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Assay Detail

CHEMBL881978

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

Binding
Percent inhibition against P2Y Purinoceptor at 1 uM
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

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 2 7.76 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL132722 DIPHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER 1 7.85
CHEMBL2390988 DATPALPHAS 1 7.66
CHEMBL197669 ST1535 1.0 1 -
CHEMBL196258 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL132722 DIPHOSPHOMETHYLPHOSPHONIC ACID ADENOSYL ESTER IC50 = 14.0 nM 7.85
CHEMBL2390988 DATPALPHAS IC50 = 22.0 nM 7.66
CHEMBL197669 ST1535 Inhibition < 10.0 % -
CHEMBL196258 Inhibition < 10.0 % -