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Assay Detail

CHEMBL649127

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

Functional
Negative chronotropic activity via A2 Adenosine receptor was tested monitoring vasodilation in rat aorta
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Tissue Aorta
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117)
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

2-Alkynyl derivatives of adenosine-5'-N-ethyluronamide: selective A2 adenosine receptor agonists with potent inhibitory activity on platelet aggregation.
Cristalli G, Volpini R, Vittori S, Camaioni E, Monopoli A, Conti A, Dionisotti S, Zocchi C, Ongini E.
J Med Chem (1994) 37 : 1720 -1726
PubMed 8201607 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 21 6.47 7.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2113414 1 7.23
CHEMBL2113409 1 7.16
CHEMBL2113402 1 6.96
CHEMBL2094083 1 6.91
CHEMBL2113482 1 6.85
CHEMBL2113413 1 6.52
CHEMBL2113411 1 6.48
CHEMBL2113405 1 6.47
CHEMBL2113483 1 6.43
CHEMBL2113485 1 6.42
CHEMBL464859 NECA 1 6.41
CHEMBL2113407 1 6.41
CHEMBL2113449 1 6.36
CHEMBL2113399 1 6.34
CHEMBL2113403 1 6.25
CHEMBL410873 1 6.22
CHEMBL2113412 1 6.15
CHEMBL2113410 1 6.08
CHEMBL2113417 1 5.92
CHEMBL2113408 1 5.78
CHEMBL284969 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2113414 EC50 = 59.4 nM 7.23
CHEMBL2113409 EC50 = 69.3 nM 7.16
CHEMBL2113402 EC50 = 111.0 nM 6.96
CHEMBL2094083 EC50 = 123.0 nM 6.91
CHEMBL2113482 EC50 = 140.0 nM 6.85
CHEMBL2113413 EC50 = 300.0 nM 6.52
CHEMBL2113411 EC50 = 329.0 nM 6.48
CHEMBL2113405 EC50 = 338.0 nM 6.47
CHEMBL2113483 EC50 = 367.0 nM 6.43
CHEMBL2113485 EC50 = 382.0 nM 6.42
CHEMBL464859 NECA EC50 = 394.0 nM 6.41
CHEMBL2113407 EC50 = 391.0 nM 6.41
CHEMBL2113449 EC50 = 440.0 nM 6.36
CHEMBL2113399 EC50 = 456.0 nM 6.34
CHEMBL2113403 EC50 = 564.0 nM 6.25
CHEMBL410873 EC50 = 596.0 nM 6.22
CHEMBL2113412 EC50 = 715.0 nM 6.15
CHEMBL2113410 EC50 = 828.0 nM 6.08
CHEMBL2113417 EC50 = 1200.0 nM 5.92
CHEMBL2113408 EC50 = 1650.0 nM 5.78
CHEMBL284969 EC50 > 10000.0 nM -