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Assay Detail

CHEMBL640337

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

Functional
Prolongation of the stimulus-QRS interval by 50% of the maximum response at the Adenosine A1 receptor in langendorff guinea pig heart preparation
23
Total Activities
23
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Cavia porcellus
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A1 (CHEMBL2304404)
Type SINGLE PROTEIN
Organism Cavia porcellus

Publication

2-Alkoxyadenosines: potent and selective agonists at the coronary artery A2 adenosine receptor.
Ueeda M, Thompson RD, Arroyo LH, Olsson RA.
J Med Chem (1991) 34 : 1334 -1339
PubMed 2016707 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 23 5.17 8.27

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112181 1 8.27
CHEMBL605469 1 7.47
CHEMBL464859 NECA 1 7.20
CHEMBL1688963 ISOGUANOSINE 1 5.94
CHEMBL605879 1 5.66
CHEMBL603588 1 5.58
CHEMBL603373 1 5.35
CHEMBL605466 1 4.86
CHEMBL604429 1 4.80
CHEMBL604223 1 4.64
CHEMBL331372 CGS-21680 1 4.61
CHEMBL604009 1 4.45
CHEMBL603379 1 4.43
CHEMBL605464 1 4.34
CHEMBL603374 1 4.20
CHEMBL604224 1 4.18
CHEMBL604844 1 4.10
CHEMBL2311200 1 4.10
CHEMBL605472 1 4.00
CHEMBL605679 1 -
CHEMBL604838 1 -
CHEMBL606510 1 -
CHEMBL604426 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112181 EC50 = 5.37 nM 8.27
CHEMBL605469 EC50 = 33.88 nM 7.47
CHEMBL464859 NECA EC50 = 63.1 nM 7.20
CHEMBL1688963 ISOGUANOSINE EC50 = 1148.15 nM 5.94
CHEMBL605879 EC50 = 2187.76 nM 5.66
CHEMBL603588 EC50 = 2630.27 nM 5.58
CHEMBL603373 EC50 = 4466.84 nM 5.35
CHEMBL605466 EC50 = 13803.84 nM 4.86
CHEMBL604429 EC50 = 15848.93 nM 4.80
CHEMBL604223 EC50 = 22908.68 nM 4.64
CHEMBL331372 CGS-21680 EC50 = 24547.09 nM 4.61
CHEMBL604009 EC50 = 35481.34 nM 4.45
CHEMBL603379 EC50 = 37153.52 nM 4.43
CHEMBL605464 EC50 = 45708.82 nM 4.34
CHEMBL603374 EC50 = 63095.73 nM 4.20
CHEMBL604224 EC50 = 66069.34 nM 4.18
CHEMBL604844 EC50 = 79432.82 nM 4.10
CHEMBL2311200 EC50 = 79432.82 nM 4.10
CHEMBL605472 EC50 = 100000.0 nM 4.00
CHEMBL605679 EC50 = 891250.94 nM -
CHEMBL604838 EC50 = 107151.93 nM -
CHEMBL606510 EC50 = 147910.84 nM -
CHEMBL604426 EC50 = 223872.11 nM -