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Assay Detail

CHEMBL756007

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

Binding
The compound was evaluated for percentage inhibition of binding of [3H]- nicotine to Nicotinic acetylcholine receptor alpha4-beta2 in Rat Cerebral Cortical Membranes
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

6beta-Acetoxynortropane: a potent muscarinic agonist with apparent selectivity toward M2-receptors.
Pei XF, Gupta TH, Badio B, Padgett WL, Daly JW.
J Med Chem (1998) 41 : 2047 -2055
PubMed 9622546 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 10 5.75 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3 NICOTINE 4.0 1 9.00
CHEMBL64788 1 6.82
CHEMBL7303 ARECOLINE -1.0 1 6.57
CHEMBL294273 1 5.82
CHEMBL64000 1 5.52
CHEMBL2115494 1 5.40
CHEMBL412663 1 5.05
CHEMBL2114478 1 4.62
CHEMBL2115495 1 4.50
CHEMBL2114477 1 4.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3 NICOTINE Ki = 1.0 nM 9.00
CHEMBL64788 Ki = 150.0 nM 6.82
CHEMBL7303 ARECOLINE Ki = 270.0 nM 6.57
CHEMBL294273 Ki = 1500.0 nM 5.82
CHEMBL64000 Ki = 3000.0 nM 5.52
CHEMBL2115494 Ki = 4000.0 nM 5.40
CHEMBL412663 Ki = 8900.0 nM 5.05
CHEMBL2114478 Ki = 24000.0 nM 4.62
CHEMBL2115495 Ki = 32000.0 nM 4.50
CHEMBL2114477 Ki = 64000.0 nM 4.19