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Assay Detail

CHEMBL751264

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

Functional
The compound was tested on recombinant human alpha4-beta4 cell lines of Human embryonic kidney for nicotinic acetylcholine receptor agonist functional potency
5
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta4 (CHEMBL1907591)
Type PROTEIN COMPLEX
Organism Homo sapiens

Publication

(S)-(-)-5-ethynyl-3-(1-methyl-2-pyrrolidinyl)pyridine maleate (SIB-1508Y): a novel anti-parkinsonian agent with selectivity for neuronal nicotinic acetylcholine receptors.
Cosford ND, Bleicher L, Herbaut A, McCallum JS, Vernier JM, Dawson H, Whitten JP, Adams P, Chavez-Noriega L, Correa LD, Crona JH, Mahaffy LS, Menzaghi F, Rao TS, Reid R, Sacaan AI, Santori E, Stauderman KA, Whelan K, Lloyd GK, McDonald IA.
J Med Chem (1996) 39 : 3235 -3237
PubMed 8765504 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 4.80 5.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3 NICOTINE 4.0 1 5.15
CHEMBL111659 ALTINICLINE 2.0 2 5.05
CHEMBL111580 2 4.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3 NICOTINE EC50 = 7100.0 nM 5.15
CHEMBL111659 ALTINICLINE EC50 = 9000.0 nM 5.05
CHEMBL111580 EC50 = 23000.0 nM 4.64
CHEMBL111580 EC50 = 25000.0 nM 4.60
CHEMBL111659 ALTINICLINE EC50 = 26000.0 nM 4.58