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Assay Detail

CHEMBL3390251

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

Binding
Displacement of [3H]2-[p-(2-carboxyethyl)phenyl-ethylamino]-5'-N-ethylcarboxamidoadenosine from human adenosine A2a receptor expressed in HEK293 cells
5
Total Activities
5
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

Structure-Based Design of Reactive Nucleosides for Site-Specific Modification of the A2A Adenosine Receptor.
Moss SM, Jayasekara PS, Paoletta S, Gao ZG, Jacobson KA.
ACS Med Chem Lett (2014) 5 : 1043 -1048
PubMed 25221664 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 6.44 7.64

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3335523 1 7.64
CHEMBL331372 CGS-21680 1 7.16
CHEMBL3335526 1 6.57
CHEMBL3335525 1 5.48
CHEMBL3335524 1 5.36

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3335523 Ki = 23.0 nM 7.64
CHEMBL331372 CGS-21680 Ki = 70.0 nM 7.16
CHEMBL3335526 Ki = 267.0 nM 6.57
CHEMBL3335525 Ki = 3280.0 nM 5.48
CHEMBL3335524 Ki = 4360.0 nM 5.36