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Assay Detail

CHEMBL870067

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Functional
Activity against human adenosine A3 receptor H272E mutant expressed in COS7 cells as measured by accumulation of inositol phosphate by PLC assay
4
Total Activities
4
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type COS-7
Confidence 9 — Direct single protein target
Curated By Expert

Target

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

Publication

Orthogonal activation of the reengineered A3 adenosine receptor (neoceptor) using tailored nucleoside agonists.
Gao ZG, Duong HT, Sonina T, Kim SK, Van Rompaey P, Van Calenbergh S, Mamedova L, Kim HO, Kim MJ, Kim AY, Liang BT, Jeong LS, Jacobson KA.
J Med Chem (2006) 49 : 2689 -2702
PubMed 16640329 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 2 5.87 6.75
Activity 2 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL382194 1 6.75
CHEMBL464859 NECA 1 4.98
CHEMBL377071 1 -
CHEMBL2113221 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL382194 EC50 = 180.0 nM 6.75
CHEMBL464859 NECA EC50 = 10400.0 nM 4.98
CHEMBL377071 Activity - -
CHEMBL2113221 Activity - -