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Assay Detail

CHEMBL819944

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

Binding
In vitro inhibition of tumor necrosis factor-alpha converting enzyme
20
Total Activities
20
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Acetylenic TACE inhibitors. Part 1. SAR of the acyclic sulfonamide hydroxamates.
Levin JI, Chen JM, Cheung K, Cole D, Crago C, Santos ED, Du X, Khafizova G, MacEwan G, Niu C, Salaski EJ, Zask A, Cummons T, Sung A, Xu J, Zhang Y, Xu W, Ayral-Kaloustian S, Jin G, Cowling R, Barone D, Mohler KM, Black RA, Skotnicki JS.
Bioorg Med Chem Lett (2003) 13 : 2799 -2803
PubMed 12873518 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 20 7.83 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96396 1 8.52
CHEMBL94948 1 8.40
CHEMBL94715 1 8.30
CHEMBL94643 1 8.30
CHEMBL316928 1 8.22
CHEMBL316298 1 8.22
CHEMBL92927 1 8.15
CHEMBL321556 1 8.15
CHEMBL328751 1 8.00
CHEMBL96417 1 8.00
CHEMBL94363 1 7.89
CHEMBL94357 1 7.82
CHEMBL317624 1 7.77
CHEMBL96636 1 7.75
CHEMBL98061 1 7.58
CHEMBL94518 1 7.42
CHEMBL96637 1 7.27
CHEMBL96419 1 7.14
CHEMBL94386 1 6.92
CHEMBL97762 1 6.84

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96396 IC50 = 3.0 nM 8.52
CHEMBL94948 IC50 = 4.0 nM 8.40
CHEMBL94715 IC50 = 5.0 nM 8.30
CHEMBL94643 IC50 = 5.0 nM 8.30
CHEMBL316928 IC50 = 6.0 nM 8.22
CHEMBL316298 IC50 = 6.0 nM 8.22
CHEMBL92927 IC50 = 7.0 nM 8.15
CHEMBL321556 IC50 = 7.0 nM 8.15
CHEMBL328751 IC50 = 10.0 nM 8.00
CHEMBL96417 IC50 = 10.0 nM 8.00
CHEMBL94363 IC50 = 13.0 nM 7.89
CHEMBL94357 IC50 = 15.0 nM 7.82
CHEMBL317624 IC50 = 17.0 nM 7.77
CHEMBL96636 IC50 = 18.0 nM 7.75
CHEMBL98061 IC50 = 26.0 nM 7.58
CHEMBL94518 IC50 = 38.0 nM 7.42
CHEMBL96637 IC50 = 54.0 nM 7.27
CHEMBL96419 IC50 = 73.0 nM 7.14
CHEMBL94386 IC50 = 120.0 nM 6.92
CHEMBL97762 IC50 = 145.0 nM 6.84