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Assay Detail

CHEMBL4013264

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

Binding
Inhibition of human ADAMTS4 using VQTVTWPDMELPLPRNITEGEARGSVILTVKPIFEVSPSPLKG peptide as substrate after 3 hrs by Alphascreen assay
8
Total Activities
8
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

A Highly Selective Hydantoin Inhibitor of Aggrecanase-1 and Aggrecanase-2 with a Low Projected Human Dose.
Durham TB, Marimuthu J, Toth JL, Liu C, Adams L, Mudra DR, Swearingen C, Lin C, Chambers MG, Thirunavukkarasu K, Wiley MR.
J Med Chem (2017) 60 : 5933 -5939
PubMed 28613895 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.47 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4066965 1 9.00
CHEMBL187092 1 9.00
CHEMBL4072836 1 8.70
CHEMBL3980860 1 8.70
CHEMBL4102193 1 8.40
CHEMBL3972836 1 8.15
CHEMBL4094455 1 7.92
CHEMBL3955404 1 7.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4066965 IC50 = 1.0 nM 9.00
CHEMBL187092 IC50 = 1.0 nM 9.00
CHEMBL4072836 IC50 = 2.0 nM 8.70
CHEMBL3980860 IC50 = 2.0 nM 8.70
CHEMBL4102193 IC50 = 4.0 nM 8.40
CHEMBL3972836 IC50 = 7.0 nM 8.15
CHEMBL4094455 IC50 = 12.0 nM 7.92
CHEMBL3955404 IC50 = 14.0 nM 7.85