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Assay Detail

CHEMBL643483

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

Binding
Binding affinity at A1 adenosine receptor in rat brain cortical membrane using [3H]- N6-R-phenylisopropyladenosine (R-PIA)
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis of paraxanthine analogs (1,7-disubstituted xanthines) and other xanthines unsubstituted at the 3-position: structure-activity relationships at adenosine receptors.
Müller CE, Shi D, Manning M, Daly JW.
J Med Chem (1993) 36 : 3341 -3349
PubMed 8230124 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.65 7.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL325959 1 7.17
CHEMBL274855 1 7.17
CHEMBL285191 1 5.60

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL325959 Ki = 68.0 nM 7.17
CHEMBL274855 Ki = 67.0 nM 7.17
CHEMBL285191 Ki = 2500.0 nM 5.60