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Assay Detail

CHEMBL3371729

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of recombinant human caspase-7 activity using Ac-DEVD-AMC as substrate preincubated for 10 mins by fluorescence assay
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Caspase-7 (CHEMBL3468)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of N-acyl-substituted 1,2-benzisothiazol-3-one derivatives as caspase-3 inhibitors.
Li Z, Pan Y, Zhong W, Zhu Y, Zhao Y, Li L, Liu W, Zhou H, Yang C.
Bioorg Med Chem (2014) 22 : 6735 -6745
PubMed 25468037 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 38 6.77 7.29

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3360048 1 7.29
CHEMBL3360047 1 7.27
CHEMBL3360059 1 7.25
CHEMBL3360051 1 7.22
CHEMBL3360046 1 7.20
CHEMBL3360053 1 7.14
CHEMBL3360045 1 7.14
CHEMBL3360056 1 7.13
CHEMBL3360050 1 7.11
CHEMBL3360049 1 7.06
CHEMBL3360055 1 7.01
CHEMBL3360057 1 7.00
CHEMBL3360044 1 6.96
CHEMBL3360043 1 6.95
CHEMBL3360060 1 6.94
CHEMBL3360061 1 6.94
CHEMBL3360035 1 6.91
CHEMBL3360038 1 6.84
CHEMBL417149 1 6.81
CHEMBL3360052 1 6.80
CHEMBL3233630 1 6.79
CHEMBL3360054 1 6.78
CHEMBL3360030 1 6.74
CHEMBL3360031 1 6.74
CHEMBL3360063 1 6.73
CHEMBL3360042 1 6.70
CHEMBL3360032 1 6.68
CHEMBL3360034 1 6.67
CHEMBL3360033 1 6.67
CHEMBL3360028 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3360048 IC50 = 51.9 nM 7.29
CHEMBL3360047 IC50 = 54.0 nM 7.27
CHEMBL3360059 IC50 = 56.7 nM 7.25
CHEMBL3360051 IC50 = 59.7 nM 7.22
CHEMBL3360046 IC50 = 63.7 nM 7.20
CHEMBL3360053 IC50 = 72.7 nM 7.14
CHEMBL3360045 IC50 = 72.5 nM 7.14
CHEMBL3360056 IC50 = 74.9 nM 7.13
CHEMBL3360050 IC50 = 78.4 nM 7.11
CHEMBL3360049 IC50 = 86.9 nM 7.06
CHEMBL3360055 IC50 = 97.9 nM 7.01
CHEMBL3360057 IC50 = 100.9 nM 7.00
CHEMBL3360044 IC50 = 109.0 nM 6.96
CHEMBL3360043 IC50 = 111.9 nM 6.95
CHEMBL3360061 IC50 = 115.0 nM 6.94
CHEMBL3360060 IC50 = 115.1 nM 6.94
CHEMBL3360035 IC50 = 123.0 nM 6.91
CHEMBL3360038 IC50 = 144.9 nM 6.84
CHEMBL417149 IC50 = 155.2 nM 6.81
CHEMBL3360052 IC50 = 158.2 nM 6.80
CHEMBL3233630 IC50 = 164.0 nM 6.79
CHEMBL3360054 IC50 = 166.3 nM 6.78
CHEMBL3360030 IC50 = 184.0 nM 6.74
CHEMBL3360031 IC50 = 182.3 nM 6.74
CHEMBL3360063 IC50 = 185.1 nM 6.73
CHEMBL3360042 IC50 = 198.3 nM 6.70
CHEMBL3360032 IC50 = 207.2 nM 6.68
CHEMBL3360034 IC50 = 213.3 nM 6.67
CHEMBL3360033 IC50 = 211.2 nM 6.67
CHEMBL3360028 IC50 = 268.7 nM 6.57
CHEMBL3360062 IC50 = 296.7 nM 6.53
CHEMBL3360041 IC50 = 330.1 nM 6.48
CHEMBL3360029 IC50 = 370.3 nM 6.43
CHEMBL3360036 IC50 = 457.7 nM 6.34
CHEMBL3360040 IC50 = 585.6 nM 6.23
CHEMBL3360039 IC50 = 607.1 nM 6.22
CHEMBL3360037 IC50 = 608.1 nM 6.22
CHEMBL3360058 IC50 = 18080.0 nM 4.74