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Assay Detail

CHEMBL1056089

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

Binding
Displacement of [3H]NECA from human recombinant adenosine A2A receptor expressed in CHO cells
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Intermediate

Target

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

Publication

Synthesis and biological evaluation of 2-alkynyl-N6-methyl-5'-N-methylcarboxamidoadenosine derivatives as potent and highly selective agonists for the human adenosine A3 receptor.
Volpini R, Buccioni M, Dal Ben D, Lambertucci C, Lammi C, Marucci G, Ramadori AT, Klotz KN, Cristalli G.
J Med Chem (2009) 52 : 7897 -7900
PubMed 19839592 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 4.79 5.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL573032 1 5.15
CHEMBL573950 1 4.98
CHEMBL573269 1 4.90
CHEMBL221206 1 4.79
CHEMBL223514 1 4.75
CHEMBL427077 1 4.73
CHEMBL575027 1 4.61
CHEMBL574602 1 4.38

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL573032 Ki = 7030.0 nM 5.15
CHEMBL573950 Ki = 10400.0 nM 4.98
CHEMBL573269 Ki = 12700.0 nM 4.90
CHEMBL221206 Ki = 16300.0 nM 4.79
CHEMBL223514 Ki = 18000.0 nM 4.75
CHEMBL427077 Ki = 18700.0 nM 4.73
CHEMBL575027 Ki = 24300.0 nM 4.61
CHEMBL574602 Ki = 41700.0 nM 4.38