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Assay Detail

CHEMBL656201

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

Binding
Inhibition of the cysteine protease human Calpain 1
ChEMBL ↗
86
Total Activities
86
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Calpain-1 catalytic subunit (CHEMBL3891) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Novel peptidyl alpha-keto amide inhibitors of calpains and other cysteine proteases.
Li Z, Ortega-Vilain AC, Patil GS, Chu DL, Foreman JE, Eveleth DD, Powers JC.
J Med Chem (1996) 39 : 4089 -4098
PubMed 8831774 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 86 6.37 7.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL132586 — — 1 7.72
CHEMBL129831 — — 1 7.30
CHEMBL331850 — — 1 7.28
CHEMBL134092 — — 1 7.16
CHEMBL133521 — — 1 7.10
CHEMBL131002 — — 1 7.00
CHEMBL130338 — — 1 6.96
CHEMBL134283 — — 1 6.96
CHEMBL134173 — — 1 6.92
CHEMBL335291 — — 1 6.92
CHEMBL132987 — — 1 6.92
CHEMBL133970 — — 1 6.89
CHEMBL130756 — — 1 6.89
CHEMBL134002 — — 1 6.85
CHEMBL132773 — — 1 6.80
CHEMBL413308 — — 1 6.75
CHEMBL133936 — — 1 6.70
CHEMBL337830 — — 1 6.70
CHEMBL117336 — — 1 6.70
CHEMBL130345 — — 1 6.70
CHEMBL420872 — — 1 6.70
CHEMBL118025 — — 1 6.70
CHEMBL132566 — — 1 6.66
CHEMBL3706737 — — 1 6.66
CHEMBL130146 — — 1 6.64
CHEMBL130599 — — 1 6.62
CHEMBL422260 — — 1 6.60
CHEMBL336649 — — 1 6.60
CHEMBL325147 — — 1 6.60
CHEMBL131639 — — 1 6.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL132586 — Ki = 19.0 nM 7.72
CHEMBL129831 — Ki = 50.0 nM 7.30
CHEMBL331850 — Ki = 52.0 nM 7.28
CHEMBL134092 — Ki = 70.0 nM 7.16
CHEMBL133521 — Ki = 80.0 nM 7.10
CHEMBL131002 — Ki = 100.0 nM 7.00
CHEMBL130338 — Ki = 110.0 nM 6.96
CHEMBL134283 — Ki = 110.0 nM 6.96
CHEMBL134173 — Ki = 120.0 nM 6.92
CHEMBL335291 — Ki = 120.0 nM 6.92
CHEMBL132987 — Ki = 120.0 nM 6.92
CHEMBL133970 — Ki = 130.0 nM 6.89
CHEMBL130756 — Ki = 130.0 nM 6.89
CHEMBL134002 — Ki = 140.0 nM 6.85
CHEMBL132773 — Ki = 160.0 nM 6.80
CHEMBL413308 — Ki = 180.0 nM 6.75
CHEMBL133936 — Ki = 200.0 nM 6.70
CHEMBL337830 — Ki = 200.0 nM 6.70
CHEMBL117336 — Ki = 200.0 nM 6.70
CHEMBL130345 — Ki = 200.0 nM 6.70
CHEMBL420872 — Ki = 200.0 nM 6.70
CHEMBL118025 — Ki = 200.0 nM 6.70
CHEMBL132566 — Ki = 220.0 nM 6.66
CHEMBL3706737 — Ki = 220.0 nM 6.66
CHEMBL130146 — Ki = 230.0 nM 6.64
CHEMBL130599 — Ki = 240.0 nM 6.62
CHEMBL336649 — Ki = 250.0 nM 6.60
CHEMBL325147 — Ki = 250.0 nM 6.60
CHEMBL422260 — Ki = 250.0 nM 6.60
CHEMBL131639 — Ki = 270.0 nM 6.57
CHEMBL131866 — Ki = 280.0 nM 6.55
CHEMBL133634 — Ki = 290.0 nM 6.54
CHEMBL131540 — Ki = 300.0 nM 6.52
CHEMBL130215 — Ki = 300.0 nM 6.52
CHEMBL3706738 — Ki = 310.0 nM 6.51
CHEMBL130122 — Ki = 330.0 nM 6.48
CHEMBL131319 — Ki = 330.0 nM 6.48
CHEMBL130580 — Ki = 350.0 nM 6.46
CHEMBL421910 — Ki = 350.0 nM 6.46
CHEMBL133749 — Ki = 350.0 nM 6.46
CHEMBL116477 — Ki = 350.0 nM 6.46
CHEMBL130629 — Ki = 350.0 nM 6.46
CHEMBL3706739 — Ki = 370.0 nM 6.43
CHEMBL130359 — Ki = 380.0 nM 6.42
CHEMBL130753 — Ki = 380.0 nM 6.42
CHEMBL3706740 — Ki = 380.0 nM 6.42
CHEMBL132839 — Ki = 410.0 nM 6.39
CHEMBL131781 — Ki = 420.0 nM 6.38
CHEMBL435203 — Ki = 460.0 nM 6.34
CHEMBL133806 — Ki = 480.0 nM 6.32