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Assay Detail

CHEMBL822798

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

Binding
Compound was evaluated for its ability to displace [125 I]alpha-bungarotoxin (alpha-BgT) from torpedo alpha1-beta1-gamma1 electroplax
3
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Torpedo
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Acetylcholine receptor subunit alpha (CHEMBL3097)
Type SINGLE PROTEIN
Organism Torpedo californica

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
Ki 3 5.63 6.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL262769 1 6.42
CHEMBL430497 TEBANICLINE 2.0 2 5.47

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL262769 Ki = 384.0 nM 6.42
CHEMBL430497 TEBANICLINE Ki = 3400.0 nM 5.47
CHEMBL430497 TEBANICLINE Ki = 10000.0 nM 5.00