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Assay Detail

CHEMBL654355

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

Binding
Antagonist binding of N6-cyclohexyl-[3H]-adenosine to bovine brain
8
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL4975)
Type SINGLE PROTEIN
Organism Bos taurus

Publication

Adenosine receptors: targets for future drugs.
Daly JW.
J Med Chem (1982) 25 : 197 -207
PubMed 6279840 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 8 7.21 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139000 (R)-PIA 1 9.60
CHEMBL45891 1 8.60
CHEMBL420705 (S)-PIA 1 8.10
CHEMBL285819 1 7.60
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 6.70
CHEMBL275084 ISOBUTYLMETHYLXANTHINE 1 5.16
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.70
CHEMBL113 CAFFEINE 4.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139000 (R)-PIA Ki = 0.25 nM 9.60
CHEMBL45891 Ki = 2.5 nM 8.60
CHEMBL420705 (S)-PIA Ki = 8.0 nM 8.10
CHEMBL285819 Ki = 25.0 nM 7.60
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 200.0 nM 6.70
CHEMBL275084 ISOBUTYLMETHYLXANTHINE Ki = 7000.0 nM 5.16
CHEMBL1355736 THEOPHYLLINE Ki = 20000.0 nM 4.70
CHEMBL113 CAFFEINE Ki = 130000.0 nM -