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Assay Detail

CHEMBL894097

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

Functional
Agonist activity at rat GABA alpha-1-T129S-beta-2-gamma-2 receptor mutant expressed in HEK293 cells by Whole-cell patch-clamp technique
5
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Cell Type HEK293
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

5-Substituted imidazole-4-acetic acid analogues: synthesis, modeling, and pharmacological characterization of a series of novel gamma-aminobutyric acid(C) receptor agonists.
Madsen C, Jensen AA, Liljefors T, Kristiansen U, Nielsen B, Hansen CP, Larsen M, Ebert B, Bang-Andersen B, Krogsgaard-Larsen P, Frølund B.
J Med Chem (2007) 50 : 4147 -4161
PubMed 17655213 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 5 4.80 4.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 2 4.89
CHEMBL784 IMIDAZOLE ACETIC ACID 2 4.70
CHEMBL243929 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID EC50 = 12882.5 nM 4.89
CHEMBL96 GAMMA-AMINOBUTYRIC ACID EC50 = 12800.0 nM 4.89
CHEMBL784 IMIDAZOLE ACETIC ACID EC50 = 20000.0 nM 4.70
CHEMBL784 IMIDAZOLE ACETIC ACID EC50 = 19952.62 nM 4.70
CHEMBL243929 EC50 > 1000000.0 nM -