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Assay Detail

CHEMBL646667

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Functional
Stimulation of [35S]GTP-gamma-S, binding to human adenosine A1 receptor
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Methanocarba analogues of purine nucleosides as potent and selective adenosine receptor agonists.
Jacobson KA, Ji X, Li AH, Melman N, Siddiqui MA, Shin KJ, Marquez VE, Ravi RG.
J Med Chem (2000) 43 : 2196 -2203
PubMed 10841798 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 7 7.41 8.38

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 8.38
CHEMBL27952 1 7.67
CHEMBL284216 1 7.51
CHEMBL66393 1 7.37
CHEMBL27809 1 6.85
CHEMBL417292 1 6.66
CHEMBL71385 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE EC50 = 4.15 nM 8.38
CHEMBL27952 EC50 = 21.5 nM 7.67
CHEMBL284216 EC50 = 31.2 nM 7.51
CHEMBL66393 EC50 = 43.1 nM 7.37
CHEMBL27809 EC50 = 142.0 nM 6.85
CHEMBL417292 EC50 = 218.0 nM 6.66
CHEMBL71385 EC50 > 10000.0 nM -