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Assay Detail

CHEMBL656680

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Binding
Inhibitory activity against human cathepsin K
26
Total Activities
26
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of small molecule ketoamide-based inhibitors of cathepsin K.
Catalano JG, Deaton DN, Long ST, McFadyen RB, Miller LR, Payne JA, Wells-Knecht KJ, Wright LL.
Bioorg Med Chem Lett (2004) 14 : 719 -722
PubMed 14741275 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.70 9.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL92708 CALPEPTIN 1 9.96
CHEMBL354473 1 9.15
CHEMBL163286 1 9.10
CHEMBL349045 1 8.96
CHEMBL355138 1 8.20
CHEMBL164373 1 7.70
CHEMBL162041 1 7.50
CHEMBL163185 1 7.47
CHEMBL96875 1 7.29
CHEMBL163757 1 7.16
CHEMBL351877 1 7.12
CHEMBL266851 1 6.04
CHEMBL162812 1 5.92
CHEMBL163240 1 5.85
CHEMBL162793 1 5.54
CHEMBL439649 1 5.47
CHEMBL163555 1 5.38
CHEMBL159411 1 5.30
CHEMBL159569 1 5.23
CHEMBL164535 1 5.20
CHEMBL159452 1 5.04
CHEMBL346748 1 4.75
CHEMBL159905 1 4.68
CHEMBL159869 1 -
CHEMBL84691 1 -
CHEMBL165345 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL92708 CALPEPTIN IC50 = 0.11 nM 9.96
CHEMBL354473 IC50 = 0.71 nM 9.15
CHEMBL163286 IC50 = 0.79 nM 9.10
CHEMBL349045 IC50 = 1.1 nM 8.96
CHEMBL355138 IC50 = 6.3 nM 8.20
CHEMBL164373 IC50 = 20.0 nM 7.70
CHEMBL162041 IC50 = 32.0 nM 7.50
CHEMBL163185 IC50 = 34.0 nM 7.47
CHEMBL96875 IC50 = 51.0 nM 7.29
CHEMBL163757 IC50 = 69.0 nM 7.16
CHEMBL351877 IC50 = 76.0 nM 7.12
CHEMBL266851 IC50 = 912.0 nM 6.04
CHEMBL162812 IC50 = 1200.0 nM 5.92
CHEMBL163240 IC50 = 1400.0 nM 5.85
CHEMBL162793 IC50 = 2900.0 nM 5.54
CHEMBL439649 IC50 = 3400.0 nM 5.47
CHEMBL163555 IC50 = 4200.0 nM 5.38
CHEMBL159411 IC50 = 5000.0 nM 5.30
CHEMBL159569 IC50 = 5900.0 nM 5.23
CHEMBL164535 IC50 = 6300.0 nM 5.20
CHEMBL159452 IC50 = 9100.0 nM 5.04
CHEMBL346748 IC50 = 18000.0 nM 4.75
CHEMBL159905 IC50 = 21000.0 nM 4.68
CHEMBL159869 IC50 > 100000.0 nM -
CHEMBL84691 IC50 = 2.5 nM -
CHEMBL165345 IC50 > 100000.0 nM -