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Assay Detail

CHEMBL750361

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

Binding
Binding affinity towards nicotinic acetylcholine receptor using [3H]nicotine as radioligand in rat brain homogenates
28
Total Activities
28
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Neuronal acetylcholine receptor (CHEMBL2094110)
Type PROTEIN COMPLEX GROUP
Organism Rattus norvegicus

Publication

A comparison of the binding of three series of nicotinic ligands.
Lee M, Dukat M, Liao L, Flammia D, Damaj MI, Martin B, Glennon RA.
Bioorg Med Chem Lett (2002) 12 : 1989 -1992
PubMed 12113825 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 28 7.57 10.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59986 1 10.30
CHEMBL293435 1 9.35
CHEMBL58231 1 9.35
CHEMBL61013 1 9.20
CHEMBL62128 1 8.99
CHEMBL3 NICOTINE 4.0 1 8.89
CHEMBL294757 1 8.74
CHEMBL61772 1 8.16
CHEMBL61883 1 7.95
CHEMBL303530 1 7.85
CHEMBL62015 1 7.80
CHEMBL61616 1 7.68
CHEMBL57912 1 7.66
CHEMBL292114 1 7.66
CHEMBL60792 1 7.55
CHEMBL60141 1 7.39
CHEMBL292655 1 7.21
CHEMBL60124 1 7.18
CHEMBL59967 1 7.03
CHEMBL61520 1 7.03
CHEMBL61527 1 6.94
CHEMBL60937 1 6.54
CHEMBL58616 1 6.35
CHEMBL61165 1 6.19
CHEMBL294499 1 6.07
CHEMBL59420 1 5.96
CHEMBL61764 1 5.61
CHEMBL60356 1 5.39

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59986 Ki = 0.05 nM 10.30
CHEMBL293435 Ki = 0.45 nM 9.35
CHEMBL58231 Ki = 0.45 nM 9.35
CHEMBL61013 Ki = 0.63 nM 9.20
CHEMBL62128 Ki = 1.03 nM 8.99
CHEMBL3 NICOTINE Ki = 1.3 nM 8.89
CHEMBL294757 Ki = 1.8 nM 8.74
CHEMBL61772 Ki = 6.9 nM 8.16
CHEMBL61883 Ki = 11.2 nM 7.95
CHEMBL303530 Ki = 14.0 nM 7.85
CHEMBL62015 Ki = 16.0 nM 7.80
CHEMBL61616 Ki = 21.0 nM 7.68
CHEMBL57912 Ki = 22.0 nM 7.66
CHEMBL292114 Ki = 22.0 nM 7.66
CHEMBL60792 Ki = 28.0 nM 7.55
CHEMBL60141 Ki = 41.0 nM 7.39
CHEMBL292655 Ki = 62.0 nM 7.21
CHEMBL60124 Ki = 66.0 nM 7.18
CHEMBL59967 Ki = 93.0 nM 7.03
CHEMBL61520 Ki = 93.0 nM 7.03
CHEMBL61527 Ki = 115.0 nM 6.94
CHEMBL60937 Ki = 290.0 nM 6.54
CHEMBL58616 Ki = 447.0 nM 6.35
CHEMBL61165 Ki = 640.0 nM 6.19
CHEMBL294499 Ki = 850.0 nM 6.07
CHEMBL59420 Ki = 1110.0 nM 5.96
CHEMBL61764 Ki = 2470.0 nM 5.61
CHEMBL60356 Ki = 4070.0 nM 5.39