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Assay Detail

CHEMBL637554

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

Binding
Intrinsic activity towards Adenosine A1 receptor as displacement of [3H]DPCPX from bovine cortical membranes without GTP
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Bos taurus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL4975)
Type SINGLE PROTEIN
Organism Bos taurus

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 7.09 7.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL112756 1 7.61
CHEMBL7909 1 7.03
CHEMBL326752 1 6.62

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL112756 Ki = 24.7 nM 7.61
CHEMBL7909 Ki = 93.1 nM 7.03
CHEMBL326752 Ki = 240.0 nM 6.62