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Assay Detail

CHEMBL1062475

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Binding
Inhibition of cathepsin K assessed as inhibition of fluorogenic substrate cleavage
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cathepsin K (CHEMBL268)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design of selective Cathepsin inhibitors.
Bethel PA, Gerhardt S, Jones EV, Kenny PW, Karoutchi GI, Morley AD, Oldham K, Rankine N, Augustin M, Krapp S, Simader H, Steinbacher S.
Bioorg Med Chem Lett (2009) 19 : 4622 -4625
PubMed 19616430 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.22 7.20

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL550872 1 7.20
CHEMBL549791 1 7.00
CHEMBL554065 1 6.90
CHEMBL549378 1 6.90
CHEMBL562915 1 6.90
CHEMBL555122 1 6.80
CHEMBL559880 1 6.20
CHEMBL557455 1 6.00
CHEMBL564626 1 5.90
CHEMBL565079 1 5.60
CHEMBL550246 1 5.50
CHEMBL564131 1 5.50
CHEMBL562844 1 5.50
CHEMBL563471 1 5.20
CHEMBL563056 1 -
CHEMBL556434 1 -
CHEMBL556436 1 -
CHEMBL563517 1 -
CHEMBL561802 1 -
CHEMBL551533 1 -
CHEMBL550059 1 -
CHEMBL556504 1 -
CHEMBL559248 1 -
CHEMBL560736 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL550872 IC50 = 63.1 nM 7.20
CHEMBL549791 IC50 = 100.0 nM 7.00
CHEMBL554065 IC50 = 125.89 nM 6.90
CHEMBL549378 IC50 = 125.89 nM 6.90
CHEMBL562915 IC50 = 125.89 nM 6.90
CHEMBL555122 IC50 = 158.49 nM 6.80
CHEMBL559880 IC50 = 630.96 nM 6.20
CHEMBL557455 IC50 = 1000.0 nM 6.00
CHEMBL564626 IC50 = 1258.93 nM 5.90
CHEMBL565079 IC50 = 2511.89 nM 5.60
CHEMBL550246 IC50 = 3162.28 nM 5.50
CHEMBL564131 IC50 = 3162.28 nM 5.50
CHEMBL562844 IC50 = 3162.28 nM 5.50
CHEMBL563471 IC50 = 6309.57 nM 5.20
CHEMBL563056 IC50 > 10000.0 nM -
CHEMBL556434 IC50 > 10000.0 nM -
CHEMBL556436 IC50 > 6309.57 nM -
CHEMBL563517 IC50 > 10000.0 nM -
CHEMBL561802 IC50 > 10000.0 nM -
CHEMBL551533 IC50 > 7943.28 nM -
CHEMBL550059 IC50 > 7943.28 nM -
CHEMBL556504 IC50 > 10000.0 nM -
CHEMBL559248 IC50 > 10000.0 nM -
CHEMBL560736 IC50 > 10000.0 nM -