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Assay Detail

CHEMBL663318

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Binding
In vitro inhibition of human Cathepsin K.
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Cyclic ketone inhibitors of the cysteine protease cathepsin K.
Marquis RW, Ru Y, Zeng J, Trout RE, LoCastro SM, Gribble AD, Witherington J, Fenwick AE, Garnier B, Tomaszek T, Tew D, Hemling ME, Quinn CJ, Smith WW, Zhao B, McQueney MS, Janson CA, D'Alessio K, Veber DF.
J Med Chem (2001) 44 : 725 -736
PubMed 11262083 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.64 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL348842 1 9.22
CHEMBL350591 1 8.80
CHEMBL162175 1 8.72
CHEMBL100563 1 8.64
CHEMBL118449 1 8.59
CHEMBL62239 1 7.36
CHEMBL301683 1 7.22
CHEMBL2371402 1 7.11
CHEMBL61805 1 6.85
CHEMBL162631 1 6.82
CHEMBL423995 1 6.75
CHEMBL163592 1 6.64
CHEMBL349445 1 6.60
CHEMBL349823 1 -
CHEMBL436437 1 -
CHEMBL162389 1 -
CHEMBL161964 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL348842 Ki = 0.6 nM 9.22
CHEMBL350591 Ki = 1.6 nM 8.80
CHEMBL162175 Ki = 1.9 nM 8.72
CHEMBL100563 Ki = 2.3 nM 8.64
CHEMBL118449 Ki = 2.6 nM 8.59
CHEMBL62239 Ki = 44.0 nM 7.36
CHEMBL301683 Ki = 60.0 nM 7.22
CHEMBL2371402 Ki = 77.0 nM 7.11
CHEMBL61805 Ki = 140.0 nM 6.85
CHEMBL162631 Ki = 150.0 nM 6.82
CHEMBL423995 Ki = 180.0 nM 6.75
CHEMBL163592 Ki = 230.0 nM 6.64
CHEMBL349445 Ki = 250.0 nM 6.60
CHEMBL349823 Ki > 10000.0 nM -
CHEMBL436437 Ki > 1000.0 nM -
CHEMBL162389 Ki > 10000.0 nM -
CHEMBL161964 Ki > 1000.0 nM -