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Assay Detail

CHEMBL871846

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

Binding
Binding affinity towards human nicotinic acetylcholine receptor alpha 7 expressed in GH4C1 cell using [3H]methyllycaconitine
17
Total Activities
17
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type GH4-C1
Confidence 9 — Direct single protein target
Curated By Expert

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

High affinity ligands for the alpha7 nicotinic receptor that show no cross-reactivity with the 5-HT3 receptor.
Baker SR, Boot J, Brunavs M, Dobson D, Green R, Hayhurst L, Keenan M, Wallace L.
Bioorg Med Chem Lett (2005) 15 : 4727 -4730
PubMed 16165358 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 17 7.89 8.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL195190 1 8.96
CHEMBL364069 1 8.89
CHEMBL370535 1 8.74
CHEMBL195345 1 8.51
CHEMBL194100 1 8.47
CHEMBL195329 1 8.47
CHEMBL372041 1 8.39
CHEMBL188469 1 8.16
CHEMBL510275 METHYLLYCACONITINE 1 8.14
CHEMBL193329 1 8.08
CHEMBL365323 1 7.84
CHEMBL195800 1 7.78
CHEMBL194984 1 7.57
CHEMBL372895 1 6.92
CHEMBL365181 1 6.57
CHEMBL195519 1 6.38
CHEMBL440387 1 6.28

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL195190 Ki = 1.1 nM 8.96
CHEMBL364069 Ki = 1.3 nM 8.89
CHEMBL370535 Ki = 1.8 nM 8.74
CHEMBL195345 Ki = 3.1 nM 8.51
CHEMBL194100 Ki = 3.4 nM 8.47
CHEMBL195329 Ki = 3.4 nM 8.47
CHEMBL372041 Ki = 4.1 nM 8.39
CHEMBL188469 Ki = 6.9 nM 8.16
CHEMBL510275 METHYLLYCACONITINE Ki = 7.3 nM 8.14
CHEMBL193329 Ki = 8.3 nM 8.08
CHEMBL365323 Ki = 14.6 nM 7.84
CHEMBL195800 Ki = 16.7 nM 7.78
CHEMBL194984 Ki = 26.9 nM 7.57
CHEMBL372895 Ki = 121.2 nM 6.92
CHEMBL365181 Ki = 268.4 nM 6.57
CHEMBL195519 Ki = 420.0 nM 6.38
CHEMBL440387 Ki = 524.5 nM 6.28