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

3.4.22.36

inflammasome

pyroptosis

pyrin

caspases

nod-like

lps

necrosis

tnf

apoptosis-associated

speck-like

lipopolysaccharide

adaptor

pro-il-1

toll-like

card

domain-containing

nucleotide-binding

neuroinflammation

autoinflammatory

lps-induced

bcl-2

domain-like

thp-1

multiprotein

tunel

microglia

gasdermin

danger

marrow-derived

interleukin-18

leucine-rich

cpp32

urate

nod2

damage-associated

nigericin

medicine

txnip

il-1ra

bmdms

pan-caspase

hmgb1

gouty

lymphopoietin

monosodium

fas-mediated

z-vad-fmk

fas-associated

caspase-3-like

pathogen-associated

z-devd-fmk

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

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Results	in table
52	Activating Compound
27	AA Sequence
2	Application
1	CAS Registry Number
32	Cloned(Commentary)
4	Crystallization (Commentary)
5816	Disease/ Diagnostics
9	Expression
27	General Information
64	IC50 Value
239	Inhibitors
82	Ki Value [mM]
16	KM Value [mM]
13	Localization
2	Metals/Ions
14	Molecular Weight [Da]
166	Natural Substrates/ Products (Substrates)
764	Organism
91	PDB ID
4	pH Optimum
17	Posttranslational Modification
55	Protein Variants
8	Purification (Commentary)
1	Reaction
1	Reaction Type
152	Reference
2	Renatured (Commentary)
143	Source Tissue
1	Specific Activity [micromol/min/mg]
295	Substrates and Products (Substrate)
13	Subunits
66	Synonyms
3	Temperature Optimum [°C]
8	Turnover Number [1/s]

IC50 Value

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of the Enzyme Summary Page.

IC50 Value on EC 3.4.22.36 - caspase-1

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0.0000036

(1S,9S)-N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-9-[(isoquinolin-1-ylcarbonyl)amino]-6,10-dioxooctahydro-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxamide

Homo sapiens

good selectivity against the related enzymes caspase-3 and caspase-8

678638

0.000004

(3S)-3-[([(1S,9S)-9-[(isoquinolin-1-ylcarbonyl)amino]-6,10-dioxooctahydro-6H-pyridazino[1,2-a][1,2]diazepin-1-yl]carbonyl)amino]-4-oxobutanoic acid

Homo sapiens

678593

0.000004

(3S)-3-[([(3S,6S,9aR)-6-[(isoquinolin-1-ylcarbonyl)amino]-5-oxo-2,3,5,6,9,9a-hexahydro-1H-pyrrolo[1,2-a]azepin-3-yl]carbonyl)amino]-4-oxobutanoic acid

Homo sapiens

678593

0.000003

(3S)-3-[([(4S,7S,10aS)-7-[(isoquinolin-1-ylcarbonyl)amino]-6-oxo-3,4,6,7,10,10a-hexahydro-1H-[1,4]oxazino[4,3-a]azepin-4-yl]carbonyl)amino]-4-oxobutanoic acid

Homo sapiens

678593

0.0007

1-([2-[(2,6-dimethoxyphenyl)carbonyl]hydrazino]carbonyl)-N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]cyclohexanecarboxamide

Homo sapiens

678637

0.000007 - 0.000015

2,5-dichloro-N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]benzamide

2 entries

0.000008 - 0.000029

3-chloro-N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]benzamide

2 entries

0.000015

acetyl-L-Leu-L-Glu-L-His-L-Asp-CHO

Homo sapiens

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

708128

0.1

berkedrimane A

Homo sapiens

at 37°C, pH not specified in the publication

732359

0.09

berkedrimane B

Homo sapiens

at 37°C, pH not specified in the publication

732359

0.00001

L-Tyr-L-Val-L-Ala-L-Asp-CHO

Homo sapiens

708272

0.0000216

L-Tyr-L-Val-L-Ala-L-Asp-CN

Homo sapiens

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

708128

0.000001

N-((S,Z)-1-((R)-1-((3S)-2-hydroxy-5-oxo-tetrahydrofuran-3-ylamino)-1-oxopropan-2-yl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl)-2-naphthamide

Homo sapiens

678593

0.000013

N-((S,Z)-1-((S)-1-((3S)-2-hydroxy-5-oxo-tetrahydrofuran-3-ylamino)-1-oxopropan-2-yl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl)-2-naphthamide

Homo sapiens

678593

0.00002

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]-1-benzothiophene-2-carboxamide

Homo sapiens

678593

0.000011

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]-3-(trifluoromethyl)benzamide

Homo sapiens

678593

0.000053

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]-3-methoxybenzamide

Homo sapiens

678593

0.000168

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]benzamide

Homo sapiens

678593

0.000027

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]isoquinoline-1-carboxamide

Homo sapiens

678593

0.000014

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide

Homo sapiens

678593

0.000002

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-6-[[(phenylcarbonyl)amino]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide

Homo sapiens

678593

0.000003

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-6-[[(phenylsulfonyl)amino]methyl]-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide

Homo sapiens

678593

0.000002

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-6-([[(2-methoxyphenyl)carbonyl]amino]methyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide

Homo sapiens

678593

0.000001

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-6-([[(3-methoxyphenyl)carbonyl]amino]methyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide

Homo sapiens

678593

0.000001

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-6-([[(4-methoxyphenyl)carbonyl]amino]methyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide

Homo sapiens

678593

0.000019

N-[(3S)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-6-methyl-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide

Homo sapiens

678593

0.00024

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methoxyphenyl)carbonyl]hydrazino]carbonyl)cyclohexanecarboxamide

Homo sapiens

678637

0.0002

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methoxyphenyl)carbonyl]hydrazino]carbonyl)cyclopentanecarboxamide

Homo sapiens

678637

0.00043

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methylphenyl)carbonyl]hydrazino]carbonyl)cyclohexanecarboxamide

Homo sapiens

678637

0.00049

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-([2-[(3-methylphenyl)carbonyl]hydrazino]carbonyl)cyclopentanecarboxamide

Homo sapiens

678637

0.00031

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(2-methylbenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide

Homo sapiens

678637

0.0029

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(2-naphthoyl)hydrazino]carbonyl]cyclopropanecarboxamide

Homo sapiens

678637

0.00026

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(3-methoxybenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide

Homo sapiens

678637

0.00015

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(3-methylbenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide

Homo sapiens

678637

0.00058

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(4-methylbenzoyl)hydrazino]carbonyl]cyclobutanecarboxamide

Homo sapiens

678637

0.00005

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-1-ylcarbonyl)hydrazino]carbonyl]cyclobutanecarboxamide

Homo sapiens

678637

0.00005

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-1-ylcarbonyl)hydrazino]carbonyl]cyclohexanecarboxamide

Homo sapiens

678637

0.0004

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-1-ylcarbonyl)hydrazino]carbonyl]cyclopentanecarboxamide

Homo sapiens

678637

0.00024

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]cyclobutanecarboxamide

Homo sapiens

678637

0.00009

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]cyclohexanecarboxamide

Homo sapiens

678637

0.00015

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-1-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]cyclopentanecarboxamide

Homo sapiens

678637

0.00043

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-2-([2-[(3-methylphenyl)carbonyl]hydrazino]carbonyl)-2,3-dihydro-1H-indene-2-carboxamide

Homo sapiens

678637

0.00004

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-2-[[2-(naphthalen-1-ylcarbonyl)hydrazino]carbonyl]-2,3-dihydro-1H-indene-2-carboxamide

Homo sapiens

678637

0.00003

N-[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]-2-[[2-(naphthalen-2-ylcarbonyl)hydrazino]carbonyl]-2,3-dihydro-1H-indene-2-carboxamide

Homo sapiens

678637

0.000022

N-[(3S)-6-(hydroxymethyl)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-2,3,4,7-tetrahydro-1H-azepin-3-yl]naphthalene-2-carboxamide

Homo sapiens

678593

0.000077

N-[(3S,5Z)-1-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-2-oxo-1,2,3,4,7,8-hexahydroazocin-3-yl]isoquinoline-1-carboxamide

Homo sapiens

678593

0.00032

N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]-1-benzothiophene-2-carboxamide

Homo sapiens

good selectivity against the related enzymes caspase-3 and caspase-8

678638

0.0023

N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]benzamide

Homo sapiens

good selectivity against the related enzymes caspase-3 and caspase-8

678638

0.00013

N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]isoquinoline-1-carboxamide

Homo sapiens

good selectivity against the related enzymes caspase-3 and caspase-8

678638

0.00015

N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-1,1-dioxido-5-oxo-1,4-thiazepan-6-yl]naphthalene-2-carboxamide

Homo sapiens

good selectivity against the related enzymes caspase-3 and caspase-8

678638

0.00008

N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]-1-benzothiophene-2-carboxamide

Homo sapiens

good selectivity against the related enzymes caspase-3 and caspase-8

678638

N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]-3-(trifluoromethyl)benzamide

Homo sapiens

good selectivity against the related enzymes caspase-3 and caspase-8

678638

0.00035

N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]benzamide

Homo sapiens

good selectivity against the related enzymes caspase-3 and caspase-8

678638

0.00007

N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]isoquinoline-1-carboxamide

Homo sapiens

good selectivity against the related enzymes caspase-3 and caspase-8

678638

0.00003

N-[(6R)-4-(2-[[(3S)-2-hydroxy-5-oxotetrahydrofuran-3-yl]amino]-2-oxoethyl)-5-oxo-1,4-thiazepan-6-yl]naphthalene-2-carboxamide

Homo sapiens

good selectivity against the related enzymes caspase-3 and caspase-8

678638

0.000000023

NCGC00183434

Homo sapiens

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

708128

0.00000258

NCGC00183681

Homo sapiens

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

708128

0.0000434

NCGC00185682

Homo sapiens

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

708128

0.0000005

p35

Spodoptera frugiperda

P89116

IC50: 0.5 nM

648074

0.0000036

pralnacasan

Homo sapiens

678637

0.000000204

VRT-043198

Homo sapiens

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

708128

0.000024

YN-1234

Homo sapiens

708272