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Assay Detail

CHEMBL4614753

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

Binding
Inhibition of serine protease factor B in 50% human whole blood assessed as reduction in alternative pathway-mediated membrane attack complex formation pre-incubated for 15 mins before activated zymosan A stimulation for 50 mins by ELISA
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Complement factor B (CHEMBL5731)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of 4-((2S,4S)-4-Ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoic Acid (LNP023), a Factor B Inhibitor Specifically Designed To Be Applicable to Treating a Diverse Array of Complement Mediated Diseases.
Mainolfi N, Ehara T, Karki RG, Anderson K, Mac Sweeney A, Liao SM, Argikar UA, Jendza K, Zhang C, Powers J, Klosowski DW, Crowley M, Kawanami T, Ding J, April M, Forster C, Serrano-Wu M, Capparelli M, Ramqaj R, Solovay C, Cumin F, Smith TM, Ferrara L, Lee W, Long D, Prentiss M, De Erkenez A, Yang L, Liu F, Sellner H, Sirockin F, Valeur E, Erbel P, Ostermeier D, Ramage P, Gerhartz B, Schubart A, Flohr S, Gradoux N, Feifel R, Vogg B, Wiesmann C, Maibaum J, Eder J, Sedrani R, Harrison RA, Mogi M, Jaffee BD, Adams CM.
J Med Chem (2020) 63 : 5697 -5722
PubMed 32073845 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 7 6.78 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4644208 1 6.96
CHEMBL4594448 IPTACOPAN 4.0 1 6.89
CHEMBL4639592 1 6.85
CHEMBL4646504 1 6.82
CHEMBL4632794 1 6.75
CHEMBL4641109 1 6.62
CHEMBL4644994 1 6.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4644208 IC50 = 110.0 nM 6.96
CHEMBL4594448 IPTACOPAN IC50 = 130.0 nM 6.89
CHEMBL4639592 IC50 = 140.0 nM 6.85
CHEMBL4646504 IC50 = 150.0 nM 6.82
CHEMBL4632794 IC50 = 180.0 nM 6.75
CHEMBL4641109 IC50 = 240.0 nM 6.62
CHEMBL4644994 IC50 = 250.0 nM 6.60