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Assay Detail

CHEMBL951866

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

Functional
Antagonist activity at human adenosine A3 receptor expressed in CHO cells assessed as reversal of NECA-mediated inhibition of forskolin-induced 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 Autocuration

Target

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

Publication

Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.
Cosimelli B, Greco G, Ehlardo M, Novellino E, Da Settimo F, Taliani S, La Motta C, Bellandi M, Tuccinardi T, Martinelli A, Ciampi O, Trincavelli ML, Martini C.
J Med Chem (2008) 51 : 1764 -1770
PubMed 18269230 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.56 8.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL429131 1 8.90
CHEMBL272795 1 8.73
CHEMBL402848 1 8.57
CHEMBL270676 1 8.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL429131 IC50 = 1.25 nM 8.90
CHEMBL272795 IC50 = 1.84 nM 8.73
CHEMBL402848 IC50 = 2.7 nM 8.57
CHEMBL270676 IC50 = 9.2 nM 8.04