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Assay Detail

CHEMBL882455

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

Binding
In vitro binding affinity towards rat Nicotinic acetylcholine receptor alpha2-beta2 using 0.5 nM [3H]epibatidine
14
Total Activities
14
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

Epibatidine analogues as selective ligands for the alpha(x)beta2-containing subtypes of nicotinic acetylcholine receptors.
Huang Y, Zhu Z, Xiao Y, Laruelle M.
Bioorg Med Chem Lett (2005) 15 : 4385 -4388
PubMed 16039849 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 14 9.82 10.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 10.60
CHEMBL197830 1 10.46
CHEMBL291961 1 10.43
CHEMBL372133 1 10.40
CHEMBL197526 1 10.36
CHEMBL198228 1 10.28
CHEMBL185612 1 10.19
CHEMBL372638 1 10.18
CHEMBL185060 1 10.10
CHEMBL372326 1 9.61
CHEMBL58935 1 9.19
CHEMBL382533 1 8.96
CHEMBL197725 1 8.81
CHEMBL3 NICOTINE 4.0 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE Ki = 0.025 nM 10.60
CHEMBL197830 Ki = 0.035 nM 10.46
CHEMBL291961 Ki = 0.037 nM 10.43
CHEMBL372133 Ki = 0.04 nM 10.40
CHEMBL197526 Ki = 0.044 nM 10.36
CHEMBL198228 Ki = 0.053 nM 10.28
CHEMBL185612 Ki = 0.064 nM 10.19
CHEMBL372638 Ki = 0.066 nM 10.18
CHEMBL185060 Ki = 0.079 nM 10.10
CHEMBL372326 Ki = 0.245 nM 9.61
CHEMBL58935 Ki = 0.643 nM 9.19
CHEMBL382533 Ki = 1.11 nM 8.96
CHEMBL197725 Ki = 1.54 nM 8.81
CHEMBL3 NICOTINE Ki = 12.0 nM 7.92