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Assay Detail

CHEMBL911395

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

Binding
Inhibition of human recombinant cathepsin K
21
Total Activities
21
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

2-Cyano-pyrimidines: a new chemotype for inhibitors of the cysteine protease cathepsin K.
Altmann E, Aichholz R, Betschart C, Buhl T, Green J, Irie O, Teno N, Lattmann R, Tintelnot-Blomley M, Missbach M.
J Med Chem (2007) 50 : 591 -594
PubMed 17256925 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 9.46 11.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386506 1 11.00
CHEMBL374890 1 10.96
CHEMBL414530 1 10.96
CHEMBL449096 1 10.89
CHEMBL218024 1 10.66
CHEMBL220760 1 10.60
CHEMBL436303 1 10.51
CHEMBL219536 1 10.33
CHEMBL374695 1 9.52
CHEMBL217930 1 9.12
CHEMBL363847 1 8.22
CHEMBL221804 1 6.92
CHEMBL221591 1 6.77
CHEMBL218522 1 6.00
CHEMBL220496 1 -
CHEMBL385632 1 -
CHEMBL221707 1 -
CHEMBL218007 1 -
CHEMBL218685 1 -
CHEMBL218684 1 -
CHEMBL384685 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386506 IC50 = 0.01 nM 11.00
CHEMBL374890 IC50 = 0.011 nM 10.96
CHEMBL414530 IC50 = 0.011 nM 10.96
CHEMBL449096 IC50 = 0.013 nM 10.89
CHEMBL218024 IC50 = 0.022 nM 10.66
CHEMBL220760 IC50 = 0.025 nM 10.60
CHEMBL436303 IC50 = 0.031 nM 10.51
CHEMBL219536 IC50 = 0.047 nM 10.33
CHEMBL374695 IC50 = 0.3 nM 9.52
CHEMBL217930 IC50 = 0.75 nM 9.12
CHEMBL363847 IC50 = 6.0 nM 8.22
CHEMBL221804 IC50 = 120.0 nM 6.92
CHEMBL221591 IC50 = 170.0 nM 6.77
CHEMBL218522 IC50 = 1000.0 nM 6.00
CHEMBL220496 IC50 < 0.003 nM -
CHEMBL385632 IC50 = 0.009 nM -
CHEMBL221707 IC50 < 0.003 nM -
CHEMBL218007 IC50 = 0.003 nM -
CHEMBL218685 IC50 > 1000.0 nM -
CHEMBL218684 IC50 > 1000.0 nM -
CHEMBL384685 IC50 = 0.003 nM -