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Assay Detail

CHEMBL1024509

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 by liquid scintillation counting
8
Total Activities
8
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 Intermediate

Target

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

Publication

Structure-activity relationships of truncated adenosine derivatives as highly potent and selective human A3 adenosine receptor antagonists.
Pal S, Choi WJ, Choe SA, Heller CL, Gao ZG, Chinn M, Jacobson KA, Hou X, Lee SK, Kim HO, Jeong LS.
Bioorg Med Chem (2009) 17 : 3733 -3738
PubMed 19375920 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 5.79 6.65

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL200732 1 6.65
CHEMBL413686 1 6.47
CHEMBL549352 1 6.00
CHEMBL561855 1 5.85
CHEMBL564676 1 5.47
CHEMBL549563 1 5.44
CHEMBL431733 NAMODENOSON 3.0 1 5.27
CHEMBL564883 1 5.18

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL200732 Ki = 223.0 nM 6.65
CHEMBL413686 Ki = 341.0 nM 6.47
CHEMBL549352 Ki = 997.0 nM 6.00
CHEMBL561855 Ki = 1400.0 nM 5.85
CHEMBL564676 Ki = 3410.0 nM 5.47
CHEMBL549563 Ki = 3630.0 nM 5.44
CHEMBL431733 NAMODENOSON Ki = 5400.0 nM 5.27
CHEMBL564883 Ki = 6560.0 nM 5.18