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Assay Detail

CHEMBL945080

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Binding
Inhibition of cathepsin B
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cathepsin B (CHEMBL4072)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

The discovery of odanacatib (MK-0822), a selective inhibitor of cathepsin K.
Gauthier JY, Chauret N, Cromlish W, Desmarais S, Duong LT, Falgueyret JP, Kimmel DB, Lamontagne S, Léger S, LeRiche T, Li CS, Massé F, McKay DJ, Nicoll-Griffith DA, Oballa RM, Palmer JT, Percival MD, Riendeau D, Robichaud J, Rodan GA, Rodan SB, Seto C, Thérien M, Truong VL, Venuti MC, Wesolowski G, Young RN, Zamboni R, Black WC.
Bioorg Med Chem Lett (2008) 18 : 923 -928
PubMed 18226527 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 14 5.99 7.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL399733 1 7.00
CHEMBL252784 1 6.36
CHEMBL399361 1 6.02
CHEMBL481611 ODANACATIB 3.0 1 5.99
CHEMBL252582 1 5.82
CHEMBL252179 1 5.46
CHEMBL437501 1 5.28
CHEMBL252571 1 -
CHEMBL398910 1 -
CHEMBL252581 1 -
CHEMBL252383 1 -
CHEMBL428417 1 -
CHEMBL252382 1 -
CHEMBL250294 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL399733 IC50 = 100.0 nM 7.00
CHEMBL252784 IC50 = 434.0 nM 6.36
CHEMBL399361 IC50 = 953.0 nM 6.02
CHEMBL481611 ODANACATIB IC50 = 1034.0 nM 5.99
CHEMBL252582 IC50 = 1528.0 nM 5.82
CHEMBL252179 IC50 = 3453.0 nM 5.46
CHEMBL437501 IC50 = 5239.0 nM 5.28
CHEMBL252571 IC50 > 10000.0 nM -
CHEMBL398910 IC50 > 10000.0 nM -
CHEMBL252581 IC50 > 10000.0 nM -
CHEMBL252383 IC50 > 10000.0 nM -
CHEMBL428417 IC50 > 10000.0 nM -
CHEMBL252382 IC50 > 10000.0 nM -
CHEMBL250294 IC50 > 10000.0 nM -