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Assay Detail

CHEMBL2401082

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

Binding
Displacement of [3H]DPCPX from human recombinant adenosine A1 receptor expressed in CHO-K1 cells after 60 mins
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO-K1
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Synthesis and biological evaluation of metabolites of 2-n-butyl-9-methyl-8-[1,2,3]triazol-2-yl-9H-purin-6-ylamine (ST1535), a potent antagonist of the A2A adenosine receptor for the treatment of Parkinson's disease.
Piersanti G, Bartoccini F, Lucarini S, Cabri W, Stasi MA, Riccioni T, Borsini F, Tarzia G, Minetti P.
J Med Chem (2013) 56 : 5456 -5463
PubMed 23789814 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 7.08 7.47

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2398484 1 7.47
CHEMBL2398482 1 7.47
CHEMBL2398483 1 7.28
CHEMBL197669 ST1535 1.0 1 7.00
CHEMBL2398485 1 6.82
CHEMBL2398480 1 6.80
CHEMBL2398486 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2398484 Ki = 34.0 nM 7.47
CHEMBL2398482 Ki = 34.0 nM 7.47
CHEMBL2398483 Ki = 53.0 nM 7.28
CHEMBL197669 ST1535 Ki = 100.0 nM 7.00
CHEMBL2398485 Ki = 150.0 nM 6.82
CHEMBL2398480 Ki = 160.0 nM 6.80
CHEMBL2398486 Ki = 200.0 nM 6.70