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Assay Detail

CHEMBL645500

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Functional activity at Adenosine A2A receptor as vasorelaxation of 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-[N'-(3-arylallylidene)hydrazino]adenosines showing A2a adenosine agonist properties and vasodilation activity.
Viziano M, Ongini E, Conti A, Zocchi C, Seminati M, Pocar D.
J Med Chem (1995) 38 : 3581 -3585
PubMed 7658444 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 14 6.36 6.94

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL331372 CGS-21680 1 6.94
CHEMBL2113564 1 6.71
CHEMBL2113563 1 6.57
CHEMBL2113559 1 6.55
CHEMBL464859 NECA 1 6.41
CHEMBL2113556 1 6.32
CHEMBL2113554 1 6.28
CHEMBL2113558 1 6.20
CHEMBL2113560 1 6.17
CHEMBL2113552 1 6.15
CHEMBL2113553 1 6.14
CHEMBL611571 1 6.13
CHEMBL2113555 1 6.10
CHEMBL284969 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL331372 CGS-21680 EC50 = 115.0 nM 6.94
CHEMBL2113564 EC50 = 195.0 nM 6.71
CHEMBL2113563 EC50 = 269.0 nM 6.57
CHEMBL2113559 EC50 = 281.0 nM 6.55
CHEMBL464859 NECA EC50 = 394.0 nM 6.41
CHEMBL2113556 EC50 = 482.0 nM 6.32
CHEMBL2113554 EC50 = 529.0 nM 6.28
CHEMBL2113558 EC50 = 638.0 nM 6.20
CHEMBL2113560 EC50 = 677.0 nM 6.17
CHEMBL2113552 EC50 = 704.0 nM 6.15
CHEMBL2113553 EC50 = 728.0 nM 6.14
CHEMBL611571 EC50 = 747.0 nM 6.13
CHEMBL2113555 EC50 = 800.0 nM 6.10
CHEMBL284969 EC50 > 10000.0 nM -