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Assay Detail

CHEMBL640299

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Functional
G-protein activation in human Adenosine A2A receptor expressed in CHO cells using cAMP assay
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type CHO
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,5'-Disubstituted adenosine derivatives: evaluation of selectivity and efficacy for the adenosine A(1), A(2A), and A(3) receptor.
van Tilburg EW, von Frijtag Drabbe Kunzel J, de Groote M, IJzerman AP.
J Med Chem (2002) 45 : 420 -429
PubMed 11784146 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 11 5.77 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL319387 1 8.00
CHEMBL2113605 1 6.30
CHEMBL2113595 1 6.16
CHEMBL2113604 1 6.10
CHEMBL2113592 1 5.96
CHEMBL2113601 1 5.44
CHEMBL2113588 1 5.30
CHEMBL2113519 1 5.27
CHEMBL2113580 1 5.12
CHEMBL2113606 1 4.98
CHEMBL2113581 1 4.89

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL319387 EC50 = 10.0 nM 8.00
CHEMBL2113605 EC50 = 500.0 nM 6.30
CHEMBL2113595 EC50 = 700.0 nM 6.16
CHEMBL2113604 EC50 = 800.0 nM 6.10
CHEMBL2113592 EC50 = 1100.0 nM 5.96
CHEMBL2113601 EC50 = 3600.0 nM 5.44
CHEMBL2113588 EC50 = 5000.0 nM 5.30
CHEMBL2113519 EC50 = 5400.0 nM 5.27
CHEMBL2113580 EC50 = 7500.0 nM 5.12
CHEMBL2113606 EC50 = 10400.0 nM 4.98
CHEMBL2113581 EC50 = 12900.0 nM 4.89