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Assay Detail

CHEMBL2167993

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

Binding
Inhibition of ADAMTS-4 using WAAG-3R as substrate preincubated for 15 mins measured after 1 hr
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Publication

Discovery of highly potent and selective small molecule ADAMTS-5 inhibitors that inhibit human cartilage degradation via encoded library technology (ELT).
Deng H, O'Keefe H, Davie CP, Lind KE, Acharya RA, Franklin GJ, Larkin J, Matico R, Neeb M, Thompson MM, Lohr T, Gross JW, Centrella PA, O'Donovan GK, Bedard KL, van Vloten K, Mataruse S, Skinner SR, Belyanskaya SL, Carpenter TY, Shearer TW, Clark MA, Cuozzo JW, Arico-Muendel CC, Morgan BA.
J Med Chem (2012) 55 : 7061 -7079
PubMed 22891645 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.03 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL187092 1 8.52
CHEMBL2164113 1 5.92
CHEMBL2164094 1 5.89
CHEMBL2164121 1 5.82
CHEMBL2164120 1 5.73
CHEMBL2164122 1 5.22
CHEMBL2164111 1 5.08

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL187092 IC50 = 3.0 nM 8.52
CHEMBL2164113 IC50 = 1200.0 nM 5.92
CHEMBL2164094 IC50 = 1300.0 nM 5.89
CHEMBL2164121 IC50 = 1500.0 nM 5.82
CHEMBL2164120 IC50 = 1870.0 nM 5.73
CHEMBL2164122 IC50 = 6000.0 nM 5.22
CHEMBL2164111 IC50 = 8300.0 nM 5.08