Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL873902

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

Binding
Inhibition of human recombinant tumor necrosis factor-alpha converting enzyme.
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Synthesis and biological activity of piperazine-based dual MMP-13 and TNF-alpha converting enzyme inhibitors.
Letavic MA, Barberia JT, Carty TJ, Hardink JR, Liras J, Lopresti-Morrow LL, Mitchell PG, Noe MC, Reeves LM, Snow SL, Stam EJ, Sweeney FJ, Vaughn ML, Yu CH.
Bioorg Med Chem Lett (2003) 13 : 3243 -3246
PubMed 12951101 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.84 8.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL110211 1 8.30
CHEMBL110901 1 8.22
CHEMBL111862 1 8.22
CHEMBL110591 1 8.22
CHEMBL110576 1 8.22
CHEMBL263054 1 8.15
CHEMBL109775 1 8.15
CHEMBL281920 1 8.05
CHEMBL278060 1 7.96
CHEMBL322476 1 7.96
CHEMBL95807 1 7.89
CHEMBL326221 1 7.85
CHEMBL112232 1 7.72
CHEMBL109833 1 7.60
CHEMBL110994 1 7.58
CHEMBL109267 1 7.55
CHEMBL322705 1 7.51
CHEMBL111460 1 7.50
CHEMBL111068 1 7.47
CHEMBL111262 1 7.40
CHEMBL325150 1 7.17

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL110211 IC50 = 5.0 nM 8.30
CHEMBL110901 IC50 = 6.0 nM 8.22
CHEMBL111862 IC50 = 6.0 nM 8.22
CHEMBL110591 IC50 = 6.0 nM 8.22
CHEMBL110576 IC50 = 6.0 nM 8.22
CHEMBL263054 IC50 = 7.0 nM 8.15
CHEMBL109775 IC50 = 7.0 nM 8.15
CHEMBL281920 IC50 = 9.0 nM 8.05
CHEMBL278060 IC50 = 11.0 nM 7.96
CHEMBL322476 IC50 = 11.0 nM 7.96
CHEMBL95807 IC50 = 13.0 nM 7.89
CHEMBL326221 IC50 = 14.0 nM 7.85
CHEMBL112232 IC50 = 19.0 nM 7.72
CHEMBL109833 IC50 = 25.0 nM 7.60
CHEMBL110994 IC50 = 26.0 nM 7.58
CHEMBL109267 IC50 = 28.0 nM 7.55
CHEMBL322705 IC50 = 31.0 nM 7.51
CHEMBL111460 IC50 = 32.0 nM 7.50
CHEMBL111068 IC50 = 34.0 nM 7.47
CHEMBL111262 IC50 = 40.0 nM 7.40
CHEMBL325150 IC50 = 68.0 nM 7.17