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

CHEMBL3370250

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

Binding
Displacement of [3H]muscimol from GABAA receptor in SPRD rat brain synaptic membranes by scintillation counting method
ChEMBL ↗
47
Total Activities
31
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

GABA-A receptor; anion channel (CHEMBL2093872) ↗
Type PROTEIN COMPLEX GROUP
Organism Homo sapiens

Publication

Synthesis and pharmacological evaluation of 6-aminonicotinic acid analogues as novel GABA(A) receptor agonists.
Petersen JG, Sørensen T, Damgaard M, Nielsen B, Jensen AA, Balle T, Bergmann R, Frølund B.
Eur J Med Chem (2014) 84 : 404 -416
PubMed 25038482 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 47 5.57 8.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273481 MUSCIMOL 1.0 1 8.22
CHEMBL96 GAMMA-AMINOBUTYRIC ACID 1.0 1 7.48
CHEMBL3322882 — — 2 7.36
CHEMBL39071 ISOGUVACINE — 2 7.26
CHEMBL279998 ISONIPECOTIC ACID — 2 6.30
CHEMBL3322886 — — 2 6.27
CHEMBL3322870 — — 2 5.87
CHEMBL3322871 — — 2 5.68
CHEMBL3322875 — — 2 5.44
CHEMBL3322864 — — 2 5.39
CHEMBL3322884 — — 2 5.29
CHEMBL3322872 — — 2 5.15
CHEMBL3322876 — — 2 5.03
CHEMBL3322866 — — 2 4.72
CHEMBL3322877 — — 2 4.63
CHEMBL3322883 — — 2 4.32
CHEMBL3322867 — — 2 4.14
CHEMBL3322865 — — 2 4.05
CHEMBL3322885 — — 1 -
CHEMBL247316 — — 1 -
CHEMBL235168 — — 1 -
CHEMBL3322881 — — 1 -
CHEMBL3322880 — — 1 -
CHEMBL3322879 — — 1 -
CHEMBL3322878 — — 1 -
CHEMBL3322874 — — 1 -
CHEMBL3322873 — — 1 -
CHEMBL3322869 — — 1 -
CHEMBL3322868 — — 1 -
CHEMBL282068 — — 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273481 MUSCIMOL Ki = 6.0 nM 8.22
CHEMBL96 GAMMA-AMINOBUTYRIC ACID Ki = 33.0 nM 7.48
CHEMBL3322882 — Ki = 44.0 nM 7.36
CHEMBL3322882 — Ki = 43.65 nM 7.36
CHEMBL39071 ISOGUVACINE Ki = 55.0 nM 7.26
CHEMBL39071 ISOGUVACINE Ki = 54.95 nM 7.26
CHEMBL279998 ISONIPECOTIC ACID Ki = 501.19 nM 6.30
CHEMBL279998 ISONIPECOTIC ACID Ki = 510.0 nM 6.29
CHEMBL3322886 — Ki = 540.0 nM 6.27
CHEMBL3322886 — Ki = 537.03 nM 6.27
CHEMBL3322870 — Ki = 1348.96 nM 5.87
CHEMBL3322870 — Ki = 1400.0 nM 5.85
CHEMBL3322871 — Ki = 2100.0 nM 5.68
CHEMBL3322871 — Ki = 2089.3 nM 5.68
CHEMBL3322875 — Ki = 3630.78 nM 5.44
CHEMBL3322875 — Ki = 3600.0 nM 5.44
CHEMBL3322864 — Ki = 4073.8 nM 5.39
CHEMBL3322864 — Ki = 4400.0 nM 5.36
CHEMBL3322884 — Ki = 5128.61 nM 5.29
CHEMBL3322884 — Ki = 5300.0 nM 5.28
CHEMBL3322872 — Ki = 7079.46 nM 5.15
CHEMBL3322872 — Ki = 7100.0 nM 5.15
CHEMBL3322876 — Ki = 9300.0 nM 5.03
CHEMBL3322876 — Ki = 9332.54 nM 5.03
CHEMBL3322866 — Ki = 19000.0 nM 4.72
CHEMBL3322866 — Ki = 19054.61 nM 4.72
CHEMBL3322877 — Ki = 23442.29 nM 4.63
CHEMBL3322877 — Ki = 24000.0 nM 4.62
CHEMBL3322883 — Ki = 47863.01 nM 4.32
CHEMBL3322883 — Ki = 49000.0 nM 4.31
CHEMBL3322867 — Ki = 73000.0 nM 4.14
CHEMBL3322867 — Ki = 72443.6 nM 4.14
CHEMBL3322865 — Ki = 89125.09 nM 4.05
CHEMBL3322865 — Ki = 90000.0 nM 4.05
CHEMBL3322873 — Ki > 100000.0 nM -
CHEMBL3322878 — Ki > 100000.0 nM -
CHEMBL3322879 — Ki > 100000.0 nM -
CHEMBL3322869 — Ki > 100000.0 nM -
CHEMBL3322868 — Ki > 100000.0 nM -
CHEMBL3322880 — Ki > 100000.0 nM -
CHEMBL3322874 — Ki > 100000.0 nM -
CHEMBL282068 — Ki > 100000.0 nM -
CHEMBL3322863 — Ki > 100000.0 nM -
CHEMBL235168 — Ki > 100000.0 nM -
CHEMBL247316 — Ki > 100000.0 nM -
CHEMBL3322885 — Ki > 100000.0 nM -
CHEMBL3322881 — Ki > 100000.0 nM -