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Assay Detail

CHEMBL752658

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

Binding
Binding affinity at rat brain Nicotinic acetylcholine receptor alpha3-beta4
9
Total Activities
9
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; alpha3/beta4 (CHEMBL1907593)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Synthesis and pharmacological characterization of novel analogues of the nicotinic acetylcholine receptor agonist (+/-)-UB-165.
Sharples CG, Karig G, Simpson GL, Spencer JA, Wright E, Millar NS, Wonnacott S, Gallagher T.
J Med Chem (2002) 45 : 3235 -3245
PubMed 12109907 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 6.87 10.11

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 10.11
CHEMBL63102 1 8.19
CHEMBL274538 1 7.65
CHEMBL25619 1 7.59
CHEMBL10886 1 6.63
CHEMBL111008 1 6.51
CHEMBL10863 1 5.55
CHEMBL327104 1 4.98
CHEMBL323045 1 4.66

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE Ki = 0.077 nM 10.11
CHEMBL63102 Ki = 6.5 nM 8.19
CHEMBL274538 Ki = 22.5 nM 7.65
CHEMBL25619 Ki = 25.4 nM 7.59
CHEMBL10886 Ki = 236.0 nM 6.63
CHEMBL111008 Ki = 306.0 nM 6.51
CHEMBL10863 Ki = 2846.0 nM 5.55
CHEMBL327104 Ki = 10500.0 nM 4.98
CHEMBL323045 Ki = 22000.0 nM 4.66