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Assay Detail

CHEMBL823511

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

Binding
Inhibition of [3H](-)-nicotine binding to recombinant rat alpha4-beta2 nAChR was determined; experiment 1
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Novel and potent 6-chloro-3-pyridinyl ligands for the alpha4beta2 neuronal nicotinic acetylcholine receptor.
Latli B, D'Amour K, Casida JE.
J Med Chem (1999) 42 : 2227 -2234
PubMed 10377228 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 5.58 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL71583 1 7.80
CHEMBL309136 1 5.76
CHEMBL539622 1 5.43
CHEMBL431760 1 4.90
CHEMBL69446 1 4.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL71583 IC50 = 16.0 nM 7.80
CHEMBL309136 IC50 = 1740.0 nM 5.76
CHEMBL539622 IC50 = 3700.0 nM 5.43
CHEMBL431760 IC50 = 12600.0 nM 4.90
CHEMBL69446 IC50 = 99500.0 nM 4.00