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Assay Detail

CHEMBL923076

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Binding
Inhibition of human cathepsin K
27
Total Activities
27
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The identification of potent, selective, and bioavailable cathepsin S inhibitors.
Gauthier JY, Black WC, Courchesne I, Cromlish W, Desmarais S, Houle R, Lamontagne S, Li CS, Massé F, McKay DJ, Ouellet M, Robichaud J, Truchon JF, Truong VL, Wang Q, Percival MD.
Bioorg Med Chem Lett (2007) 17 : 4929 -4933
PubMed 17590332 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 6.94 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL437501 1 9.70
CHEMBL249495 1 9.52
CHEMBL249698 1 8.30
CHEMBL248889 1 8.28
CHEMBL222649 1 8.21
CHEMBL400387 1 7.51
CHEMBL249507 1 6.85
CHEMBL251719 1 6.57
CHEMBL250720 1 6.54
CHEMBL251114 1 6.52
CHEMBL443319 1 6.50
CHEMBL250121 1 6.50
CHEMBL400972 1 6.42
CHEMBL249915 1 6.39
CHEMBL249712 1 6.26
CHEMBL436636 1 6.19
CHEMBL251117 1 6.16
CHEMBL250919 1 6.08
CHEMBL250119 1 5.95
CHEMBL251327 1 5.70
CHEMBL399063 1 5.51
CHEMBL400728 1 -
CHEMBL398553 1 -
CHEMBL400750 1 -
CHEMBL427883 1 -
CHEMBL251101 1 -
CHEMBL437579 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL437501 IC50 = 0.2 nM 9.70
CHEMBL249495 IC50 = 0.3 nM 9.52
CHEMBL249698 IC50 = 5.0 nM 8.30
CHEMBL248889 IC50 = 5.3 nM 8.28
CHEMBL222649 IC50 = 6.2 nM 8.21
CHEMBL400387 IC50 = 31.0 nM 7.51
CHEMBL249507 IC50 = 141.0 nM 6.85
CHEMBL251719 IC50 = 269.0 nM 6.57
CHEMBL250720 IC50 = 290.0 nM 6.54
CHEMBL251114 IC50 = 305.0 nM 6.52
CHEMBL443319 IC50 = 314.0 nM 6.50
CHEMBL250121 IC50 = 314.0 nM 6.50
CHEMBL400972 IC50 = 376.0 nM 6.42
CHEMBL249915 IC50 = 405.0 nM 6.39
CHEMBL249712 IC50 = 555.0 nM 6.26
CHEMBL436636 IC50 = 639.0 nM 6.19
CHEMBL251117 IC50 = 691.0 nM 6.16
CHEMBL250919 IC50 = 825.0 nM 6.08
CHEMBL250119 IC50 = 1117.0 nM 5.95
CHEMBL251327 IC50 = 2003.0 nM 5.70
CHEMBL399063 IC50 = 3058.0 nM 5.51
CHEMBL400728 IC50 > 10000.0 nM -
CHEMBL398553 IC50 > 10000.0 nM -
CHEMBL400750 IC50 > 10000.0 nM -
CHEMBL427883 IC50 > 10000.0 nM -
CHEMBL251101 IC50 > 10000.0 nM -
CHEMBL437579 IC50 > 10000.0 nM -