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Assay Detail

CHEMBL5106294

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Binding
Inhibition of human Cathepsin K
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

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Lead optimization of cathepsin K inhibitors for the treatment of Osteoarthritis.
Ginnetti AT, Paone DV, Nanda KK, Li J, Busuek M, Johnson SA, Lu J, Soisson SM, Robinson R, Fisher J, Webber A, Wesolowski G, Ma B, Duong L, Carroll S, Burgey CS, Stachel SJ.
Bioorg Med Chem Lett (2022) 74 : 128927 -128927
PubMed 35944849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 8 8.91 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5200434 1 9.30
CHEMBL5178296 1 9.30
CHEMBL5187327 1 9.22
CHEMBL5203617 1 9.15
CHEMBL5177796 1 9.15
CHEMBL523352 1 8.74
CHEMBL5187747 1 8.28
CHEMBL5203247 1 8.16

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5200434 IC50 = 0.5 nM 9.30
CHEMBL5178296 IC50 = 0.5 nM 9.30
CHEMBL5187327 IC50 = 0.6 nM 9.22
CHEMBL5203617 IC50 = 0.7 nM 9.15
CHEMBL5177796 IC50 = 0.7 nM 9.15
CHEMBL523352 IC50 = 1.8 nM 8.74
CHEMBL5187747 IC50 = 5.3 nM 8.28
CHEMBL5203247 IC50 = 6.9 nM 8.16