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Assay Detail

CHEMBL642373

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

Binding
Displacement of [125 I]AB-MECA from adenosine A3 receptor in bovine cortical membranes with 20 nM DPCPX
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.
Da Settimo F, Primofiore G, Taliani S, Marini AM, La Motta C, Novellino E, Greco G, Lavecchia A, Trincavelli L, Martini C.
J Med Chem (2001) 44 : 316 -327
PubMed 11462973 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 8.40 9.66

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL307199 1 9.66
CHEMBL464859 NECA 1 7.14
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL307199 Ki = 0.22 nM 9.66
CHEMBL464859 NECA Ki = 73.0 nM 7.14
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki > 10000.0 nM -