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Assay Detail

CHEMBL645502

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Functional
Vasorelaxation as Adenosine A2A receptor activity in rat aorta
14
Total Activities
14
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Tissue Aorta
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

2-alkenyl and 2-alkyl derivatives of adenosine and adenosine-5'-N-ethyluronamide: different affinity and selectivity of E- and Z-diastereomers at A2A adenosine receptors.
Vittori S, Camaioni E, Di Francesco E, Volpini R, Monopoli A, Dionisotti S, Ongini E, Cristalli G.
J Med Chem (1996) 39 : 4211 -4217
PubMed 8863798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 6.71 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113529 1 9.00
CHEMBL319387 1 7.10
CHEMBL2113526 1 6.71
CHEMBL464859 NECA 1 6.41
CHEMBL2113450 1 6.30
CHEMBL2304158 1 6.24
CHEMBL2113528 1 6.23
CHEMBL410873 1 6.22
CHEMBL611256 1 6.17
CHEMBL608918 1 -
CHEMBL98603 1 -
CHEMBL223270 1 -
CHEMBL2113527 1 -
CHEMBL2113525 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113529 EC50 = 1.0 nM 9.00
CHEMBL319387 EC50 = 79.2 nM 7.10
CHEMBL2113526 EC50 = 194.0 nM 6.71
CHEMBL464859 NECA EC50 = 394.0 nM 6.41
CHEMBL2113450 EC50 = 497.0 nM 6.30
CHEMBL2304158 EC50 = 576.0 nM 6.24
CHEMBL2113528 EC50 = 594.0 nM 6.23
CHEMBL410873 EC50 = 596.0 nM 6.22
CHEMBL611256 EC50 = 676.0 nM 6.17
CHEMBL608918 EC50 - nM -
CHEMBL98603 EC50 - nM -
CHEMBL223270 EC50 > 1.0 nM -
CHEMBL2113527 EC50 - nM -
CHEMBL2113525 EC50 > 1.0 nM -