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Assay Detail

CHEMBL839667

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Binding
Inhibition constant against human cathepsin K in fluorescence assay using Cbz-Phe-Arg-AMC
17
Total Activities
17
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

Acyclic cyanamide-based inhibitors of cathepsin K.
Barrett DG, Deaton DN, Hassell AM, McFadyen RB, Miller AB, Miller LR, Payne JA, Shewchuk LM, Willard DH, Wright LL.
Bioorg Med Chem Lett (2005) 15 : 3039 -3043
PubMed 15896958 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.33 10.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL371420 1 10.72
CHEMBL191558 1 10.49
CHEMBL189149 1 7.58
CHEMBL362925 1 7.21
CHEMBL370529 1 6.08
CHEMBL192604 1 5.82
CHEMBL189842 1 5.64
CHEMBL191367 1 5.10
CHEMBL433967 1 -
CHEMBL190063 1 -
CHEMBL192995 1 -
CHEMBL193095 1 -
CHEMBL190831 1 -
CHEMBL190544 1 -
CHEMBL190121 1 -
CHEMBL190864 1 -
CHEMBL189891 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL371420 Ki = 0.019 nM 10.72
CHEMBL191558 Ki = 0.032 nM 10.49
CHEMBL189149 Ki = 26.0 nM 7.58
CHEMBL362925 Ki = 62.0 nM 7.21
CHEMBL370529 Ki = 830.0 nM 6.08
CHEMBL192604 Ki = 1500.0 nM 5.82
CHEMBL189842 Ki = 2300.0 nM 5.64
CHEMBL191367 Ki = 7900.0 nM 5.10
CHEMBL433967 Ki = 0.006 nM -
CHEMBL190063 Ki = 0.007 nM -
CHEMBL192995 Ki = 0.004 nM -
CHEMBL193095 Ki = 0.004 nM -
CHEMBL190831 Ki > 13000.0 nM -
CHEMBL190544 Ki = 0.003 nM -
CHEMBL190121 Ki = 0.009 nM -
CHEMBL190864 Ki > 13000.0 nM -
CHEMBL189891 Ki > 13000.0 nM -