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Assay Detail

CHEMBL643298

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

Binding
Inhibitory activity against cyclic AMP production in rat Adenosine A1 receptor assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

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
IC50 2 7.49 7.76

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL440115 FK453 1.0 1 7.76
CHEMBL27508 1 7.21

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL440115 FK453 IC50 = 17.2 nM 7.76
CHEMBL27508 IC50 = 62.0 nM 7.21