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Assay Detail

CHEMBL756125

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

Binding
Binding affinity towards nicotinic acetylcholine receptor alpha4-beta2 from rat brain homogenates
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

3-(4-Aminobutyn-1-yl)pyridines: binding at alpha 4 beta 2 nicotinic cholinergic receptors.
Dogruer D, Lee M, Dukat M, Damaj MI, Martin BR, Glennon RA.
Bioorg Med Chem Lett (2004) 14 : 523 -526
PubMed 14698195 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 7.19 9.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL345732 1 9.30
CHEMBL3 NICOTINE 4.0 1 8.68
CHEMBL61616 1 7.68
CHEMBL57912 1 7.66
CHEMBL60792 1 7.55
CHEMBL148489 N-(3-PYRIDYLMETHYL)PYRROLIDINE 1 7.52
CHEMBL112221 1 7.46
CHEMBL348693 1 6.96
CHEMBL54860 1 6.95
CHEMBL347558 1 6.81
CHEMBL328429 1 6.67
CHEMBL151817 1 6.33
CHEMBL150893 1 6.29
CHEMBL331904 1 6.27
CHEMBL150948 1 5.75
CHEMBL147446 1 -
CHEMBL151983 1 -
CHEMBL357101 1 -
CHEMBL146956 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL345732 Ki = 0.5 nM 9.30
CHEMBL3 NICOTINE Ki = 2.1 nM 8.68
CHEMBL61616 Ki = 21.0 nM 7.68
CHEMBL57912 Ki = 22.0 nM 7.66
CHEMBL60792 Ki = 28.0 nM 7.55
CHEMBL148489 N-(3-PYRIDYLMETHYL)PYRROLIDINE Ki = 30.0 nM 7.52
CHEMBL112221 Ki = 35.0 nM 7.46
CHEMBL348693 Ki = 110.0 nM 6.96
CHEMBL54860 Ki = 113.0 nM 6.95
CHEMBL347558 Ki = 154.0 nM 6.81
CHEMBL328429 Ki = 212.0 nM 6.67
CHEMBL151817 Ki = 470.0 nM 6.33
CHEMBL150893 Ki = 510.0 nM 6.29
CHEMBL331904 Ki = 540.0 nM 6.27
CHEMBL150948 Ki = 1770.0 nM 5.75
CHEMBL147446 Ki > 10000.0 nM -
CHEMBL151983 Ki > 10000.0 nM -
CHEMBL357101 Ki > 10000.0 nM -
CHEMBL146956 Ki = - nM -