Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL4614746

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

Binding
Inhibition of human serine protease factor B catalytic domain (D470 to L764 residues) assessed as inhibition of cleavage cobra venom factor (CVF):Bb complex pre-incubated for 1 hr before addition of C3 by ELISA
26
Total Activities
24
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 26 5.03 5.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4633437 2 5.85
CHEMBL4634827 1 5.47
CHEMBL4638836 1 5.23
CHEMBL4638349 2 5.22
CHEMBL4647985 1 5.20
CHEMBL4636550 1 5.18
CHEMBL4638325 1 5.18
CHEMBL4637130 1 5.17
CHEMBL4637156 1 5.10
CHEMBL4643155 1 5.06
CHEMBL4633534 1 4.96
CHEMBL4646654 1 4.85
CHEMBL4636547 1 4.48
CHEMBL4636124 1 4.30
CHEMBL4648708 1 4.19
CHEMBL4645983 1 -
CHEMBL4642825 1 -
CHEMBL4638117 1 -
CHEMBL4644797 1 -
CHEMBL4635101 1 -
CHEMBL4638538 1 -
CHEMBL4646117 1 -
CHEMBL4641221 1 -
CHEMBL4638143 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4633437 IC50 = 1400.0 nM 5.85
CHEMBL4634827 IC50 = 3350.0 nM 5.47
CHEMBL4638836 IC50 = 5900.0 nM 5.23
CHEMBL4638349 IC50 = 6000.0 nM 5.22
CHEMBL4647985 IC50 = 6300.0 nM 5.20
CHEMBL4636550 IC50 = 6600.0 nM 5.18
CHEMBL4638325 IC50 = 6600.0 nM 5.18
CHEMBL4637130 IC50 = 6700.0 nM 5.17
CHEMBL4637156 IC50 = 8000.0 nM 5.10
CHEMBL4643155 IC50 = 8800.0 nM 5.06
CHEMBL4633534 IC50 = 11000.0 nM 4.96
CHEMBL4633437 IC50 = 11000.0 nM 4.96
CHEMBL4646654 IC50 = 14000.0 nM 4.85
CHEMBL4636547 IC50 = 33000.0 nM 4.48
CHEMBL4636124 IC50 = 50000.0 nM 4.30
CHEMBL4648708 IC50 = 65000.0 nM 4.19
CHEMBL4642825 IC50 > 100000.0 nM -
CHEMBL4638117 IC50 > 100000.0 nM -
CHEMBL4645983 IC50 > 100000.0 nM -
CHEMBL4644797 IC50 > 100000.0 nM -
CHEMBL4635101 IC50 > 100000.0 nM -
CHEMBL4638538 IC50 > 100000.0 nM -
CHEMBL4646117 IC50 > 100000.0 nM -
CHEMBL4638349 IC50 > 100000.0 nM -
CHEMBL4641221 IC50 > 100000.0 nM -
CHEMBL4638143 IC50 > 100000.0 nM -