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Assay Detail

CHEMBL751862

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

Binding
Binding affinity at heteropentameric Nicotinic acetylcholine receptor alpha4-beta2 subtype using [3H]bungarotoxin as radioligand
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907589)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

Molecular recognition in nicotinic acetylcholine receptors: the importance of pi-cation interactions.
Schmitt JD, Sharples CG, Caldwell WS.
J Med Chem (1999) 42 : 3066 -3074
PubMed 10447950 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 8.31 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL6623 EPIBATIDINE 1 10.30
CHEMBL291498 1 9.59
CHEMBL105374 1 9.00
CHEMBL323325 1 8.96
CHEMBL3 NICOTINE 4.0 1 8.40
CHEMBL46486 TETRAMETHYLAMMONIUM ION 1 7.62
CHEMBL6200 NORNICOTINE 1.0 1 7.54
CHEMBL280963 DL-ANABASINE 1 7.04
CHEMBL102246 1 6.35
CHEMBL321099 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL6623 EPIBATIDINE Ki = 0.05 nM 10.30
CHEMBL291498 Ki = 0.26 nM 9.59
CHEMBL105374 Ki = 1.0 nM 9.00
CHEMBL323325 Ki = 1.1 nM 8.96
CHEMBL3 NICOTINE Ki = 4.0 nM 8.40
CHEMBL46486 TETRAMETHYLAMMONIUM ION Ki = 24.0 nM 7.62
CHEMBL6200 NORNICOTINE Ki = 29.0 nM 7.54
CHEMBL280963 DL-ANABASINE Ki = 92.0 nM 7.04
CHEMBL102246 Ki = 450.0 nM 6.35
CHEMBL321099 Ki - nM -