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Assay Detail

CHEMBL752538

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Binding
Binding affinity towards rat Nicotinic acetylcholine receptor alpha3-beta2 expressed in HEK293 cells using [3H]EB as radioligand
10
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuronal acetylcholine receptor; alpha3/beta2 (CHEMBL1907587)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Pharmacology of the agonist binding sites of rat neuronal nicotinic receptor subtypes expressed in HEK 293 cells.
Xiao Y, Baydyuk M, Wang HP, Davis HE, Kellar KJ.
Bioorg Med Chem Lett (2004) 14 : 1845 -1848
PubMed 15050613 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 7.94 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 2 10.60
CHEMBL59986 1 9.62
CHEMBL55138 1 9.38
CHEMBL497939 CYTISINICLINE 3.0 1 7.43
CHEMBL667 ACETYLCHOLINE 4.0 1 7.39
CHEMBL47814 DIMETHYLPHENYLPIPERAZINIUM IODIDE 1 7.38
CHEMBL3 NICOTINE 4.0 1 7.37
CHEMBL14 CARBACHOL 4.0 1 5.96
CHEMBL920 CHOLINE 0.5 1 4.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE Ki = 0.025 nM 10.60
CHEMBL6623 EPIBATIDINE Ki = 0.16 nM 9.80
CHEMBL59986 Ki = 0.24 nM 9.62
CHEMBL55138 Ki = 0.42 nM 9.38
CHEMBL497939 CYTISINICLINE Ki = 37.0 nM 7.43
CHEMBL667 ACETYLCHOLINE Ki = 41.0 nM 7.39
CHEMBL47814 DIMETHYLPHENYLPIPERAZINIUM IODIDE Ki = 42.0 nM 7.38
CHEMBL3 NICOTINE Ki = 43.0 nM 7.37
CHEMBL14 CARBACHOL Ki = 1100.0 nM 5.96
CHEMBL920 CHOLINE Ki = 37000.0 nM 4.43