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Assay Detail

CHEMBL1021994

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

Binding
Inhibition of 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 Intermediate

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5-Aminopyrimidin-2-ylnitriles as cathepsin K inhibitors.
Morley AD, Kenny PW, Burton B, Heald RA, Macfaul PA, Mullett J, Page K, Porres SS, Ribeiro LR, Smith P, Ward S, Wilkinson TJ.
Bioorg Med Chem Lett (2009) 19 : 1658 -1661
PubMed 19231183 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 17 7.49 8.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL470915 1 8.70
CHEMBL474484 1 8.22
CHEMBL514805 1 8.05
CHEMBL472618 1 7.89
CHEMBL474829 1 7.85
CHEMBL471757 1 7.77
CHEMBL450061 1 7.75
CHEMBL471951 1 7.66
CHEMBL471584 1 7.64
CHEMBL474828 1 7.62
CHEMBL474830 1 7.50
CHEMBL470916 1 7.22
CHEMBL474831 1 7.21
CHEMBL471578 1 6.96
CHEMBL470897 1 6.52
CHEMBL446519 1 6.47
CHEMBL471579 1 6.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL470915 IC50 = 2.0 nM 8.70
CHEMBL474484 IC50 = 6.0 nM 8.22
CHEMBL514805 IC50 = 9.0 nM 8.05
CHEMBL472618 IC50 = 13.0 nM 7.89
CHEMBL474829 IC50 = 14.0 nM 7.85
CHEMBL471757 IC50 = 17.0 nM 7.77
CHEMBL450061 IC50 = 18.0 nM 7.75
CHEMBL471951 IC50 = 22.0 nM 7.66
CHEMBL471584 IC50 = 23.0 nM 7.64
CHEMBL474828 IC50 = 24.0 nM 7.62
CHEMBL474830 IC50 = 32.0 nM 7.50
CHEMBL470916 IC50 = 60.0 nM 7.22
CHEMBL474831 IC50 = 62.0 nM 7.21
CHEMBL471578 IC50 = 110.0 nM 6.96
CHEMBL470897 IC50 = 300.0 nM 6.52
CHEMBL446519 IC50 = 340.0 nM 6.47
CHEMBL471579 IC50 = 560.0 nM 6.25