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Assay Detail

CHEMBL2067494

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

Binding
Displacement of [3H]CGS21680 from human recombinant adenosine A2A receptor expressed in HEK293 cells after 60 mins by liquid scintillation counting
6
Total Activities
6
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-guided design of A(3) adenosine receptor-selective nucleosides: combination of 2-arylethynyl and bicyclo[3.1.0]hexane substitutions.
Tosh DK, Deflorian F, Phan K, Gao ZG, Wan TC, Gizewski E, Auchampach JA, Jacobson KA.
J Med Chem (2012) 55 : 4847 -4860
PubMed 22559880 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.55 5.90

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2064641 1 5.90
CHEMBL2064656 1 5.76
CHEMBL175543 1 5.64
CHEMBL2064661 1 5.51
CHEMBL2064649 1 5.28
CHEMBL280580 1 5.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2064641 Ki = 1270.0 nM 5.90
CHEMBL2064656 Ki = 1740.0 nM 5.76
CHEMBL175543 Ki = 2300.0 nM 5.64
CHEMBL2064661 Ki = 3110.0 nM 5.51
CHEMBL2064649 Ki = 5300.0 nM 5.28
CHEMBL280580 Ki = 6200.0 nM 5.21