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Assay Detail

CHEMBL4604710

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

Binding
Antagonist activity at alpha4beta2 nAChR (unknown origin) expressed in HEK293 cells assessed as reduction in acetylcholine-induced currents at -80 mV holding potential by whole-cell patch clamp method
1
Total Activities
1
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Discovery and Development of 3-(6-Chloropyridine-3-yloxymethyl)-2-azabicyclo[3.1.0]hexane Hydrochloride (SUVN-911): A Novel, Potent, Selective, and Orally Active Neuronal Nicotinic Acetylcholine α4β2 Receptor Antagonist for the Treatment of Depression.
Nirogi R, Mohammed AR, Shinde AK, Ravella SR, Bogaraju N, Subramanian R, Mekala VR, Palacharla RC, Muddana N, Thentu JB, Bhyrapuneni G, Abraham R, Jasti V.
J Med Chem (2020) 63 : 2833 -2853
PubMed 32026697 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 5.14 5.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4642118 1 5.14

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4642118 IC50 = 7310.0 nM 5.14