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Assay Detail

CHEMBL748019

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Binding
Binding affinity value obtained by measuring the displacement of radioligand [3H](-)-cytisine from whole rat brain Nicotinic acetylcholine receptor
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

Structure-activity studies on 2-methyl-3-(2(S)-pyrrolidinylmethoxy) pyridine (ABT-089): an orally bioavailable 3-pyridyl ether nicotinic acetylcholine receptor ligand with cognition-enhancing properties.
Lin NH, Gunn DE, Ryther KB, Garvey DS, Donnelly-Roberts DL, Decker MW, Brioni JD, Buckley MJ, Rodrigues AD, Marsh KG, Anderson DJ, Buccafusco JJ, Prendergast MA, Sullivan JP, Williams M, Arneric SP, Holladay MW.
J Med Chem (1997) 40 : 385 -390
PubMed 9022806 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 7.07 7.78

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL127071 POZANICLINE 2.0 1 7.78
CHEMBL84692 1 7.57
CHEMBL126692 1 7.41
CHEMBL129609 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL127071 POZANICLINE Ki = 16.7 nM 7.78
CHEMBL84692 Ki = 27.2 nM 7.57
CHEMBL126692 Ki = 39.0 nM 7.41
CHEMBL129609 Ki = 3000.0 nM 5.52