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Assay Detail

CHEMBL2168689

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

Functional
Antagonist activity at rat alpha7 nAChR expressed in Xenopus laevis oocytes assessed as inhibition of acetylcholine-induced response after 2 to 6 days by two electrode voltage clamp assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type Oocyte
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and nicotinic acetylcholine receptor in vitro and in vivo pharmacological properties of 2'-fluoro-3'-(substituted phenyl)deschloroepibatidine analogues of 2'-fluoro-3'-(4-nitrophenyl)deschloroepibatidine.
Ondachi P, Castro A, Luetje CW, Damaj MI, Mascarella SW, Navarro HA, Carroll FI.
J Med Chem (2012) 55 : 6512 -6522
PubMed 22742586 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 4.62 5.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2164663 1 5.40
CHEMBL2164664 1 4.72
CHEMBL361465 1 4.50
CHEMBL2164667 1 4.46
CHEMBL372638 1 4.01

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2164663 IC50 = 4000.0 nM 5.40
CHEMBL2164664 IC50 = 19000.0 nM 4.72
CHEMBL361465 IC50 = 32000.0 nM 4.50
CHEMBL2164667 IC50 = 35000.0 nM 4.46
CHEMBL372638 IC50 = 98000.0 nM 4.01