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Assay Detail

CHEMBL4322685

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Functional
Agonist activity at wild type human A3 receptor V169'5.30E mutant stably expressed in Flp-In CHO cells cotransfected with pOG44 assessed as inhibition of forskolin-induced cAMP accumulation measured after 30 mins by LANCE assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Structural Characterization of Agonist Binding to an A<sub>3</sub> Adenosine Receptor through Biomolecular Simulations and Mutagenesis Experiments.
Stamatis D, Lagarias P, Barkan K, Vrontaki E, Ladds G, Kolocouris A.
J Med Chem (2019) 62 : 8831 -8846
PubMed 31502843 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 9.68 9.68

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 9.68
CHEMBL119709 IB-MECA 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA IC50 = 0.2089 nM 9.68
CHEMBL119709 IB-MECA IC50 = 0.003311 nM -