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Assay Detail

CHEMBL901023

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Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as inhibition of forskolin-stimulated cAMP accumulation
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.
Da Settimo F, Primofiore G, Taliani S, Marini AM, La Motta C, Simorini F, Salerno S, Sergianni V, Tuccinardi T, Martinelli A, Cosimelli B, Greco G, Novellino E, Ciampi O, Trincavelli ML, Martini C.
J Med Chem (2007) 50 : 5676 -5684
PubMed 17927167 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.40 9.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL400812 1 9.24
CHEMBL235513 1 8.50
CHEMBL235717 1 7.93
CHEMBL193141 1 7.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL400812 IC50 = 0.58 nM 9.24
CHEMBL235513 IC50 = 3.14 nM 8.50
CHEMBL235717 IC50 = 11.61 nM 7.93
CHEMBL193141 IC50 = 12.0 nM 7.92