Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL839719

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

Binding
Inhibition of [3H]nicotine binding to alpha4-beta2 nicotinic acetylcholine receptor of rat brain membrane
3
Total Activities
3
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; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion.
Papke RL, Zheng G, Horenstein NA, Dwoskin LP, Crooks PA.
Bioorg Med Chem Lett (2005) 15 : 3874 -3880
PubMed 16005216 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.17 7.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL282473 1 7.39
CHEMBL21553 1 6.22
CHEMBL281410 1 4.91

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL282473 Ki = 41.0 nM 7.39
CHEMBL21553 Ki = 600.0 nM 6.22
CHEMBL281410 Ki = 12200.0 nM 4.91