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Assay Detail

CHEMBL660761

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Binding
Inhibitory activity against human cysteine protease, cathepsin K.
29
Total Activities
29
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

Solid-phase synthesis of cyclic alkoxyketones, inhibitors of the cysteine protease cathepsin K.
Fenwick AE, Garnier B, Gribble AD, Ife RJ, Rawlings AD, Witherington J.
Bioorg Med Chem Lett (2001) 11 : 195 -198
PubMed 11206457 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 29 7.02 7.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL292106 1 7.96
CHEMBL61051 1 7.82
CHEMBL58814 1 7.72
CHEMBL61826 1 7.42
CHEMBL62239 1 7.36
CHEMBL300347 1 7.28
CHEMBL301683 1 7.22
CHEMBL59115 1 7.21
CHEMBL60427 1 7.19
CHEMBL61805 1 6.85
CHEMBL58567 1 6.75
CHEMBL62014 1 6.72
CHEMBL59170 1 6.38
CHEMBL61482 1 6.19
CHEMBL59738 1 6.15
CHEMBL291628 1 6.09
CHEMBL58236 1 -
CHEMBL62042 1 -
CHEMBL59454 1 -
CHEMBL60898 1 -
CHEMBL61333 1 -
CHEMBL58166 1 -
CHEMBL58349 1 -
CHEMBL418645 1 -
CHEMBL301232 1 -
CHEMBL61730 1 -
CHEMBL294569 1 -
CHEMBL61758 1 -
CHEMBL61797 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL292106 Ki = 11.0 nM 7.96
CHEMBL61051 Ki = 15.0 nM 7.82
CHEMBL58814 Ki = 19.0 nM 7.72
CHEMBL61826 Ki = 38.0 nM 7.42
CHEMBL62239 Ki = 44.0 nM 7.36
CHEMBL300347 Ki = 53.0 nM 7.28
CHEMBL301683 Ki = 60.0 nM 7.22
CHEMBL59115 Ki = 61.0 nM 7.21
CHEMBL60427 Ki = 64.0 nM 7.19
CHEMBL61805 Ki = 140.0 nM 6.85
CHEMBL58567 Ki = 180.0 nM 6.75
CHEMBL62014 Ki = 190.0 nM 6.72
CHEMBL59170 Ki = 420.0 nM 6.38
CHEMBL61482 Ki = 640.0 nM 6.19
CHEMBL59738 Ki = 710.0 nM 6.15
CHEMBL291628 Ki = 820.0 nM 6.09
CHEMBL58236 Ki > 10000.0 nM -
CHEMBL62042 Ki > 1000.0 nM -
CHEMBL59454 Ki > 10000.0 nM -
CHEMBL60898 Ki > 10000.0 nM -
CHEMBL61333 Ki > 1000.0 nM -
CHEMBL58166 Ki > 10000.0 nM -
CHEMBL58349 Ki > 10000.0 nM -
CHEMBL418645 Ki > 10000.0 nM -
CHEMBL301232 Ki > 10000.0 nM -
CHEMBL61730 Ki > 10000.0 nM -
CHEMBL294569 Ki > 10000.0 nM -
CHEMBL61758 Ki > 10000.0 nM -
CHEMBL61797 Ki > 1000.0 nM -