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Assay Detail

CHEMBL894092

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

Functional
Agonist activity at GABAC rho 1 receptor expressed in tsA-201 cells by FMP assay
14
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type tsA-201
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 14 5.71 6.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 2 6.40
CHEMBL273481 MUSCIMOL 1.0 2 6.21
CHEMBL784 IMIDAZOLE ACETIC ACID 2 5.30
CHEMBL243929 2 5.00
CHEMBL390012 2 -
CHEMBL388249 2 -
CHEMBL243932 2 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID EC50 = 398.11 nM 6.40
CHEMBL96 GAMMA-AMINOBUTYRIC ACID EC50 = 430.0 nM 6.37
CHEMBL273481 MUSCIMOL EC50 = 620.0 nM 6.21
CHEMBL273481 MUSCIMOL EC50 = 630.96 nM 6.20
CHEMBL784 IMIDAZOLE ACETIC ACID EC50 = 5011.87 nM 5.30
CHEMBL784 IMIDAZOLE ACETIC ACID EC50 = 5500.0 nM 5.26
CHEMBL243929 EC50 = 10000.0 nM 5.00
CHEMBL243929 EC50 = 11000.0 nM 4.96
CHEMBL390012 EC50 = 330000.0 nM -
CHEMBL390012 EC50 = 316227.77 nM -
CHEMBL388249 EC50 = 220000.0 nM -
CHEMBL388249 EC50 = 199526.23 nM -
CHEMBL243932 EC50 = 140000.0 nM -
CHEMBL243932 EC50 = 158489.32 nM -