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Assay Detail

CHEMBL1047083

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

Binding
Displacement of [3H]epibatidine from rat alpha4beta2 nAChR
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Autocuration

Target

Neuronal acetylcholine receptor; alpha4/beta2 (CHEMBL1907596)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Design of novel alpha7-subtype-preferring nicotinic acetylcholine receptor agonists: application of docking and MM-PBSA computational approaches, synthetic and pharmacological studies.
Grazioso G, Pomè DY, Matera C, Frigerio F, Pucci L, Gotti C, Dallanoce C, De Amici M.
Bioorg Med Chem Lett (2009) 19 : 6353 -6357
PubMed 19804970 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.22 6.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL64779 1 6.96
CHEMBL577107 1 5.51
CHEMBL571077 1 4.92
CHEMBL570620 1 4.68
CHEMBL579276 1 4.66
CHEMBL577968 1 4.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL64779 Ki = 110.0 nM 6.96
CHEMBL577107 Ki = 3100.0 nM 5.51
CHEMBL571077 Ki = 12000.0 nM 4.92
CHEMBL570620 Ki = 21000.0 nM 4.68
CHEMBL579276 Ki = 22000.0 nM 4.66
CHEMBL577968 Ki = 25000.0 nM 4.60