
-
66.63% residual activity at 0.1 mg/ml
toxostatin
-
endogenous inhibitor, acts both on cathepsin L and cathepsin B in the nanomolar range
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
YFLLR
-
0.05 mM, 30% inhibition
YFLTF
-
0.05 mM, 29% inhibition
YKLLR
-
0.05 mM, 72% inhibition
YLLFW
-
0.05 mM, 37% inhibition
YLYLF
-
0.05 mM, 40% inhibition
YWFTF
-
0.05 mM, 43% inhibition
YWLLR
-
0.05 mM, 73% inhibition
YWYYL
-
0.05 mM, 20% inhibition
YYLLR
-
0.05 mM, 56% inhibition
Z-Phe-Phe-CH2F
-
i.e. inhibitor I, blocks sea urchin embryogenesis. Complete arrest of cell division is obtained when the embryos are incubated with 100 microM of inhibitor I
Z-Phe-Tyr-CHO
-
specifically inhibits cathepsin L
(2S,3S)-oxirane-2,3-dicarboxylic acid 2-[((S)-1-benzylcarbamoyl-2-phenyl-ethyl)-amide] 3-[[2-(4-hydroxy-phenyl)-ethyl]-amide]
-
i.e. CAA0225. Significantly inhibits degradation of long-lived proteins in HeLa and Huh-7 cells cultured under nutrient-deprived conditions. CAA0225 effectively inhibits degradation of microtubule-associated protein IA/IB light chain 3-II and gamma-aminobutyric acid (A) receptor-associated protein
(2S,3S)-oxirane-2,3-dicarboxylic acid 2-[((S)-1-benzylcarbamoyl-2-phenyl-ethyl)-amide] 3-[[2-(4-hydroxy-phenyl)-ethyl]-amide]
-
i.e. CAA0225. IC50 value for rat liver cathepsin B above 1 microM
(2S,3S)-oxirane-2,3-dicarboxylic acid 2-[((S)-1-benzylcarbamoyl-2-phenyl-ethyl)-amide] 3-[[2-(4-hydroxy-phenyl)-ethyl]-amide]
-
specific inhibitor, CAA0225, more than 99% inhibition at 0.1 mM
(N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide)
-
(N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide)
-
(N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide)
-
1,10-phenanthroline
-
-
1,10-phenanthroline
36.6% inhibition at 0.1 mM
1-naphthalenesulfonyl-Ile-Trp-aldehyde
-
cathepsin L inhibitor
1-naphthalenesulfonyl-Ile-Trp-aldehyde
-
selective intra- and extracellular cathepsin L inhibitor
2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol
-
2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol
-
2,6-dimethoxy-4-[4-(4-phenoxyphenyl)-5-phenyl-1H-imidazol-2-yl]phenol
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
-
2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
-
2,6-dimethoxy-4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
-
2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
-
2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
-
2-(1,3-benzodioxol-5-yl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
-
2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
-
2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
-
2-(3,4-dimethoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
-
2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
-
2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
-
2-(4-methoxyphenyl)-4-[8-[2-(4-methoxyphenyl)-4-phenyl-1H-imidazol-5-yl]dibenzo[b,d]furan-2-yl]-5-phenyl-1H-imidazole
-
2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
-
2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
-
2-(4-methoxyphenyl)-5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazole
-
2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide
-
2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide
-
2-(acetylamino)-N-[4-(6-[[2-(acetylamino)benzoyl]amino]-1H-benzimidazol-2-yl)phenyl]benzamide
-
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
-
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
-
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
-
4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline
-
4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline
-
4,4'-[methanediylbis(1H-benzimidazole-5,2-diyl)]dianiline
has H-bond and steric interactions with Cys 25 of rhodesain's catalytic triad as well as residues Leu67 and Met68 while its dianiline motifs have steric interactions with Gly64 and Leu160
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
-
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
-
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
-
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
-
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
-
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
-
4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide
-
4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide
-
4-amino-N-(4-[6-[(4-aminobenzoyl)amino]-1H-benzimidazol-2-yl]phenyl)benzamide
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide
-
4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide
-
4-[(E)-benzylideneamino]-N-[4-[6-([4-[(E)-benzylideneamino]benzoyl]amino)-1H-benzimidazol-2-yl]phenyl]benzamide
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol
-
4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol
-
4-[4-(5,5-dioxidodibenzo[b,d]thiophen-2-yl)-5-phenyl-1H-imidazol-2-yl]-2,6-dimethoxyphenol
-
4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline
-
4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline
-
4-[5-(4-[[2-(4-aminophenyl)-1H-benzimidazol-6-yl]oxy]phenoxy)-1H-benzimidazol-2-yl]aniline
-
4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
-
4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
-
4-[5-phenyl-4-[4-(phenylsulfanyl)phenyl]-1H-imidazol-2-yl]phenol
-
4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole)
-
4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole)
-
4-[8-(2,4-diphenyl-1H-imidazol-5-yl)dibenzo[b,d]furan-2-yl]-2,5-diphenyl-1H-imidazole)
-
5,5'-dithiobis(2-nitrobenzoic acid)
-
-
5,5'-dithiobis(2-nitrobenzoic acid)
-
-
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole
-
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole
-
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(2,4,5-trimethoxyphenyl)-1H-imidazole
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole
-
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole
-
5-phenyl-4-[4-(phenylsulfanyl)phenyl]-2-(3,4,5-trimethoxyphenyl)-1H-imidazole
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)-2-fluorophenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
pyrrolopyrimidine inhibitor by modification of the P3 moieties
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-(2-cyclohexylethyl)-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
6-[[4-(4-acetylpiperazin-1-yl)phenoxy]methyl]-7-[2-(4,4-difluorocyclohexyl)ethyl]-7H-pyrrolo[2,3-d]pyrimidine-2-carbonitrile
-
-
antipain
-
1 mM, complete loss of activity
antipain
97.26% inhibition at 0.1 mM
benzyloxycarbonyl-L-Phe-L-Phe-fluoromethylketone
-
-
benzyloxycarbonyl-L-Phe-L-Phe-fluoromethylketone
-
irreversible and selective inhibitor of cathepsin L
benzyloxycarbonyl-L-Phe-L-Phe-fluoromethylketone
-
-
benzyloxycarbonyl-Phe-Ala-CNH2
-
-
benzyloxycarbonyl-Phe-Ala-CNH2
-
-
benzyloxycarbonyl-Phe-Ala-CNH2
-
-
benzyloxycarbonyl-Phe-Ala-CNH2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
Benzyloxycarbonyl-Phe-Phe-CHN2
-
-
benzyloxycarbonyl-Phe-Tyr-(tert-butyl)-diazomethylketone
-
irreversible cathepsin L inhibitor
benzyloxycarbonyl-Phe-Tyr-(tert-butyl)-diazomethylketone
-
-
benzyloxycarbonyl-Phe-Tyr-CHO
-
-
benzyloxycarbonyl-Phe-Tyr-CHO
-
-
benzyloxycarbonyl-Phe-Tyr-CHO
-
-
benzyloxycarbonyl-Phe-Tyr-CHO
-
-
bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone
-
bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone
-
bis[2-(4-aminophenyl)-1H-benzimidazol-5-yl]methanone
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
CA-074Me
-
in cells transfected with Nipah virus fusion protein, treatment with inhibitor CA-074ME almost completely prevents proteolytic processing of F0 into F1 and F2
CA-074Me
-
cathepsin L activity is suppressed by 0.04 mM CA-074Me in NIH-3T3 cells
chymostatin
-
-
chymostatin
-
93% inhibition at 5 mM
chymostatin
-
32.24% residual activity at 0.2 mM
chymostatin
95% inhibition at 0.1 mM
chymostatin
21.29% inhibition at 0.1 mM
CLIK-148
-
CLIK-148
cathepsin L-specific inhibitor
CLIK-148
treatment of AtT-20 cells results in reduced production of adrenocorticotropic hormone and accumulation of proopiomelanocortin
CLIK-148
-
specific cathepsin L inhibitor
CLIK-148
-
specific inhibitor of cathepsin L
CLIK148
0.1 mM
CLIK148
cathepsin L-specific inhibitor
CLIK148
-
complete inhibition at 0.01 mM
CLIK148
-
cathepsin L-specific inhibitor
CLIK148
-
cathepsin L-specific inhibitor, CLIK148 attenuates Eco-MLV infection in NIH3T3 cells
CLIK148
-
cathepsin L-specific inhibitor
Co2+
-
complete inhibition at 1 mM
Co2+
8.01% residual activity at 5 mM
Co2+
58.88% residual activity at 5 mM
Cu2+
-
1 mM, 19% residual activity
Cu2+
-
complete inhibition at 1 mM
Cu2+
complete inhibition at 5 mM
CuCl2
-
-
Cys
-
-
cystatin
-
from chicken, activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
-
cystatin
-
important role of Gly4 in the binding to the enzyme
-
cystatin A
-
-
-
cystatin B
-
-
-
cystatin B
-
cystatin B (stefin B) plays an important role in regulating the proteolytic activity of cathepsin L in the nucleus by protecting the CUX1 transcription factor and probably other substrates from proteolytic cleavage by cathepsin L
-
cystatin C
-
-
-
cystatin D
-
-
-
cystatin F
-
-
-
E-64
complete inhibition
E-64
-
almost complete inhibition at 0.01 mM
E-64
-
i.e. L-trans-epoxysuccinyl-leucylamide-(4-guanido)-butane, 24.76% residual activity at 1 mg/ml
E-64
98% inhibition at 0.01 mM
E-64
-
activity with benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin
E-64
-
irreversible inhibitor
E-64
-
broad-spectrum cathepsin inhibitor, cathepsin L irreversible binding
E-64
-
i.e. 1-[N-[(L-3-trans-carboxyoxirane-2-carbonyl)-L-leucyl]amino]-4-guanidinobutane
E-64
a broad-spectrum cysteine peptidase inhibitor
E-64
a pan cysteine cathepsin inhibitor
E-64
-
complete inhibition at 0.1 mM
E-64
i.e. transepoxysuccinyl-L-leucyl-amido(4-guanidino) butane, 60.1% inhibition at 0.5 mM
E-64
-
i.e. L-trans-epoxy-succinyl-leucylamido-(4-guanidino)-butane
E-64
i.e. trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane; i.e. trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
E-64
99.7% inhibition at 0.01 mM
E-64d
-
in cells transfected with Nipah virus fusion protein, treatment with inhibitor E-64d almost completely prevents proteolytic processing of F0 into F1 and F2
E64
0.1 mM, complete inhibition
E64
inhibition of gelatinolytic activity
EDTA
5 mM, 81% residual activity
EDTA
-
98% residual activity at 2 mM
EDTA
10.81% inhibition at 0.1 mM
endopin 2
-
endogenous protease inhibitor. High level of co-localization with enkephalin and NPY neuropeptides present in secretory vesicles of adrenal medullary chriomaffin cells in primary culture. Expression in brain, pituitary, adrenal medulla, and other neuroendocrine tissues
-
endopin 2
-
enodgenous inhibitor, present in pituitary gland
-
Ep-460
-
-
Ep-475
-
-
Ep-475
-
cathepsin L irreversible binding
fragment p41 of major histocompatibility complex class II-associated invariant chain
inhibitory to human cathepsin V, cathepsin L, cathepsin K, cathepsin F with Ki values in the low nanomolar range. Ki values are sufficiently low to ensure complex formation at physiological concentrations. Regulation of the proteolytic activity of most of the cysteine cathepsins by the p41 fragment is an important and widespread control mechanism of antigen presentation
-
fragment p41 of major histocompatibility complex class II-associated invariant chain
inhibitory to human cathepsin V, cathepsin L, cathepsin K, cathepsin F with Ki values in the low nanomolar range. Ki values are sufficiently low to ensure complex formation at physiological concentrations. Regulation of the proteolytic activity of most of the cysteine cathepsins by the p41 fragment is an important and widespread control mechanism of antigen presentation
-
Hg2+
-
-
Hg2+
37.32% residual activity at 1 mM
Hg2+
19.61% residual activity at 5 mM
iodoacetamide
complete inhibition
iodoacetic acid
-
1 mM, complete loss of activity
iodoacetic acid
10 mM, 15% residual activity
leupeptin
-
1 mM, 31% residual activity
leupeptin
0.1 mM, less than 10% residual activity
leupeptin
strong inhibition
leupeptin
-
about 95% inhibition at 0.1 mM
leupeptin
-
11.06% residual activity at 0.001 mg/ml
leupeptin
-
complete inhibition at 0.1 mM
leupeptin
98% inhibition at 0.1 mM
leupeptin
inhibition of gelatinolytic activity and of autolcleavage of cathepsin L
leupeptin
95.85% inhibition at 0.1 mM
leupeptin
-
reversible inhibition of hydrolysis of leucine enkephalin
leupeptin
-
pseudo-irreversible inhibitor
MDL28170
-
-
Mn2+
-
65% residual activity at 1 mM
N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide
-
N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide
-
N-[4-(1H-benzimidazol-2-yl)phenyl]-2,2-diphenylacetamide
the compound shows significant inhibitory activity against rhodesain, but displays poor antitrypanosomal activity at 0.020 mM
N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide
-
N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide
-
N-[4-(5-benzoyl-1H-benzimidazol-2-yl)phenyl]-2-chlorobenzamide
-
NEM
40.84% inhibition at 0.1 mM
p-21s
-
c-Ha-ras gene product
-
p-21s
-
c-Ha-ras proteins produced by Escherichia coli potent inhibitor
-
p41-fragment-human
64 residues present in the p41 form of the human major histocompatibility complex II (MHCII)-associated invariant chain
-
p41-fragment-human
64 residues present in the p41 form of the human major histocompatibility complex II (MHCII)-associated invariant chain
-
PCMB
-
-
pefabloc
-
about 30% inhibition at 1 mM
pefabloc
-
78.43% residual activity at 2 mg/ml
pepstatin
0.01 mM, 90% residual activity
pepstatin
-
58.06% residual activity at 0.001 mg/ml
phenylmethylsulfonyl fluoride
10 mM, less than 10% residual activity
phenylmethylsulfonyl fluoride
10.6% inhibition at 0.1 mM
PMSF
low inhibition
PMSF
37.5% inhibition at 5 mM
quercetin
15% inhibition of FhCL1; 8% inhibition of FhCL3
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
-
-
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
-
slow binding and slowly reversible inhibitor. 7- to 151fold greater selectivity towards cathepsin L then papain and cathepsins B, K, V, and S with no activity against cathepsin G. Inhibitor lacks toxicitiy in human aortic endothelial cells and inhibits in vitro propagation of Plasmodium falciparum with an IC50 value of 15.4 microM and of Leishmania major with an IC50 value of 12.5 microM
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
-
CID16725315, slowly reversible inhibition
S-[2-[(2-ethylphenyl)amino]-2-oxoethyl] 2-[(2S)-2-[(tert-butoxycarbonyl)amino]-3-(1H-indol-3-yl)propanoyl]hydrazinecarbothioate
-
-
tosyl-Lys-CH2Cl
-
-
tosyl-Phe-CH2Cl
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
95% inhibition at 0.01 mM
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
i.e. E-64, irreversible
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
i.e. E-64, in vivo, the inhibitor is transported to the liver cytosol in the free form in the blood and permeated into the lysosomes, where it binds to, and inactivates the enzyme
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane
-
-
Zn2+
-
1 mM, complete loss of activity
Zn2+
-
10% residual activity at 1 mM
Zn2+
14.75% residual activity at 5 mM
additional information
-
the enzyme is inhibited by cysteine proteases inhibitors
-
additional information
no inhibition by EDTA
-
additional information
-
no inhibition by EDTA
-
additional information
no inhibition by EDTA, AEBSF, approtinin, and pepstatin A
-
additional information
-
no inhibition by EDTA, AEBSF, approtinin, and pepstatin A
-
additional information
-
not inhibited by aprotinin and benzamidine
-
additional information
identification of chalcones as Fasciola hepatica cathepsin L inhibitors using a comprehensive experimental and computational approach, library screening, overview. No inhibition of cathepsin L1 by (2E)-1-(2-hydroxyphenyl)-3-[4-(methylsulfanyl)phenyl]prop-2-en-1-one, N-[4-[(1E)-3-(2-hydroxyphenyl)-3-oxoprop-1-en-1-yl]phenyl]acetamide, and 2-(4-chlorophenyl)-4H-chromen-4-one; identification of chalcones as Fasciola hepatica cathepsin L inhibitors using a comprehensive experimental and computational approach, library screening, overview. No inhibition of cathepsin L3 by (2E)-1-(2-hydroxyphenyl)-3-phenylprop-2-en-1-one, (2E)-1-(2-hydroxyphenyl)-3-(pyridin-2-yl)prop-2-en-1-one, and (2Z)-1-(2-hydroxyphenyl)-3-(pyridin-2-yl)prop-2-en-1-one; not inhibitory: (2E)-1-(2-hydroxyphenyl)-3-[4-(methylsulfanyl)phenyl]prop-2-en-1-one; not inhibitory: N-[4-[(1E)-3-(2-hydroxyphenyl)-3-oxoprop-1-en-1-yl]phenyl]acetamide
-
additional information
identification of chalcones as Fasciola hepatica cathepsin L inhibitors using a comprehensive experimental and computational approach, library screening, overview. No inhibition of cathepsin L1 by (2E)-1-(2-hydroxyphenyl)-3-[4-(methylsulfanyl)phenyl]prop-2-en-1-one, N-[4-[(1E)-3-(2-hydroxyphenyl)-3-oxoprop-1-en-1-yl]phenyl]acetamide, and 2-(4-chlorophenyl)-4H-chromen-4-one; identification of chalcones as Fasciola hepatica cathepsin L inhibitors using a comprehensive experimental and computational approach, library screening, overview. No inhibition of cathepsin L3 by (2E)-1-(2-hydroxyphenyl)-3-phenylprop-2-en-1-one, (2E)-1-(2-hydroxyphenyl)-3-(pyridin-2-yl)prop-2-en-1-one, and (2Z)-1-(2-hydroxyphenyl)-3-(pyridin-2-yl)prop-2-en-1-one; not inhibitory: (2E)-1-(2-hydroxyphenyl)-3-[4-(methylsulfanyl)phenyl]prop-2-en-1-one; not inhibitory: N-[4-[(1E)-3-(2-hydroxyphenyl)-3-oxoprop-1-en-1-yl]phenyl]acetamide
-
additional information
-
identification of chalcones as Fasciola hepatica cathepsin L inhibitors using a comprehensive experimental and computational approach, library screening, overview. No inhibition of cathepsin L1 by (2E)-1-(2-hydroxyphenyl)-3-[4-(methylsulfanyl)phenyl]prop-2-en-1-one, N-[4-[(1E)-3-(2-hydroxyphenyl)-3-oxoprop-1-en-1-yl]phenyl]acetamide, and 2-(4-chlorophenyl)-4H-chromen-4-one; identification of chalcones as Fasciola hepatica cathepsin L inhibitors using a comprehensive experimental and computational approach, library screening, overview. No inhibition of cathepsin L3 by (2E)-1-(2-hydroxyphenyl)-3-phenylprop-2-en-1-one, (2E)-1-(2-hydroxyphenyl)-3-(pyridin-2-yl)prop-2-en-1-one, and (2Z)-1-(2-hydroxyphenyl)-3-(pyridin-2-yl)prop-2-en-1-one; not inhibitory: (2E)-1-(2-hydroxyphenyl)-3-[4-(methylsulfanyl)phenyl]prop-2-en-1-one; not inhibitory: N-[4-[(1E)-3-(2-hydroxyphenyl)-3-oxoprop-1-en-1-yl]phenyl]acetamide
-
additional information
structure-based design of enzyme inhibitors through a computational study that combined virtual screening, molecular dynamics simulations, and binding free energy calculations. Docking protocol validation is carried out through the non-covalent re-docking of nitrile ((2S,4R)-1-[1-(4-chlorophenyl) cyclopropyl] carbonyl-4-(2-chlorophenyl) sulfonyl-N-[1-(iminomethyl)cyclopropyl] pyrrolidine-2-carboxamide) inhibitor into the active site of this protease, three-dimensional structure determination using the crystal structure of proFhCL1 C25G (PDB ID 2O6X) as a template
-
additional information
-
structure-based design of enzyme inhibitors through a computational study that combined virtual screening, molecular dynamics simulations, and binding free energy calculations. Docking protocol validation is carried out through the non-covalent re-docking of nitrile ((2S,4R)-1-[1-(4-chlorophenyl) cyclopropyl] carbonyl-4-(2-chlorophenyl) sulfonyl-N-[1-(iminomethyl)cyclopropyl] pyrrolidine-2-carboxamide) inhibitor into the active site of this protease, three-dimensional structure determination using the crystal structure of proFhCL1 C25G (PDB ID 2O6X) as a template
-
additional information
-
not inhibited by CA074Me
-
additional information
-
not inhibited by EDTA
-
additional information
-
MHC class II-associated invariant chain fragment from human kidney that has inhibitory effect on the enzyme
-
additional information
-
no inhibition with 0.14 mM (2R,3R)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-prolyl]aziridine-2,3-dicarboxylate, (2R,3R)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(R)-nipecotyl]aziridine-2,3-dicarboxylate, (2R,3R)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-nipecotyl]aziridine-2,3-dicarboxylate, (2R,3R)-diethyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(R)-azetidine-2-carbonyl]aziridine-2,3-dicarboxylate, or (2S,3S)-dibenzyl-1-[N-(tert-butoxycarbonyl)-(S)-leucyl-(S)-prolyl]-aziridine-2,3-dicarboxylate
-
additional information
-
not inhibited by N-(L-3-trans-(propylcarbamoyl)oxilane-2-carbonyl)-L-isoluecyl-L-proline (CA-074)
-
additional information
-
heparin cofactor II and plasminogen activator inhibitor 1 do not inhibit cathepsin L
-
additional information
-
native cathepsin L was completely inhibited by 0.001, 0.004, or 0.01 mM cathepsin L propeptide (10 min, pH 6.5, room temperature)
-
additional information
-
histones do not inhibit cathepsin L activity even at a 100fold molar excess (0.00215 mM histone concentration)
-
additional information
endogenous cysteine peptidase inhibitors like stefin B act in safe-guarding mammalian cells by their presence in the cyto- or nucleoplasm, and thus protect from activities of proteolytic enzymes leaking into the cytoplasm upon, for instance, non-intended rupture of endolysosomes in pathological situations
-
additional information
development and synthesis of a clickable and tagless activity-based probes of cathepsin L, method, overview. The probe KDP-1 is highly efficient, active-site directed and activity-dependent, selective, cell penetrable, and non-toxic to human cells. Using a zebrafish model, it is schown that the probe can inhibit cathepsin L function in vivo during the hatching process. KDP-1 exhibits a strong time dependent inactivation of cathepsin L activity, although with about 10fold lower rate than KD-1
-
additional information
-
development and synthesis of a clickable and tagless activity-based probes of cathepsin L, method, overview. The probe KDP-1 is highly efficient, active-site directed and activity-dependent, selective, cell penetrable, and non-toxic to human cells. Using a zebrafish model, it is schown that the probe can inhibit cathepsin L function in vivo during the hatching process. KDP-1 exhibits a strong time dependent inactivation of cathepsin L activity, although with about 10fold lower rate than KD-1
-
additional information
synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L, molecular modeling, overview
-
additional information
-
synthesis and biochemical evaluation of benzoylbenzophenone thiosemicarbazone analogues as potent and selective inhibitors of cathepsin L, molecular modeling, overview
-
additional information
screening and identification of inhibitors of Trypanosoma brucei cathepsin L with antitrypanosomal activity, overview
-
additional information
-
screening and identification of inhibitors of Trypanosoma brucei cathepsin L with antitrypanosomal activity, overview
-
additional information
no inhibition by EDTA, PMSF, and pepstatin A
-
additional information
-
no inhibition by EDTA, PMSF, and pepstatin A
-
additional information
-
insensitive to K+, phenylmethylsulfonylfluoride and pepstatin A
-
additional information
natural products as inhibitors of recombinant cathepsin L of Leishmania mexicana, overview
-
additional information
-
natural products as inhibitors of recombinant cathepsin L of Leishmania mexicana, overview
-
additional information
-
not inhibited by CA074Me
-
additional information
-
no inhibition by pepstatin, phenylmethane sulfonyl fluoride
-
additional information
not inhibited by N-ethylmaleimide, phenylmethylsulfonyl fluoride, antiprotinin, EDTA, EGTA, 1,10-phenanthroline, and pepstatin A
-
additional information
-
not inhibited by CA074Me
-
additional information
-
in vivo inhibitor from bovine skeletal muscle, purification, MW 30000 Da
-
additional information
screening and identification of inhibitors of Trypanosoma brucei cathepsin L with antitrypanosomal activity, overview
-
additional information
screening and identification of inhibitors of Trypanosoma brucei cathepsin L with antitrypanosomal activity, overview. No inhibition by 7 and 13
-