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Assay Detail

CHEMBL894090

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

Functional
Agonist activity at human GABAC rho 1 receptor expressed in HEK293 cells by FMP assay
26
Total Activities
17
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
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 24 5.13 6.26
Ki 2 5.89 5.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 2 6.26
CHEMBL397209 2 5.89
CHEMBL273481 MUSCIMOL 1.0 2 5.66
CHEMBL784 IMIDAZOLE ACETIC ACID 2 4.89
CHEMBL243929 2 4.66
CHEMBL39071 ISOGUVACINE 2 4.17
CHEMBL389759 1 -
CHEMBL390208 1 -
CHEMBL243723 1 -
CHEMBL244137 1 -
CHEMBL390207 1 -
CHEMBL390012 2 -
CHEMBL388249 2 -
CHEMBL244136 1 -
CHEMBL388248 1 -
CHEMBL243932 2 -
CHEMBL243281 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL96 GAMMA-AMINOBUTYRIC ACID EC50 = 550.0 nM 6.26
CHEMBL397209 Ki = 1300.0 nM 5.89
CHEMBL273481 MUSCIMOL EC50 = 2200.0 nM 5.66
CHEMBL784 IMIDAZOLE ACETIC ACID EC50 = 13000.0 nM 4.89
CHEMBL243929 EC50 = 22000.0 nM 4.66
CHEMBL39071 ISOGUVACINE EC50 = 67000.0 nM 4.17
CHEMBL96 GAMMA-AMINOBUTYRIC ACID EC50 = 1995262314968882.8 nM -
CHEMBL39071 ISOGUVACINE EC50 = 15848931924611.11 nM -
CHEMBL273481 MUSCIMOL EC50 = 501187233627271.44 nM -
CHEMBL397209 Ki = 794328234724282.1 nM -
CHEMBL784 IMIDAZOLE ACETIC ACID EC50 = 79432823472428.22 nM -
CHEMBL243929 EC50 = 39810717055349.7 nM -
CHEMBL389759 EC50 > 1000000.0 nM -
CHEMBL243723 EC50 > 1000000.0 nM -
CHEMBL244137 EC50 > 1000000.0 nM -
CHEMBL390207 EC50 > 1000000.0 nM -
CHEMBL390012 EC50 = 210000.0 nM -
CHEMBL388249 EC50 = 240000.0 nM -
CHEMBL244136 EC50 > 1000000.0 nM -
CHEMBL388248 EC50 > 1000000.0 nM -
CHEMBL243932 EC50 = 420000.0 nM -
CHEMBL243932 EC50 = 2511886431509.58 nM -
CHEMBL388249 EC50 = 3981071705534.97 nM -
CHEMBL390012 EC50 = 5011872336272.71 nM -
CHEMBL243281 EC50 - -
CHEMBL390208 EC50 > 1000000.0 nM -