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Assay Detail

CHEMBL2072278

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

Binding
Displacement of 3[H]CGS21680 from rat A2A adenosine receptor expressed in HEK293 cells after 60 min by Liquid scintillation analysis
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Optimization of adenosine 5'-carboxamide derivatives as adenosine receptor agonists using structure-based ligand design and fragment screening.
Tosh DK, Phan K, Gao ZG, Gakh AA, Xu F, Deflorian F, Abagyan R, Stevens RC, Jacobson KA, Katritch V.
J Med Chem (2012) 55 : 4297 -4308
PubMed 22486652 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 6.85 7.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 7.92
CHEMBL261482 1 7.92
CHEMBL2070398 1 6.39
CHEMBL2070399 1 6.39
CHEMBL1235128 1 6.26
CHEMBL2070508 1 6.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA Ki = 12.0 nM 7.92
CHEMBL261482 Ki = 12.0 nM 7.92
CHEMBL2070398 Ki = 405.0 nM 6.39
CHEMBL2070399 Ki = 410.0 nM 6.39
CHEMBL1235128 Ki = 550.0 nM 6.26
CHEMBL2070508 Ki = 610.0 nM 6.21