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Assay Detail

CHEMBL3385108

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

Binding
Displacement of [3H]epibatidine from rat forebrain alpha2beta2 nAChR by competition binding assay
7
Total Activities
7
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; alpha2/beta2 (CHEMBL1907592)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Enantiopure Cyclopropane-Bearing Pyridyldiazabicyclo[3.3.0]octanes as Selective α4β2-nAChR Ligands.
Onajole OK, Eaton JB, Lukas RJ, Brunner D, Thiede L, Caldarone BJ, Kozikowski AP.
ACS Med Chem Lett (2014) 5 : 1196 -1201
PubMed 25408831 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 9.03 9.70

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3356152 1 9.70
CHEMBL1186374 1 9.52
CHEMBL3356148 1 9.52
CHEMBL3356151 1 9.40
CHEMBL3356150 1 9.22
CHEMBL3 NICOTINE 4.0 1 8.26
CHEMBL3356149 1 7.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3356152 Ki = 0.2 nM 9.70
CHEMBL1186374 Ki = 0.3 nM 9.52
CHEMBL3356148 Ki = 0.3 nM 9.52
CHEMBL3356151 Ki = 0.4 nM 9.40
CHEMBL3356150 Ki = 0.6 nM 9.22
CHEMBL3 NICOTINE Ki = 5.5 nM 8.26
CHEMBL3356149 Ki = 25.0 nM 7.60