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Assay Detail

CHEMBL2014361

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

Binding
Displacement of [3H]CGS21680 from human recombinant adenosine receptor-2A expressed in HEK293 cell membrane after 60 mins by liquid scintillation counting
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

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

Publication

Truncated (N)-Methanocarba Nucleosides as A(1) Adenosine Receptor Agonists and Partial Agonists: Overcoming Lack of a Recognition Element.
Tosh DK, Phan K, Deflorian F, Wei Q, Gao ZG, Jacobson KA.
ACS Med Chem Lett (2011) 2 : 626 -631
PubMed 21858244 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 5.43 5.61

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2012678 1 5.61
CHEMBL2012675 1 5.57
CHEMBL2012674 1 5.52
CHEMBL2012672 1 5.50
CHEMBL2012683 1 5.43
CHEMBL2012673 1 5.43
CHEMBL2012676 1 5.41
CHEMBL2012686 1 5.40
CHEMBL2012679 1 5.39
CHEMBL2012684 1 5.36
CHEMBL2012693 1 5.12

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2012678 Ki = 2450.0 nM 5.61
CHEMBL2012675 Ki = 2720.0 nM 5.57
CHEMBL2012674 Ki = 3020.0 nM 5.52
CHEMBL2012672 Ki = 3140.0 nM 5.50
CHEMBL2012683 Ki = 3700.0 nM 5.43
CHEMBL2012673 Ki = 3700.0 nM 5.43
CHEMBL2012676 Ki = 3930.0 nM 5.41
CHEMBL2012686 Ki = 3950.0 nM 5.40
CHEMBL2012679 Ki = 4080.0 nM 5.39
CHEMBL2012684 Ki = 4410.0 nM 5.36
CHEMBL2012693 Ki = 7510.0 nM 5.12