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Assay Detail

CHEMBL867845

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

Functional
Agonist activity at rat alpha-4-beta-2 nACHR by rubidium efflux assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
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

Synthesis and pharmacological evaluation of novel 9- and 10-substituted cytisine derivatives. Nicotinic ligands of enhanced subtype selectivity.
Chellappan SK, Xiao Y, Tueckmantel W, Kellar KJ, Kozikowski AP.
J Med Chem (2006) 49 : 2673 -2676
PubMed 16640326 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.45 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL205644 1 5.89
CHEMBL3 NICOTINE 4.0 1 5.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL205644 EC50 = 1300.0 nM 5.89
CHEMBL3 NICOTINE EC50 = 10000.0 nM 5.00