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3.4.22.36: caspase-1

This is an abbreviated version!
For detailed information about caspase-1, go to the full flat file.

Word Map on EC 3.4.22.36

Reaction

Strict requirement for an Asp residue at position P1 and has a preferred cleavage sequence of Tyr-Val-Ala-Asp-/- =

Synonyms

apoptosis-related cysteine protease, C14.001, CASP-1, Casp1, caspase 1, caspase-1, Csp-1, cysteine aspartyl protease-1, effector caspase, H.a.CASP1, hearm caspase-1, ICE, IL-1 beta converting enzyme, IL-1 converting enzyme, IL-1-converting enzyme, IL-1B converting enzyme, IL-1BC, IL-1beta-converting enzyme, IL-1beta–-converting enzyme, IL1beta-converting enzyme, interleukin 1, beta, convertase, interleukin converting enzyme, interleukin-1 beta converting enzyme, interleukin-1 converting enzyme, interleukin-1-converting enzyme, interleukin-1B converting enzyme, interleukin-1beta converting enzyme, interleukin-1beta-converting enzyme, interleukin-converting enzyme, p45, procaspase-1

ECTree

     3 Hydrolases
         3.4 Acting on peptide bonds (peptidases)
             3.4.22 Cysteine endopeptidases
                3.4.22.36 caspase-1

KI Value

KI Value on EC 3.4.22.36 - caspase-1

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Ki VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000054
(3S)-3-((6-[((4-[(6-chloropyrazin-2-yl)amino]phenyl)carbonyl)amino]-2-thiophen-2-ylhexanoyl)amino)-4-oxobutanoic acid
-
-
0.000005
(3S)-3-((6-[((4-[(6-methylquinoxalin-2-yl)amino]phenyl)carbonyl)amino]-2-thiophen-2-ylhexanoyl)amino)-4-oxobutanoic acid
-
-
0.000008
(3S)-3-([2-(2-fluorophenyl)-6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)-4-oxobutanoic acid
-
-
0.000016
(3S)-3-([2-ethyl-6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)-4-oxobutanoic acid
-
-
0.000004
(3S)-3-([6-(([3-methyl-4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)-2-thiophen-2-ylhexanoyl]amino)-4-oxobutanoic acid
-
-
0.000005
(3S)-4-oxo-3-([2-phenyl-6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
0.0052
(3S)-4-oxo-3-([4-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)butanoyl]amino)butanoic acid
-
-
0.0028
(3S)-4-oxo-3-([5-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)pentanoyl]amino)butanoic acid
-
-
0.0001
(3S)-4-oxo-3-([6-(([4-(pyrazin-2-ylamino)phenyl]carbonyl)amino)-2-thiophen-2-ylhexanoyl]amino)butanoic acid
-
-
0.037
(3S)-4-oxo-3-([6-(([4-(pyrazin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
0.00019
(3S)-4-oxo-3-([6-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
0.000043 - 0.00032
(3S)-4-oxo-3-([6-(([4-(quinoxalin-2-yloxy)phenyl]carbonyl)amino)-2-thiophen-2-ylhexanoyl]amino)butanoic acid
0.0024
(3S)-4-oxo-3-([6-(([4-(quinoxalin-2-yloxy)phenyl]carbonyl)amino)hexanoyl]amino)butanoic acid
-
-
0.000005 - 0.0026
(3S)-4-oxo-3-([7-(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)heptanoyl]amino)butanoic acid
0.0001
(3S)-4-oxo-3-[((4-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]phenyl)carbonyl)amino]butanoic acid
-
-
0.00026
(3S)-4-oxo-3-[((4-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-2-yl)carbonyl)amino]butanoic acid
-
-
0.001
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]-2,3-dihydropyrazin-2-yl)carbonyl)amino]butanoic acid
-
-
0.0021
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]furan-2-yl)carbonyl)amino]butanoic acid
-
-
0.00012
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-2-yl)acetyl)amino]butanoic acid
-
-
0.000035
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-2-yl)carbonyl)amino]butanoic acid
-
-
0.00012
(3S)-4-oxo-3-[((5-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]thiophen-3-yl)carbonyl)amino]butanoic acid
-
-
0.000005
(3S)-4-oxo-3-[((6-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]pyridin-3-yl)carbonyl)amino]butanoic acid
-
-
0.00195
(3S)-4-oxo-3-[((trans-4-[(([4-(quinoxalin-2-ylamino)phenyl]carbonyl)amino)methyl]cyclohexyl)carbonyl)amino]butanoic acid
-
-
0.0021
(3S)-4-oxo-3-[(7-oxo-7-([4-(quinoxalin-2-ylamino)phenyl]amino)heptanoyl)amino]butanoic acid
-
-
0.0072
(S)-2-(4'-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
0.000047
(S)-3-((S)-2-((S)-2-(2-naphthamido)-3-methylbutanamido)-propanamido)-4-(2-hydroxy)benzylaminobutanoic acid
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30°C
0.0068
(S)-3-(2'-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
0.0069
(S)-3-(2-naphthalen-1-yl-benzenesulfonylamino)-4-oxo-butyric acid
-
-
0.0023
(S)-3-(3'-acetylamino-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
0.0031
(S)-3-(3'-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
0.0019
(S)-3-(6-methyl-biphenyl-2-sulfonylamino)-4-oxo-butyric acid
-
-
0.0016
(S)-3-(biphenyl-2-sulfonylamino)-4-oxobutyric acid
-
-
0.024
(S)-3-benzenesulfonylamino-4-oxo-5-(3-phenyl-propylsulfanyl)-pentanoic acid
-
-
0.024
(S)-3-benzenesulfonylamino-4-oxo-9-phenyl-nonanoic acid
-
-
0.025
(S)-3-benzyloxycarbonylamino-4-oxo-5-(3-phenyl-propylsulfanyl)-pentanoic acid
-
-
0.119
(S)-3-benzyloxycarbonylamino-4-oxo-9-phenyl-nonanoic acid
-
-
0.0094
(S)-3-benzynesulfonylamino-4-oxo-butyric acid
-
-
0.119
3-([(benzyloxy)carbonyl]amino)-4-oxo-9-phenylnonanoic acid
-
-
0.065
3-([(benzyloxy)carbonyl]amino)-5-([(2,3-dihydro-1H-inden-1-ylmethyl)(dihydroxy)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.016
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(2-naphthalen-1-ylethyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.011
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(2-phenylethyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.0345
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(3-phenylpropyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.022
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(naphthalen-1-yl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.037
3-([(benzyloxy)carbonyl]amino)-5-([dihydroxy(phenyl)-lambda4-sulfanyl]amino)-4-oxopentanoic acid
-
-
0.033
3-[[(benzyloxy)carbonyl]amino]-5-[[(2-cyclohexylethyl)sulfonyl]amino]-4-oxopentanoic acid
-
-
0.018
5-([benzyl(dihydroxy)-lambda4-sulfanyl]amino)-3-([(benzyloxy)carbonyl]amino)-4-oxopentanoic acid
-
-
0.083
acetyl-Ala-Pro-Nle-Asp-aldehyde
-
pH 7.5
0.000015 - 0.000018
acetyl-DEVD-aldehyde
0.00002
acetyl-DEVS-aldehyde
-
pH 7.5, 37°C
0.000011
acetyl-Tyr-Val-Ala-Asp-CO-(CH2)5-Ph
-
pH 7.5
0.000000056
acetyl-WEHD-aldehyde
-
pH 7.5, 25°C
0.00000076 - 0.000006
acetyl-YVAD-aldehyde
0.03
benzyloxycarbonyl-Pro-Nle-Asp-aldehyde
-
pH 7.5
0.000008
benzyloxycarbonyl-VAD-CHO
-
-
0.00000001
cowpox serpin CrmA
-
pH 7.5, 25°C
-
0.00036
Glu-Val-Asp-aldehyde
pH 7.5
0.3
kaempferol
-
pH not specified in the publication, 30°C, value above
0.118
luteolin
-
pH not specified in the publication, 30°C
0.014
myricetin
-
pH not specified in the publication, 30°C
0.05
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2R)-1-carboxy-5-phenylpentan-2-yl]-L-alaninamide
-
IC50 above 0.05 mM, in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30°C
0.0006
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-(benzylamino)-3-carboxypropan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30°C
0.000945
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-(cyclohexylamino)propan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30°C
0.0012
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[(2-fluorobenzyl)amino]propan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30°C
0.000965
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[(2-methoxybenzyl)amino]propan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30°C
0.00137
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[(4-hydroxybenzyl)amino]propan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30°C
0.000128
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-carboxy-3-[methyl(phenyl)amino]propan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30°C
0.00029
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-[(1,3-benzodioxol-5-ylmethyl)amino]-3-carboxypropan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30°C
0.00182
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-[(4-carbamoylbenzyl)amino]-3-carboxypropan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30°C
0.00189
N-(naphthalen-2-ylcarbonyl)-L-valyl-N-[(2S)-1-[benzyl(methyl)amino]-3-carboxypropan-2-yl]-L-alaninamide
-
in 50 mM HEPES, pH 7.4, 100 mM NaCl, 10 mM dithiothreitol, 1 mM EDTA, 10% (v/v) glycerol, 0.1% (v/v) CHAPS, 1% (v/v) DMSO, at 30°C
0.000004
N-([4-(quinoxalin-2-ylamino)phenyl]carbonyl)-L-valyl-N-[(1S)-2-carboxy-1-formylethyl]-L-alaninamide
-
-
0.000004
N-acetyl-L-tyrosyl-alpha-glutamyl-N-[1-(carboxymethyl)-3-([dihydroxy(2-phenylethyl)-lambda4-sulfanyl]amino)-2-oxopropyl]-L-alaninamide
-
-
0.000014
N-acetyl-L-tyrosylvalyl-N-[1-(carboxymethyl)-2-oxo-7-phenylheptyl]-L-alaninamide
-
-
0.0000239
N-[(benzyloxy)carbonyl]-alpha-glutamyl-N-[1-(carboxymethyl)-3-([dihydroxy(2-phenylethyl)-lambda4-sulfanyl]amino)-2-oxopropyl]-L-alaninamide
-
-
0.000004
N-[(benzyloxy)carbonyl]valyl-N-[1-(carboxymethyl)-3-([dihydroxy(2-phenylethyl)-lambda4-sulfanyl]amino)-2-oxopropyl]-L-alaninamide
-
-
0.0000004
NCGC00183434
-
in 50 mM HEPES, pH 7.4, containing 1 M sodium citrate, 100 mM NaCl, 0.1 mM EDTA, 10 mM dithiothreitol, 0.01% (v/v) CHAPS, 1% (v/v) DMSO, and 0.1 mg/ml bovine serum albumin
0.3
quercetin
-
pH not specified in the publication, 30°C, value above
additional information
additional information
-
the Ki-value for acetyl-IETD-aldehyde is below 6 nM and the Ki-value for acetyl-AEVD-aldehyde is below 12 nM
-