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Assay Detail

CHEMBL1119418

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Binding
Inhibition of human recombinant cathepsin S expressed in Escherichia coli BL21 (DE3) after 10 mins by fluorescence assay
32
Total Activities
32
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Cathepsin S (CHEMBL2954)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design and synthesis of alpha-ketoamides as cathepsin S inhibitors with potential applications against tumor invasion and angiogenesis.
Chen JC, Uang BJ, Lyu PC, Chang JY, Liu KJ, Kuo CC, Hsieh HP, Wang HC, Cheng CS, Chang YH, Chang MD, Chang WS, Lin CC.
J Med Chem (2010) 53 : 4545 -4549
PubMed 20481438 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 32 8.18 8.72

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1086235 1 8.72
CHEMBL1085728 1 8.70
CHEMBL1085970 1 8.68
CHEMBL1083620 1 8.64
CHEMBL1085726 1 8.51
CHEMBL1083930 1 8.47
CHEMBL1083919 1 8.44
CHEMBL1085729 1 8.42
CHEMBL1085966 1 8.37
CHEMBL1083318 1 8.36
CHEMBL347111 1 8.26
CHEMBL1085974 1 8.25
CHEMBL1085969 1 8.24
CHEMBL1085982 1 8.24
CHEMBL1085976 1 8.23
CHEMBL1085980 1 8.21
CHEMBL1085975 1 8.21
CHEMBL1085979 1 8.21
CHEMBL1085730 1 8.18
CHEMBL1085983 1 8.15
CHEMBL1083923 1 8.14
CHEMBL1085727 1 8.10
CHEMBL1085971 1 8.06
CHEMBL1085731 1 7.99
CHEMBL1085977 1 7.94
CHEMBL1085968 1 7.80
CHEMBL1085984 1 7.64
CHEMBL1085978 1 7.62
CHEMBL1085981 1 7.37
CHEMBL1085967 1 7.31

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1086235 IC50 = 1.9 nM 8.72
CHEMBL1085728 IC50 = 2.0 nM 8.70
CHEMBL1085970 IC50 = 2.1 nM 8.68
CHEMBL1083620 IC50 = 2.3 nM 8.64
CHEMBL1085726 IC50 = 3.1 nM 8.51
CHEMBL1083930 IC50 = 3.4 nM 8.47
CHEMBL1083919 IC50 = 3.6 nM 8.44
CHEMBL1085729 IC50 = 3.8 nM 8.42
CHEMBL1085966 IC50 = 4.3 nM 8.37
CHEMBL1083318 IC50 = 4.4 nM 8.36
CHEMBL347111 IC50 = 5.5 nM 8.26
CHEMBL1085974 IC50 = 5.6 nM 8.25
CHEMBL1085969 IC50 = 5.8 nM 8.24
CHEMBL1085982 IC50 = 5.7 nM 8.24
CHEMBL1085976 IC50 = 5.9 nM 8.23
CHEMBL1085975 IC50 = 6.2 nM 8.21
CHEMBL1085979 IC50 = 6.2 nM 8.21
CHEMBL1085980 IC50 = 6.1 nM 8.21
CHEMBL1085730 IC50 = 6.6 nM 8.18
CHEMBL1085983 IC50 = 7.1 nM 8.15
CHEMBL1083923 IC50 = 7.2 nM 8.14
CHEMBL1085727 IC50 = 8.0 nM 8.10
CHEMBL1085971 IC50 = 8.8 nM 8.06
CHEMBL1085731 IC50 = 10.3 nM 7.99
CHEMBL1085977 IC50 = 11.5 nM 7.94
CHEMBL1085968 IC50 = 15.7 nM 7.80
CHEMBL1085984 IC50 = 22.8 nM 7.64
CHEMBL1085978 IC50 = 23.8 nM 7.62
CHEMBL1085981 IC50 = 42.3 nM 7.37
CHEMBL1085967 IC50 = 49.2 nM 7.31
CHEMBL1085973 IC50 > 100.0 nM -
CHEMBL1085972 IC50 > 100.0 nM -