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Assay Detail

CHEMBL927307

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

Binding
Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells
12
Total Activities
12
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

5'-Carbamoyl derivatives of 2'-C-methyl-purine nucleosides as selective A1 adenosine receptor agonists: affinity, efficacy, and selectivity for A1 receptor from different species.
Cappellacci L, Franchetti P, Vita P, Petrelli R, Lavecchia A, Costa B, Spinetti F, Martini C, Klotz KN, Grifantini M.
Bioorg Med Chem (2008) 16 : 336 -353
PubMed 17933541 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 12 5.23 6.10

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.10
CHEMBL284969 1 5.64
CHEMBL252198 1 5.34
CHEMBL392149 TECADENOSON 2.0 1 5.19
CHEMBL399514 1 5.06
CHEMBL251997 1 5.02
CHEMBL400189 1 4.98
CHEMBL254064 1 4.98
CHEMBL254896 1 4.80
CHEMBL400782 1 -
CHEMBL400190 1 -
CHEMBL254693 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 794.0 nM 6.10
CHEMBL284969 Ki = 2300.0 nM 5.64
CHEMBL252198 Ki = 4590.0 nM 5.34
CHEMBL392149 TECADENOSON Ki = 6390.0 nM 5.19
CHEMBL399514 Ki = 8760.0 nM 5.06
CHEMBL251997 Ki = 9580.0 nM 5.02
CHEMBL400189 Ki = 10400.0 nM 4.98
CHEMBL254064 Ki = 10400.0 nM 4.98
CHEMBL254896 Ki = 15900.0 nM 4.80
CHEMBL400782 Ki > 100000.0 nM -
CHEMBL400190 Ki > 100000.0 nM -
CHEMBL254693 Ki > 100000.0 nM -