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Assay Detail

CHEMBL1058864

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Binding
Inhibition of cathepsin K
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

Dipeptidyl nitrile inhibitors of Cathepsin L.
Asaad N, Bethel PA, Coulson MD, Dawson JE, Ford SJ, Gerhardt S, Grist M, Hamlin GA, James MJ, Jones EV, Karoutchi GI, Kenny PW, Morley AD, Oldham K, Rankine N, Ryan D, Wells SL, Wood L, Augustin M, Krapp S, Simader H, Steinbacher S.
Bioorg Med Chem Lett (2009) 19 : 4280 -4283
PubMed 19515558 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 5.41 5.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL560785 1 5.90
CHEMBL551060 1 5.90
CHEMBL562462 1 5.70
CHEMBL565079 1 5.60
CHEMBL556421 1 5.60
CHEMBL550246 1 5.50
CHEMBL564131 1 5.50
CHEMBL572332 1 5.30
CHEMBL550247 1 5.30
CHEMBL559238 1 5.30
CHEMBL563886 1 5.30
CHEMBL561586 1 5.30
CHEMBL561927 1 5.20
CHEMBL551059 1 5.20
CHEMBL560786 1 5.20
CHEMBL551805 1 5.20
CHEMBL563522 1 5.00
CHEMBL556217 1 -
CHEMBL549365 1 -
CHEMBL552001 1 -
CHEMBL551121 1 -
CHEMBL562325 1 -
CHEMBL561725 1 -
CHEMBL557920 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL560785 IC50 = 1258.93 nM 5.90
CHEMBL551060 IC50 = 1258.93 nM 5.90
CHEMBL562462 IC50 = 1995.26 nM 5.70
CHEMBL565079 IC50 = 2511.89 nM 5.60
CHEMBL556421 IC50 = 2511.89 nM 5.60
CHEMBL550246 IC50 = 3162.28 nM 5.50
CHEMBL564131 IC50 = 3162.28 nM 5.50
CHEMBL572332 IC50 = 5011.87 nM 5.30
CHEMBL550247 IC50 = 5011.87 nM 5.30
CHEMBL559238 IC50 = 5011.87 nM 5.30
CHEMBL563886 IC50 = 5011.87 nM 5.30
CHEMBL561586 IC50 = 5011.87 nM 5.30
CHEMBL561927 IC50 = 6309.57 nM 5.20
CHEMBL551059 IC50 = 6309.57 nM 5.20
CHEMBL560786 IC50 = 6309.57 nM 5.20
CHEMBL551805 IC50 = 6309.57 nM 5.20
CHEMBL563522 IC50 = 10000.0 nM 5.00
CHEMBL556217 IC50 > 10000.0 nM -
CHEMBL549365 IC50 > 10000.0 nM -
CHEMBL552001 IC50 > 10000.0 nM -
CHEMBL551121 IC50 > 10000.0 nM -
CHEMBL562325 IC50 > 10000.0 nM -
CHEMBL561725 IC50 > 10000.0 nM -
CHEMBL557920 IC50 > 10000.0 nM -