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Assay Detail

CHEMBL1785677

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

Binding
Activity at alpha4beta2*nAChR in mouse striatal synaptosomes assessed as alpha-conotoxic MII-resistant DA release
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Mus musculus
Tissue Brain
Subcellular Synaptosomes
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Nicotinic acetylcholine receptor alpha-4/beta-2 (CHEMBL3301382)
Type PROTEIN COMPLEX
Organism Mus musculus

Publication

Evaluation of structurally diverse neuronal nicotinic receptor ligands for selectivity at the alpha6( *) subtype.
Breining SR, Bencherif M, Grady SR, Whiteaker P, Marks MJ, Wageman CR, Lester HA, Yohannes D.
Bioorg Med Chem Lett (2009) 19 : 4359 -4363
PubMed 19560354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 10 5.58 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3217150 1 7.47
CHEMBL1783886 1 6.35
CHEMBL1783888 1 5.75
CHEMBL1783878 1 5.50
CHEMBL3215819 1 5.47
CHEMBL1783883 1 5.36
CHEMBL1783880 1 5.23
CHEMBL1783879 1 5.08
CHEMBL1782074 1 4.89
CHEMBL1783884 1 4.72

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3217150 EC50 = 34.0 nM 7.47
CHEMBL1783886 EC50 = 450.0 nM 6.35
CHEMBL1783888 EC50 = 1800.0 nM 5.75
CHEMBL1783878 EC50 = 3200.0 nM 5.50
CHEMBL3215819 EC50 = 3400.0 nM 5.47
CHEMBL1783883 EC50 = 4400.0 nM 5.36
CHEMBL1783880 EC50 = 5900.0 nM 5.23
CHEMBL1783879 EC50 = 8300.0 nM 5.08
CHEMBL1782074 EC50 = 13000.0 nM 4.89
CHEMBL1783884 EC50 = 19000.0 nM 4.72