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Assay Detail

CHEMBL4614752

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

Binding
Inhibition of human serine protease factor B by TR-FRET based competition binding assay
21
Total Activities
16
Compounds Tested
1
Activity Types
0
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 21 6.35 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4639592 1 8.22
CHEMBL4594448 IPTACOPAN 4.0 1 7.92
CHEMBL4641109 1 7.75
CHEMBL4632794 1 7.75
CHEMBL4644208 1 7.75
CHEMBL4646504 1 7.62
CHEMBL4644994 3 7.48
CHEMBL4646691 2 5.60
CHEMBL4645710 1 4.92
CHEMBL4645336 1 4.57
CHEMBL4635047 2 4.44
CHEMBL4633437 2 4.17
CHEMBL4646654 1 -
CHEMBL4644769 1 -
CHEMBL4636577 1 -
CHEMBL4647418 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4639592 IC50 = 6.0 nM 8.22
CHEMBL4594448 IPTACOPAN IC50 = 12.0 nM 7.92
CHEMBL4644208 IC50 = 18.0 nM 7.75
CHEMBL4632794 IC50 = 18.0 nM 7.75
CHEMBL4641109 IC50 = 18.0 nM 7.75
CHEMBL4646504 IC50 = 24.0 nM 7.62
CHEMBL4644994 IC50 = 33.0 nM 7.48
CHEMBL4644994 IC50 = 62.0 nM 7.21
CHEMBL4646691 IC50 = 2500.0 nM 5.60
CHEMBL4646691 IC50 = 7300.0 nM 5.14
CHEMBL4645710 IC50 = 12000.0 nM 4.92
CHEMBL4644994 IC50 = 17000.0 nM 4.77
CHEMBL4645336 IC50 = 27000.0 nM 4.57
CHEMBL4635047 IC50 = 36000.0 nM 4.44
CHEMBL4633437 IC50 = 68000.0 nM 4.17
CHEMBL4647418 IC50 = 710.0 nM -
CHEMBL4636577 IC50 = 1300.0 nM -
CHEMBL4644769 IC50 > 100000.0 nM -
CHEMBL4633437 IC50 = 720.0 nM -
CHEMBL4635047 IC50 = 6800.0 nM -
CHEMBL4646654 IC50 > 100000.0 nM -