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Assay Detail

CHEMBL663348

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
In vitro inhibitory activity against human cathepsin L, using 2 uM of Z -Leu-Arg-AMC as substrate
39
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Procathepsin L (CHEMBL3837)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

A novel class of nonpeptidic biaryl inhibitors of human cathepsin K.
Robichaud J, Oballa R, Prasit P, Falgueyret JP, Percival MD, Wesolowski G, Rodan SB, Kimmel D, Johnson C, Bryant C, Venkatraman S, Setti E, Mendonca R, Palmer JT.
J Med Chem (2003) 46 : 3709 -3727
PubMed 12904076 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 39 5.71 7.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122513 1 7.38
CHEMBL123291 1 6.85
CHEMBL122812 2 6.47
CHEMBL122764 1 6.30
CHEMBL121807 1 6.08
CHEMBL333716 1 6.04
CHEMBL124159 1 5.80
CHEMBL123199 1 5.78
CHEMBL123037 1 5.77
CHEMBL123200 1 5.67
CHEMBL334074 1 5.65
CHEMBL122318 1 5.57
CHEMBL123038 1 5.56
CHEMBL184514 1 5.43
CHEMBL332776 1 5.41
CHEMBL123227 1 5.33
CHEMBL122149 1 5.32
CHEMBL122424 1 5.25
CHEMBL125656 1 5.24
CHEMBL123592 1 5.22
CHEMBL2111806 1 5.20
CHEMBL126152 1 5.08
CHEMBL122879 1 5.02
CHEMBL333987 1 -
CHEMBL123987 1 -
CHEMBL123178 1 -
CHEMBL122043 1 -
CHEMBL122672 1 -
CHEMBL122561 1 -
CHEMBL333413 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122513 IC50 = 42.0 nM 7.38
CHEMBL123291 IC50 = 140.0 nM 6.85
CHEMBL122812 IC50 = 338.0 nM 6.47
CHEMBL122764 IC50 = 498.0 nM 6.30
CHEMBL121807 IC50 = 825.0 nM 6.08
CHEMBL333716 IC50 = 919.0 nM 6.04
CHEMBL124159 IC50 = 1593.0 nM 5.80
CHEMBL123199 IC50 = 1667.0 nM 5.78
CHEMBL123037 IC50 = 1682.0 nM 5.77
CHEMBL123200 IC50 = 2163.0 nM 5.67
CHEMBL334074 IC50 = 2235.0 nM 5.65
CHEMBL122318 IC50 = 2710.0 nM 5.57
CHEMBL123038 IC50 = 2755.0 nM 5.56
CHEMBL184514 IC50 = 3725.0 nM 5.43
CHEMBL332776 IC50 = 3907.0 nM 5.41
CHEMBL123227 IC50 = 4641.0 nM 5.33
CHEMBL122149 IC50 = 4804.0 nM 5.32
CHEMBL122424 IC50 = 5583.0 nM 5.25
CHEMBL125656 IC50 = 5783.0 nM 5.24
CHEMBL123592 IC50 = 5952.0 nM 5.22
CHEMBL2111806 IC50 = 6273.0 nM 5.20
CHEMBL126152 IC50 = 8391.0 nM 5.08
CHEMBL122879 IC50 = 9546.0 nM 5.02
CHEMBL122350 IC50 > 10000.0 nM -
CHEMBL331422 IC50 > 10000.0 nM -
CHEMBL123754 IC50 > 10000.0 nM -
CHEMBL122324 IC50 > 10000.0 nM -
CHEMBL126210 IC50 > 10000.0 nM -
CHEMBL121801 IC50 > 10000.0 nM -
CHEMBL122431 IC50 > 10000.0 nM -
CHEMBL421457 IC50 > 10000.0 nM -
CHEMBL333413 IC50 > 10000.0 nM -
CHEMBL122561 IC50 > 10000.0 nM -
CHEMBL122672 IC50 > 10000.0 nM -
CHEMBL122043 IC50 > 10000.0 nM -
CHEMBL123178 IC50 > 10000.0 nM -
CHEMBL123987 IC50 > 10000.0 nM -
CHEMBL122812 IC50 > 10000.0 nM -
CHEMBL333987 IC50 > 10000.0 nM -