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Assay Detail

CHEMBL922121

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Functional
Agonist activity at adenosine A1 receptor assessed as inhibition of isoproterenol-stimulated cAMP accumulation in DDT1MF-2 cells
21
Total Activities
21
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Cell Type DDT1MF-2
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

N6-substituted C5'-modified adenosines as A1 adenosine receptor agonists.
Ashton TD, Baker SP, Hutchinson SA, Scammells PJ.
Bioorg Med Chem (2008) 16 : 1861 -1873
PubMed 18042389 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 21 7.41 9.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL411245 1 9.92
CHEMBL258759 1 9.52
CHEMBL410288 1 9.05
CHEMBL427737 1 8.59
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 8.57
CHEMBL262604 1 8.15
CHEMBL412104 1 7.92
CHEMBL258972 1 7.82
CHEMBL263643 1 7.68
CHEMBL258760 1 7.68
CHEMBL260631 1 7.55
CHEMBL262876 1 7.32
CHEMBL258489 1 7.17
CHEMBL260205 1 6.65
CHEMBL265947 1 6.46
CHEMBL279161 1 6.39
CHEMBL262850 1 6.22
CHEMBL411859 1 6.15
CHEMBL442468 1 6.06
CHEMBL411463 1 5.37
CHEMBL411279 1 5.30

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL411245 IC50 = 0.12 nM 9.92
CHEMBL258759 IC50 = 0.3 nM 9.52
CHEMBL410288 IC50 = 0.9 nM 9.05
CHEMBL427737 IC50 = 2.6 nM 8.59
CHEMBL68738 N6-CYCLOPENTYLADENOSINE IC50 = 2.7 nM 8.57
CHEMBL262604 IC50 = 7.0 nM 8.15
CHEMBL412104 IC50 = 12.0 nM 7.92
CHEMBL258972 IC50 = 15.0 nM 7.82
CHEMBL263643 IC50 = 21.0 nM 7.68
CHEMBL258760 IC50 = 21.0 nM 7.68
CHEMBL260631 IC50 = 28.0 nM 7.55
CHEMBL262876 IC50 = 48.0 nM 7.32
CHEMBL258489 IC50 = 68.0 nM 7.17
CHEMBL260205 IC50 = 224.0 nM 6.65
CHEMBL265947 IC50 = 351.0 nM 6.46
CHEMBL279161 IC50 = 410.0 nM 6.39
CHEMBL262850 IC50 = 605.0 nM 6.22
CHEMBL411859 IC50 = 710.0 nM 6.15
CHEMBL442468 IC50 = 867.0 nM 6.06
CHEMBL411463 IC50 = 4279.0 nM 5.37
CHEMBL411279 IC50 = 4950.0 nM 5.30