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Assay Detail

CHEMBL660762

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Binding
Inhibitory activity against recombinant human cathepsin K
14
Total Activities
14
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

(4-Piperidinylphenyl)aminoethyl amides as a novel class of non-covalent cathepsin K inhibitors.
Kim TS, Hague AB, Lee TI, Lian B, Tegley CM, Wang X, Burgess TL, Qian YX, Ross S, Tagari P, Lin CH, Mayeda C, Dao J, Jordan S, Mohr C, Cheetham J, Viswanadhan V, Tasker AS.
Bioorg Med Chem Lett (2004) 14 : 87 -90
PubMed 14684304 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 7.76 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL169448 1 8.52
CHEMBL172456 1 8.52
CHEMBL171403 1 8.40
CHEMBL354439 1 8.30
CHEMBL169560 1 8.10
CHEMBL353633 1 8.05
CHEMBL353725 1 8.00
CHEMBL170962 1 7.92
CHEMBL169708 1 7.85
CHEMBL170242 1 7.82
CHEMBL354132 1 7.32
CHEMBL171998 1 6.15
CHEMBL423447 1 5.96
CHEMBL170814 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL169448 Ki = 3.0 nM 8.52
CHEMBL172456 Ki = 3.0 nM 8.52
CHEMBL171403 Ki = 4.0 nM 8.40
CHEMBL354439 Ki = 5.0 nM 8.30
CHEMBL169560 Ki = 8.0 nM 8.10
CHEMBL353633 Ki = 9.0 nM 8.05
CHEMBL353725 Ki = 10.0 nM 8.00
CHEMBL170962 Ki = 12.0 nM 7.92
CHEMBL169708 Ki = 14.0 nM 7.85
CHEMBL170242 Ki = 15.0 nM 7.82
CHEMBL354132 Ki = 48.0 nM 7.32
CHEMBL171998 Ki = 706.0 nM 6.15
CHEMBL423447 Ki = 1100.0 nM 5.96
CHEMBL170814 Ki > 10000.0 nM -