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Assay Detail

CHEMBL749561

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

Binding
Binding affinity to subtype Nicotinic acetylcholine receptor alpha7 using [3H]-MLA as radioligand in rat brain
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL4980)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and nicotinic binding studies on enantiopure diazine analogues of the novel (2-chloro-5-pyridyl)-9-azabicyclo[4.2.1]non-2-ene UB-165.
Gohlke H, Gündisch D, Schwarz S, Seitz G, Tilotta MC, Wegge T.
J Med Chem (2002) 45 : 1064 -1072
PubMed 11855986 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 7.71 9.02

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274538 1 9.02
CHEMBL10886 1 7.97
CHEMBL275466 1 7.92
CHEMBL25619 1 7.05
CHEMBL10863 1 6.60
CHEMBL10585 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274538 Ki = 0.95 nM 9.02
CHEMBL10886 Ki = 10.7 nM 7.97
CHEMBL275466 Ki = 12.0 nM 7.92
CHEMBL25619 Ki = 90.0 nM 7.05
CHEMBL10863 Ki = 250.0 nM 6.60
CHEMBL10585 Ki > 10.0 nM -