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Assay Detail

CHEMBL4371644

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Binding
Agonist activity at human adenosine A3 receptor expressed in FlpIn-CHO cells assessed as increase in ERK1/2 phosphorylation after 5 mins by alphascreen assay
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Biased Ligands of G Protein-Coupled Receptors (GPCRs): Structure-Functional Selectivity Relationships (SFSRs) and Therapeutic Potential.
Tan L, Yan W, McCorvy JD, Cheng J.
J Med Chem (2018) 61 : 9841 -9878
PubMed 29939744 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 8.09 9.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4464176 1 9.80
CHEMBL119709 IB-MECA 1 9.60
CHEMBL2064653 1 9.30
CHEMBL2064657 1 8.10
CHEMBL2064660 1 7.60
CHEMBL2064661 1 6.20
CHEMBL2064634 1 6.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4464176 EC50 = 0.1585 nM 9.80
CHEMBL119709 IB-MECA EC50 = 0.2512 nM 9.60
CHEMBL2064653 EC50 = 0.5012 nM 9.30
CHEMBL2064657 EC50 = 7.943 nM 8.10
CHEMBL2064660 EC50 = 25.12 nM 7.60
CHEMBL2064661 EC50 = 630.96 nM 6.20
CHEMBL2064634 EC50 = 1000.0 nM 6.00