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Assay Detail

CHEMBL679467

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

Binding
Displacement of [3H]Ro-151788 from rat GABA-A receptor alpha-1-beta-2-gamma-2 subunits expressed in HEK293 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Cell Type HEK293
Confidence 7 — Homologous single protein target
Curated By Autocuration

Target

GABA-A receptor; alpha-1/beta-2/gamma-2 (CHEMBL2095167)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Benzodiazepine receptor ligands. 7. Synthesis and pharmacological evaluation of new 3-esters of the 8-chloropyrazolo[5,1-c][1,2,4]benzotriazine 5-oxide. 3-(2-Thienylmethoxycarbonyl) derivative: an anxioselective agent in rodents.
Costanzo A, Guerrini G, Ciciani G, Bruni F, Costagli C, Selleri S, Besnard F, Costa B, Martini C, Malmberg-Aiello P.
J Med Chem (2002) 45 : 5710 -5720
PubMed 12477354 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 7.94 8.39

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL303152 1 8.39
CHEMBL12 DIAZEPAM 4.0 1 7.85
CHEMBL911 ZOLPIDEM 4.0 1 7.57

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL303152 Ki = 4.1 nM 8.39
CHEMBL12 DIAZEPAM Ki = 14.0 nM 7.85
CHEMBL911 ZOLPIDEM Ki = 26.7 nM 7.57