Assay Detail

CHEMBL4614788

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Binding

Inhibition of human serine protease factor B in human PNH patient derived sample assessed as prevention of erythrocyte lysis

ChEMBL ↗

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Target

Complement factor B (CHEMBL5731) ↗

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Complement factor B (CHEMBL5731) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Complement factor B

CHEMBL5731

Anchored from Assay target.

Protein identity Complement factor B

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Homo sapiens
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	1	6.40	6.40

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4594448	IPTACOPAN	4.0	1	6.40

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4594448	IPTACOPAN	IC50	=	400.0	nM	6.40