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Assay Detail

CHEMBL840051

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

Binding
Inhibition of [3H]-MLA binding to alpha-7 nicotinic acetylcholine receptor of rat brain membrane
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion.
Papke RL, Zheng G, Horenstein NA, Dwoskin LP, Crooks PA.
Bioorg Med Chem Lett (2005) 15 : 3874 -3880
PubMed 16005216 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 5.72 6.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL417278 1 6.23
CHEMBL3 NICOTINE 4.0 1 6.11
CHEMBL282473 1 4.82
CHEMBL281410 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL417278 Ki = 590.0 nM 6.23
CHEMBL3 NICOTINE Ki = 770.0 nM 6.11
CHEMBL282473 Ki = 15200.0 nM 4.82
CHEMBL281410 Ki > 100000.0 nM -