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Assay Detail

CHEMBL3222370

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

Binding
Inhibition of human catalytic domain of TACE assessed as inhibit the cleavage of the substrate by fluorescence-based FRET assay
3
Total Activities
3
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

Publication

Design, synthesis and biological evaluation of -lactam hydroxamate based TACE inhibitors
Argade A, Bahekar R, Desai J, Thombare P, Shah K, Gite S, Sunder R, Ranvir R, Bandyopadhyay D, Chakrabarti G, Joharapurkar A, Mahapatra J, Chatterjee A, Patel H, Shaikh M, Sairam KVVM, Jain M, Patel P
Medchemcomm (2011) 2 : 966 -972
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.41 8.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3221863 1 8.68
CHEMBL3221864 1 8.64
CHEMBL489100 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3221863 IC50 = 2.1 nM 8.68
CHEMBL3221864 IC50 = 2.3 nM 8.64
CHEMBL489100 IC50 = 12.0 nM 7.92