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Assay Detail

CHEMBL911397

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

Binding
Inhibition of human recombinant cathepsin S
16
Total Activities
16
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 S (CHEMBL2954)
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 16 8.81 9.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL386506 1 9.89
CHEMBL385632 1 9.64
CHEMBL219536 1 9.32
CHEMBL384685 1 9.29
CHEMBL218024 1 9.15
CHEMBL218007 1 9.05
CHEMBL221707 1 9.05
CHEMBL220496 1 8.80
CHEMBL414530 1 8.74
CHEMBL217930 1 8.64
CHEMBL374890 1 8.60
CHEMBL436303 1 8.59
CHEMBL220760 1 8.51
CHEMBL449096 1 8.00
CHEMBL363847 1 6.82
CHEMBL374695 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL386506 IC50 = 0.13 nM 9.89
CHEMBL385632 IC50 = 0.23 nM 9.64
CHEMBL219536 IC50 = 0.48 nM 9.32
CHEMBL384685 IC50 = 0.51 nM 9.29
CHEMBL218024 IC50 = 0.7 nM 9.15
CHEMBL218007 IC50 = 0.9 nM 9.05
CHEMBL221707 IC50 = 0.9 nM 9.05
CHEMBL220496 IC50 = 1.6 nM 8.80
CHEMBL414530 IC50 = 1.8 nM 8.74
CHEMBL217930 IC50 = 2.3 nM 8.64
CHEMBL374890 IC50 = 2.5 nM 8.60
CHEMBL436303 IC50 = 2.6 nM 8.59
CHEMBL220760 IC50 = 3.1 nM 8.51
CHEMBL449096 IC50 = 10.0 nM 8.00
CHEMBL363847 IC50 = 150.0 nM 6.82
CHEMBL374695 IC50 > 10.0 nM -