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Assay Detail

CHEMBL833550

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

Binding
Inhibitory concentration against TNF-alpha converting enzyme at 1 uM
27
Total Activities
27
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 SAR of diazepine and thiazepine TACE and MMP inhibitors.
Zask A, Kaplan J, Du X, MacEwan G, Sandanayaka V, Eudy N, Levin J, Jin G, Xu J, Cummons T, Barone D, Ayral-Kaloustian S, Skotnicki J.
Bioorg Med Chem Lett (2005) 15 : 1641 -1645
PubMed 15745814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.68 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL180891 1 8.40
CHEMBL181317 1 8.30
CHEMBL369574 1 8.15
CHEMBL361809 1 8.00
CHEMBL369302 1 8.00
CHEMBL359920 1 7.96
CHEMBL180410 1 7.92
CHEMBL180181 1 7.89
CHEMBL180627 1 7.85
CHEMBL178929 1 7.82
CHEMBL180484 1 7.77
CHEMBL181328 1 7.72
CHEMBL178732 1 7.72
CHEMBL362797 1 7.70
CHEMBL361959 1 7.64
CHEMBL180130 1 7.64
CHEMBL181094 1 7.62
CHEMBL360257 1 7.62
CHEMBL180047 1 7.55
CHEMBL181365 1 7.52
CHEMBL180245 1 7.46
CHEMBL181208 1 7.43
CHEMBL180333 1 7.21
CHEMBL180197 1 7.17
CHEMBL359502 1 7.13
CHEMBL181110 1 7.12
CHEMBL183132 1 7.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL180891 IC50 = 4.0 nM 8.40
CHEMBL181317 IC50 = 5.0 nM 8.30
CHEMBL369574 IC50 = 7.0 nM 8.15
CHEMBL361809 IC50 = 10.0 nM 8.00
CHEMBL369302 IC50 = 10.0 nM 8.00
CHEMBL359920 IC50 = 11.0 nM 7.96
CHEMBL180410 IC50 = 12.0 nM 7.92
CHEMBL180181 IC50 = 13.0 nM 7.89
CHEMBL180627 IC50 = 14.0 nM 7.85
CHEMBL178929 IC50 = 15.0 nM 7.82
CHEMBL180484 IC50 = 17.0 nM 7.77
CHEMBL181328 IC50 = 19.0 nM 7.72
CHEMBL178732 IC50 = 19.0 nM 7.72
CHEMBL362797 IC50 = 20.0 nM 7.70
CHEMBL361959 IC50 = 23.0 nM 7.64
CHEMBL180130 IC50 = 23.0 nM 7.64
CHEMBL181094 IC50 = 24.0 nM 7.62
CHEMBL360257 IC50 = 24.0 nM 7.62
CHEMBL180047 IC50 = 28.0 nM 7.55
CHEMBL181365 IC50 = 30.0 nM 7.52
CHEMBL180245 IC50 = 35.0 nM 7.46
CHEMBL181208 IC50 = 37.0 nM 7.43
CHEMBL180333 IC50 = 61.0 nM 7.21
CHEMBL180197 IC50 = 68.0 nM 7.17
CHEMBL359502 IC50 = 74.0 nM 7.13
CHEMBL181110 IC50 = 75.0 nM 7.12
CHEMBL183132 IC50 = 83.0 nM 7.08