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Assay Detail

CHEMBL863706

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

Binding
Inhibition of human cathepsin V
13
Total Activities
13
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cathepsin L2 (CHEMBL3272)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure activity relationships of 5-, 6-, and 7-methyl-substituted azepan-3-one cathepsin K inhibitors.
Yamashita DS, Marquis RW, Xie R, Nidamarthy SD, Oh HJ, Jeong JU, Erhard KF, Ward KW, Roethke TJ, Smith BR, Cheng HY, Geng X, Lin F, Offen PH, Wang B, Nevins N, Head MS, Haltiwanger RC, Narducci Sarjeant AA, Liable-Sands LM, Zhao B, Smith WW, Janson CA, Gao E, Tomaszek T, McQueney M, James IE, Gress CJ, Zembryki DL, Lark MW, Veber DF.
J Med Chem (2006) 49 : 1597 -1612
PubMed 16509577 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki app 11 - -
Ki 2 9.47 10.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL203665 RELACATIB 2.0 1 10.20
CHEMBL286364 1 8.74
CHEMBL202991 1 -
CHEMBL203224 1 -
CHEMBL377713 1 -
CHEMBL440574 1 -
CHEMBL205068 1 -
CHEMBL205172 1 -
CHEMBL438435 1 -
CHEMBL203556 1 -
CHEMBL204169 1 -
CHEMBL203845 1 -
CHEMBL202668 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL203665 RELACATIB Ki = 0.063 nM 10.20
CHEMBL286364 Ki = 1.8 nM 8.74
CHEMBL202991 Ki app - -
CHEMBL203224 Ki app - -
CHEMBL377713 Ki app - -
CHEMBL440574 Ki app - -
CHEMBL205068 Ki app - -
CHEMBL205172 Ki app - -
CHEMBL438435 Ki app - -
CHEMBL203556 Ki app - -
CHEMBL204169 Ki app - -
CHEMBL203845 Ki app - -
CHEMBL202668 Ki app - -