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Assay Detail

CHEMBL748708

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

Binding
The compound was tested for the inhibition of binding of [3H]epibatidine to central nicotinic acetylcholine receptor (nAChR) in rat brain.
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor subunit alpha-9 (CHEMBL2585)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis and evaluation of N-[11C]methylated analogues of epibatidine as tracers for positron emission tomographic studies of nicotinic acetylcholine receptors.
Horti AG, Scheffel U, Kimes AS, Musachio JL, Ravert HT, Mathews WB, Zhan Y, Finley PA, London ED, Dannals RF.
J Med Chem (1998) 41 : 4199 -4206
PubMed 9784094 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Kd 8 9.89 10.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL134341 1 10.57
CHEMBL135897 1 10.57
CHEMBL134418 1 10.55
CHEMBL337276 1 10.44
CHEMBL336118 1 10.43
CHEMBL135684 1 10.35
CHEMBL3 NICOTINE 4.0 1 8.30
CHEMBL335204 1 7.87

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL134341 Kd = 0.027 nM 10.57
CHEMBL135897 Kd = 0.027 nM 10.57
CHEMBL134418 Kd = 0.028 nM 10.55
CHEMBL337276 Kd = 0.036 nM 10.44
CHEMBL336118 Kd = 0.037 nM 10.43
CHEMBL135684 Kd = 0.045 nM 10.35
CHEMBL3 NICOTINE Kd = 5.0 nM 8.30
CHEMBL335204 Kd = 13.6 nM 7.87