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Assay Detail

CHEMBL644508

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Functional
Inhibitory concentration as antagonistic activity against cAMP generation inhibited by IB-MECA in CHO cell membranes transfected with human A3 receptor
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 Expert

Target

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

Publication

Pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine derivatives as highly potent and selective human A(3) adenosine receptor antagonists.
Baraldi PG, Cacciari B, Romagnoli R, Spalluto G, Klotz KN, Leung E, Varani K, Gessi S, Merighi S, Borea PA.
J Med Chem (1999) 42 : 4473 -4478
PubMed 10579811 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 4 8.02 8.28

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL138332 1 8.28
CHEMBL65271 1 8.19
CHEMBL422820 1 7.91
CHEMBL139182 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL138332 IC50 = 5.3 nM 8.28
CHEMBL65271 IC50 = 6.5 nM 8.19
CHEMBL422820 IC50 = 12.4 nM 7.91
CHEMBL139182 IC50 = 19.81 nM 7.70