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Assay Detail

CHEMBL683018

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

Binding
Binding affinity for recombinant rat GABA-A receptor alpha-3-beta-2-gamma-2 subunits expressed in HEK293 cells
5
Total Activities
5
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 Expert

Target

GABA A receptor alpha-3/beta-2/gamma-2 (CHEMBL2111343)
Type PROTEIN COMPLEX
Organism Rattus norvegicus

Publication

Synthesis and benzodiazepine receptor affinity of pyrazolo[1,5-a]pyrimidine derivatives. 3. New 6-(3-thienyl) series as alpha 1 selective ligands.
Selleri S, Bruni F, Costagli C, Costanzo A, Guerrini G, Ciciani G, Gratteri P, Bonaccini C, Malmberg Aiello P, Besnard F, Renard S, Costa B, Martini C.
J Med Chem (2003) 46 : 310 -313
PubMed 12519068 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.99 7.82

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL12 DIAZEPAM 4.0 1 7.82
CHEMBL322313 1 7.05
CHEMBL440150 1 6.96
CHEMBL322697 1 6.71
CHEMBL911 ZOLPIDEM 4.0 1 6.42

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL12 DIAZEPAM Ki = 15.0 nM 7.82
CHEMBL322313 Ki = 89.0 nM 7.05
CHEMBL440150 Ki = 111.0 nM 6.96
CHEMBL322697 Ki = 196.0 nM 6.71
CHEMBL911 ZOLPIDEM Ki = 383.0 nM 6.42