Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL3877547

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

ADMET
Displacement of [3H]epibatidine from rat alpha3beta4 nAChR by liquid scintillation counting
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Rattus norvegicus
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha3/beta4 (CHEMBL1907593)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Synthesis and biological evaluation of novel hybrids of highly potent and selective α4β2-Nicotinic acetylcholine receptor (nAChR) partial agonists.
Zhang HK, Eaton JB, Fedolak A, Gunosewoyo H, Onajole OK, Brunner D, Lukas RJ, Yu LF, Kozikowski AP.
Eur J Med Chem (2016) 124 : 689 -697
PubMed 27639361 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.24 7.19

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL389964 1 7.19
CHEMBL71085 1 6.44
CHEMBL3970672 1 5.09
CHEMBL3948977 1 -
CHEMBL3898434 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL389964 Ki = 64.6 nM 7.19
CHEMBL71085 Ki = 366.0 nM 6.44
CHEMBL3970672 Ki = 8098.0 nM 5.09
CHEMBL3948977 Ki > 10000.0 nM -
CHEMBL3898434 Ki > 10000.0 nM -