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Assay Detail

CHEMBL1023822

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

Binding
Inhibition of humanized rabbit cathepsin K Tyr61Asp and Val157Leu mutant
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Identification of a nonbasic, nitrile-containing cathepsin K inhibitor (MK-1256) that is efficacious in a monkey model of osteoporosis.
Robichaud J, Black WC, Thérien M, Paquet J, Oballa RM, Bayly CI, McKay DJ, Wang Q, Isabel E, Léger S, Mellon C, Kimmel DB, Wesolowski G, Percival MD, Massé F, Desmarais S, Falgueyret JP, Crane SN.
J Med Chem (2008) 51 : 6410 -6420
PubMed 18811135 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 9.20 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL201782 1 9.55
CHEMBL492654 1 9.43
CHEMBL523352 1 9.21
CHEMBL495113 1 9.16
CHEMBL523836 1 9.09
CHEMBL492655 1 8.74

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL201782 IC50 = 0.28 nM 9.55
CHEMBL492654 IC50 = 0.37 nM 9.43
CHEMBL523352 IC50 = 0.62 nM 9.21
CHEMBL495113 IC50 = 0.69 nM 9.16
CHEMBL523836 IC50 = 0.81 nM 9.09
CHEMBL492655 IC50 = 1.8 nM 8.74