Assay Detail

CHEMBL4614750

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Binding

Inhibition of adrenergic receptor alpha2c (unknown origin)

ChEMBL ↗

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Target

Alpha-2C adrenergic receptor (CHEMBL1916) ↗

Open DB target context

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Alpha-2C adrenergic receptor (CHEMBL1916) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target Alpha-2C adrenergic receptor

CHEMBL1916

Anchored from Assay target.

Protein identity Alpha-2C adrenergic receptor

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

Alpha-2C adrenergic receptor (CHEMBL1916) ↗

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	3	5.78	6.75

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL4636550	—	—	1	6.75
CHEMBL4634827	—	—	1	4.80
CHEMBL4644994	—	—	1	-

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL4636550	—	IC50	=	180.0	nM	6.75
CHEMBL4634827	—	IC50	=	16000.0	nM	4.80
CHEMBL4644994	—	IC50	>	30000.0	nM	-