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Assay Detail

CHEMBL881988

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

Binding
Percent inhibition against GABAA receptor alpha at a compound concentration of 1 uM
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

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

Publication

2-n-Butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine and analogues as A2A adenosine receptor antagonists. Design, synthesis, and pharmacological characterization.
Minetti P, Tinti MO, Carminati P, Castorina M, Di Cesare MA, Di Serio S, Gallo G, Ghirardi O, Giorgi F, Giorgi L, Piersanti G, Bartoccini F, Tarzia G.
J Med Chem (2005) 48 : 6887 -6896
PubMed 16250647 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Inhibition 2 - -
IC50 1 7.80 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL273481 MUSCIMOL 1.0 1 7.80
CHEMBL197669 ST1535 1.0 1 -
CHEMBL196258 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL273481 MUSCIMOL IC50 = 16.0 nM 7.80
CHEMBL197669 ST1535 Inhibition < 10.0 % -
CHEMBL196258 Inhibition < 10.0 % -