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Assay Detail

CHEMBL752656

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

Binding
Activation potency at Nicotinic acetylcholine receptor alpha3beta4, expressed as concentration required to achieve a half maximal activation
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
EC50 9 6.10 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 7.85
CHEMBL63102 1 6.51
CHEMBL274538 1 5.80
CHEMBL25619 1 5.64
CHEMBL10886 1 5.41
CHEMBL111008 1 5.38
CHEMBL327104 1 -
CHEMBL323045 1 -
CHEMBL10863 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE EC50 = 14.0 nM 7.85
CHEMBL63102 EC50 = 310.0 nM 6.51
CHEMBL274538 EC50 = 1590.0 nM 5.80
CHEMBL25619 EC50 = 2290.0 nM 5.64
CHEMBL10886 EC50 = 3890.0 nM 5.41
CHEMBL111008 EC50 = 4190.0 nM 5.38
CHEMBL327104 EC50 > 100000.0 nM -
CHEMBL323045 EC50 > 100000.0 nM -
CHEMBL10863 EC50 > 100000.0 nM -