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Assay Detail

CHEMBL881228

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Binding
Inhibitory concentration against Aggrecanase 1
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Publication

Synthesis and SAR of highly selective MMP-13 inhibitors.
Li J, Rush TS, Li W, DeVincentis D, Du X, Hu Y, Thomason JR, Xiang JS, Skotnicki JS, Tam S, Cunningham KM, Chockalingam PS, Morris EA, Levin JI.
Bioorg Med Chem Lett (2005) 15 : 4961 -4966
PubMed 16153831 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 5.07 5.36

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL427366 1 5.36
CHEMBL198262 1 5.25
CHEMBL425020 1 5.07
CHEMBL194430 1 4.84
CHEMBL199241 1 4.82
CHEMBL194377 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL427366 IC50 = 4400.0 nM 5.36
CHEMBL198262 IC50 = 5600.0 nM 5.25
CHEMBL425020 IC50 = 8600.0 nM 5.07
CHEMBL194430 IC50 = 14300.0 nM 4.84
CHEMBL199241 IC50 = 15000.0 nM 4.82
CHEMBL194377 IC50 > 15000.0 nM -