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Assay Detail

CHEMBL641343

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

Binding
Displacement of [3H]-CGS- from Adenosine A2a receptor of rat striatal homogenate
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Synthesis of new pyrazolo[4,3-e]1,2,4-triazolo[1,5-c] pyrimidine and 1,2,3-triazolo[4,5-e]1,2,4-triazolo[1,5-c] pyrimidine displaying potent and selective activity as A2a adenosine receptor antagonists.
Baraldi PG, Manfredini S, Simoni D, Zappaterra L, Zocchi C, Dionisotti S, Ongini E
Bioorg Med Chem Lett (1994) 4 : 2539 -2544
· DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 2 7.54 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL16687 CGS-15943 1 8.92
CHEMBL53737 1 6.15

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL16687 CGS-15943 Ki = 1.2 nM 8.92
CHEMBL53737 Ki = 706.0 nM 6.15