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Assay Detail

CHEMBL655965

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Binding
Inhibition of C1r serine protease
14
Total Activities
14
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 14 5.30 6.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158926 1 6.16
CHEMBL273264 NAFAMOSTAT 3.0 1 6.00
CHEMBL157862 1 5.77
CHEMBL158577 1 5.52
CHEMBL161460 1 5.52
CHEMBL352443 1 5.38
CHEMBL157987 1 5.30
CHEMBL159104 1 5.22
CHEMBL162473 1 5.12
CHEMBL158541 1 5.02
CHEMBL158925 1 5.00
CHEMBL161656 1 4.92
CHEMBL158462 1 4.76
CHEMBL161254 1 4.44

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158926 IC50 = 700.0 nM 6.16
CHEMBL273264 NAFAMOSTAT IC50 = 1000.0 nM 6.00
CHEMBL157862 IC50 = 1700.0 nM 5.77
CHEMBL158577 IC50 = 3000.0 nM 5.52
CHEMBL161460 IC50 = 3000.0 nM 5.52
CHEMBL352443 IC50 = 4200.0 nM 5.38
CHEMBL157987 IC50 = 5000.0 nM 5.30
CHEMBL159104 IC50 = 6000.0 nM 5.22
CHEMBL162473 IC50 = 7500.0 nM 5.12
CHEMBL158541 IC50 = 9500.0 nM 5.02
CHEMBL158925 IC50 = 10000.0 nM 5.00
CHEMBL161656 IC50 = 12100.0 nM 4.92
CHEMBL158462 IC50 = 17300.0 nM 4.76
CHEMBL161254 IC50 = 36300.0 nM 4.44