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Assay Detail

CHEMBL2345605

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

Binding
Inhibition of human recombinant ADAMTS5 expressed in HEK293 cells using Abz-TESEwSRGAIY-Dpa-KK as substrate measured for 2 hrs by fluorometric analysis
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Publication

Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.
Nuti E, Santamaria S, Casalini F, Yamamoto K, Marinelli L, La Pietra V, Novellino E, Orlandini E, Nencetti S, Marini AM, Salerno S, Taliani S, Da Settimo F, Nagase H, Rossello A.
Eur J Med Chem (2013) 62 : 379 -394
PubMed 23376997 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 6.31 7.77

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL24398 1 7.77
CHEMBL2337698 1 7.46
CHEMBL198778 1 6.48
CHEMBL19611 ILOMASTAT 2.0 1 6.30
CHEMBL2337691 1 6.21
CHEMBL2337696 1 5.85
CHEMBL2337690 1 5.75
CHEMBL197842 1 5.47
CHEMBL2337697 1 5.46

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL24398 IC50 = 17.0 nM 7.77
CHEMBL2337698 IC50 = 35.0 nM 7.46
CHEMBL198778 IC50 = 330.0 nM 6.48
CHEMBL19611 ILOMASTAT IC50 = 500.0 nM 6.30
CHEMBL2337691 IC50 = 620.0 nM 6.21
CHEMBL2337696 IC50 = 1410.0 nM 5.85
CHEMBL2337690 IC50 = 1770.0 nM 5.75
CHEMBL197842 IC50 = 3400.0 nM 5.47
CHEMBL2337697 IC50 = 3500.0 nM 5.46