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Assay Detail

CHEMBL3607132

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

Binding
Agonist activity at human alpha3beta4 nAChR expressed in rat GH4C1 cells assessed as induction of peak current amplitude at holding potential of -70 mV by whole-cell patch clamp assay
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type GH4-C1
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907594)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Chemistry and Pharmacology of a Series of Unichiral Analogues of 2-(2-Pyrrolidinyl)-1,4-benzodioxane, Prolinol Phenyl Ether, and Prolinol 3-Pyridyl Ether Designed as α4β2-Nicotinic Acetylcholine Receptor Agonists.
Bolchi C, Valoti E, Gotti C, Fasoli F, Ruggeri P, Fumagalli L, Binda M, Mucchietto V, Sciaccaluga M, Budriesi R, Fucile S, Pallavicini M.
J Med Chem (2015) 58 : 6665 -6677
PubMed 26225816 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 4 4.95 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3603929 1 5.05
CHEMBL3603931 1 5.04
CHEMBL1917231 1 4.77
CHEMBL667 ACETYLCHOLINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3603929 EC50 = 9000.0 nM 5.05
CHEMBL3603931 EC50 = 9200.0 nM 5.04
CHEMBL1917231 EC50 = 17000.0 nM 4.77
CHEMBL667 ACETYLCHOLINE EC50 = 127000.0 nM -