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Assay Detail

CHEMBL641571

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

Binding
Binding Affinity for adenosine A2A receptor expressed in HEK293 cells compared to [3H]CGS-21680
3
Total Activities
3
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 Expert

Target

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

Publication

2-Alkynyl-8-aryl-9-methyladenines as novel adenosine receptor antagonists: their synthesis and structure-activity relationships toward hepatic glucose production induced via agonism of the A(2B) receptor.
Harada H, Asano O, Hoshino Y, Yoshikawa S, Matsukura M, Kabasawa Y, Niijima J, Kotake Y, Watanabe N, Kawata T, Inoue T, Horizoe T, Yasuda N, Minami H, Nagata K, Murakami M, Nagaoka J, Kobayashi S, Tanaka I, Abe S.
J Med Chem (2001) 44 : 170 -179
PubMed 11170626 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.52 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL27508 1 7.15
CHEMBL440115 FK453 1.0 1 5.89
CHEMBL52735 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL27508 Ki = 71.0 nM 7.15
CHEMBL440115 FK453 Ki = 1300.0 nM 5.89
CHEMBL52735 Ki > 10000.0 nM -