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Assay Detail

CHEMBL820317

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

Binding
Inhibition of Human cathepsin K
15
Total Activities
15
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

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Azepanone-based inhibitors of human and rat cathepsin K.
Marquis RW, Ru Y, LoCastro SM, Zeng J, Yamashita DS, Oh HJ, Erhard KF, Davis LD, Tomaszek TA, Tew D, Salyers K, Proksch J, Ward K, Smith B, Levy M, Cummings MD, Haltiwanger RC, Trescher G, Wang B, Hemling ME, Quinn CJ, Cheng HY, Lin F, Smith WW, Janson CA, Zhao B, McQueney MS, D'Alessio K, Lee CP, Marzulli A, Dodds RA, Blake S, Hwang SM, James IE, Gress CJ, Bradley BR, Lark MW, Gowen M, Veber DF.
J Med Chem (2001) 44 : 1380 -1395
PubMed 11311061 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 15 7.96 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL286364 1 9.80
CHEMBL31381 1 8.80
CHEMBL31947 1 8.70
CHEMBL29483 1 8.64
CHEMBL281086 1 8.59
CHEMBL31218 1 8.33
CHEMBL31545 1 8.12
CHEMBL286034 1 7.82
CHEMBL281540 1 7.66
CHEMBL31519 1 7.52
CHEMBL418213 1 7.27
CHEMBL416579 1 6.17
CHEMBL31674 1 6.01
CHEMBL287705 1 -
CHEMBL284939 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL286364 Ki = 0.16 nM 9.80
CHEMBL31381 Ki = 1.6 nM 8.80
CHEMBL31947 Ki = 2.0 nM 8.70
CHEMBL29483 Ki = 2.3 nM 8.64
CHEMBL281086 Ki = 2.6 nM 8.59
CHEMBL31218 Ki = 4.7 nM 8.33
CHEMBL31545 Ki = 7.5 nM 8.12
CHEMBL286034 Ki = 15.0 nM 7.82
CHEMBL281540 Ki = 22.0 nM 7.66
CHEMBL31519 Ki = 30.0 nM 7.52
CHEMBL418213 Ki = 54.0 nM 7.27
CHEMBL416579 Ki = 670.0 nM 6.17
CHEMBL31674 Ki = 980.0 nM 6.01
CHEMBL287705 Ki > 1000.0 nM -
CHEMBL284939 Ki = 0.0048 nM -