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Assay Detail

CHEMBL750437

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Functional
Compound was evaluated for functional activation from channel currents at human Nicotinic acetylcholine receptor alpha-7 expressed in oocytes.
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type Oocyte
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-7 (CHEMBL2492)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Identification and initial structure-activity relationships of (R)-5-(2-azetidinylmethoxy)-2-chloropyridine (ABT-594), a potent, orally active, non-opiate analgesic agent acting via neuronal nicotinic acetylcholine receptors.
Holladay MW, Wasicak JT, Lin NH, He Y, Ryther KB, Bannon AW, Buckley MJ, Kim DJ, Decker MW, Anderson DJ, Campbell JE, Kuntzweiler TA, Donnelly-Roberts DL, Piattoni-Kaplan M, Briggs CA, Williams M, Arneric SP.
J Med Chem (1998) 41 : 407 -412
PubMed 9484491 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 3 4.58 5.05

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL59986 1 5.05
CHEMBL262769 1 4.44
CHEMBL430497 TEBANICLINE 2.0 1 4.25

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL59986 EC50 = 8900.0 nM 5.05
CHEMBL262769 EC50 = 36000.0 nM 4.44
CHEMBL430497 TEBANICLINE EC50 = 56000.0 nM 4.25