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Assay Detail

CHEMBL2417040

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Binding
Competitive binding affinity to human adenosine A2A receptor expressed in HEK293 cells after 60 mins by fluorescence polarization assay in presence of MRS5346
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

Fluorescent ligands for adenosine receptors.
Kozma E, Jayasekara PS, Squarcialupi L, Paoletta S, Moro S, Federico S, Spalluto G, Jacobson KA.
Bioorg Med Chem Lett (2013) 23 : 26 -36
PubMed 23200243 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.11 8.89

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL113142 ZM-241385 1 8.89
CHEMBL17127 SCH-58261 1 8.72
CHEMBL273094 XANTHINE AMINE CONGENER 1 8.43
CHEMBL136689 1 7.96
CHEMBL464859 NECA 1 7.67
CHEMBL2391907 1 7.56
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.20
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 6.09
CHEMBL1355736 THEOPHYLLINE 4.0 1 5.69
CHEMBL113 CAFFEINE 4.0 1 5.61
CHEMBL431733 NAMODENOSON 3.0 1 5.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL113142 ZM-241385 Ki = 1.3 nM 8.89
CHEMBL17127 SCH-58261 Ki = 1.9 nM 8.72
CHEMBL273094 XANTHINE AMINE CONGENER Ki = 3.7 nM 8.43
CHEMBL136689 Ki = 11.1 nM 7.96
CHEMBL464859 NECA Ki = 21.2 nM 7.67
CHEMBL2391907 Ki = 27.3 nM 7.56
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 630.0 nM 6.20
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 814.0 nM 6.09
CHEMBL1355736 THEOPHYLLINE Ki = 2030.0 nM 5.69
CHEMBL113 CAFFEINE Ki = 2480.0 nM 5.61
CHEMBL431733 NAMODENOSON Ki = 3720.0 nM 5.43