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Assay Detail

CHEMBL888347

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

Binding
Inhibition of humanized rabbit 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 Autocuration

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Primary amides as selective inhibitors of cathepsin K.
Léger S, Bayly CI, Black WC, Desmarais S, Falgueyret JP, Massé F, Percival MD, Truchon JF.
Bioorg Med Chem Lett (2007) 17 : 4328 -4332
PubMed 17544269 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.38 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437501 1 9.70
CHEMBL250501 1 9.70
CHEMBL399361 1 9.22
CHEMBL250294 1 9.05
CHEMBL399359 1 8.00
CHEMBL401176 1 7.89
CHEMBL427712 1 7.57
CHEMBL250904 1 7.39
CHEMBL249885 1 7.18
CHEMBL250706 1 7.17
CHEMBL249275 1 7.06
CHEMBL250089 1 6.96
CHEMBL251100 1 6.92
CHEMBL250293 1 6.82
CHEMBL249680 1 6.76
CHEMBL248902 1 6.62
CHEMBL401175 1 6.62
CHEMBL249274 1 6.56
CHEMBL249276 1 6.56
CHEMBL402267 1 5.98
CHEMBL398608 1 5.22

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437501 IC50 = 0.2 nM 9.70
CHEMBL250501 IC50 = 0.2 nM 9.70
CHEMBL399361 IC50 = 0.6 nM 9.22
CHEMBL250294 IC50 = 0.9 nM 9.05
CHEMBL399359 IC50 = 10.0 nM 8.00
CHEMBL401176 IC50 = 13.0 nM 7.89
CHEMBL427712 IC50 = 27.0 nM 7.57
CHEMBL250904 IC50 = 41.0 nM 7.39
CHEMBL249885 IC50 = 66.0 nM 7.18
CHEMBL250706 IC50 = 67.0 nM 7.17
CHEMBL249275 IC50 = 87.0 nM 7.06
CHEMBL250089 IC50 = 109.0 nM 6.96
CHEMBL251100 IC50 = 120.0 nM 6.92
CHEMBL250293 IC50 = 151.0 nM 6.82
CHEMBL249680 IC50 = 174.0 nM 6.76
CHEMBL248902 IC50 = 238.0 nM 6.62
CHEMBL401175 IC50 = 238.0 nM 6.62
CHEMBL249274 IC50 = 273.0 nM 6.56
CHEMBL249276 IC50 = 277.0 nM 6.56
CHEMBL402267 IC50 = 1045.0 nM 5.98
CHEMBL398608 IC50 = 6070.0 nM 5.22