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Assay Detail

CHEMBL655967

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

Binding
Inhibitory activity against C1r serine protease
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 Expert

Target

Complement C1r subcomponent (CHEMBL4611)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and evaluation of 2-aryl-4H-3,1-benzoxazin-4-ones as C1r serine protease inhibitors
Gilmore JL, Hays SJ, Caprathe BW, Lee C, Emmerling MR, Michael W, Jaen JC
Bioorg Med Chem Lett (1996) 6 : 679 -682
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 4.49 4.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273264 NAFAMOSTAT 3.0 1 4.92
CHEMBL158577 1 4.56
CHEMBL159104 1 4.40
CHEMBL158541 1 4.34
CHEMBL161460 1 4.24
CHEMBL162473 1 -
CHEMBL158925 1 -
CHEMBL161254 1 -
CHEMBL161275 1 -
CHEMBL352443 1 -
CHEMBL345362 1 -
CHEMBL346547 1 -
CHEMBL347904 1 -
CHEMBL161656 1 -
CHEMBL157987 1 -
CHEMBL349853 1 -
CHEMBL349818 1 -
CHEMBL349763 1 -
CHEMBL157862 1 -
CHEMBL158926 1 -
CHEMBL158462 1 -
CHEMBL158801 1 -
CHEMBL159105 1 -
CHEMBL157808 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273264 NAFAMOSTAT IC50 = 12000.0 nM 4.92
CHEMBL158577 IC50 = 27300.0 nM 4.56
CHEMBL159104 IC50 = 40000.0 nM 4.40
CHEMBL158541 IC50 = 46000.0 nM 4.34
CHEMBL161460 IC50 = 57000.0 nM 4.24
CHEMBL162473 IC50 > 62500.0 nM -
CHEMBL158925 IC50 > 62500.0 nM -
CHEMBL161254 IC50 > 62500.0 nM -
CHEMBL161275 IC50 > 62500.0 nM -
CHEMBL352443 IC50 > 62500.0 nM -
CHEMBL345362 IC50 > 62500.0 nM -
CHEMBL346547 IC50 > 62500.0 nM -
CHEMBL347904 IC50 > 62500.0 nM -
CHEMBL161656 IC50 > 62500.0 nM -
CHEMBL157987 IC50 > 62500.0 nM -
CHEMBL349853 IC50 > 62500.0 nM -
CHEMBL349818 IC50 > 62500.0 nM -
CHEMBL349763 IC50 > 62500.0 nM -
CHEMBL157862 IC50 > 62500.0 nM -
CHEMBL158926 IC50 > 62500.0 nM -
CHEMBL158462 IC50 > 62500.0 nM -
CHEMBL158801 IC50 > 62500.0 nM -
CHEMBL159105 IC50 > 62500.0 nM -
CHEMBL157808 IC50 > 62500.0 nM -