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Assay Detail

CHEMBL881980

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

Binding
Percent inhibition against GABA-B receptor at 1 uM
3
Total Activities
3
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 6 — Multiple protein complex / RNA
Curated By Expert

Target

GABA-B receptor (CHEMBL2111463)
Type PROTEIN COMPLEX
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 7.30 7.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL701 BACLOFEN 4.0 1 7.30
CHEMBL197669 ST1535 1.0 1 -
CHEMBL196258 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL701 BACLOFEN IC50 = 50.0 nM 7.30
CHEMBL197669 ST1535 Inhibition < 10.0 % -
CHEMBL196258 Inhibition < 10.0 % -