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Assay Detail

CHEMBL798536

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

Functional
Antagonist binding of 2-chloro-[3H]-adenosine to rat brain
11
Total Activities
8
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Rattus norvegicus
Confidence 5 — Multiple protein complex / RNA
Curated By Expert

Target

Adenosine receptor (CHEMBL2111386)
Type PROTEIN FAMILY
Organism Rattus norvegicus

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 11 6.81 9.22

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL139000 (R)-PIA 1 9.22
CHEMBL261482 1 8.26
CHEMBL285819 1 8.00
CHEMBL420705 (S)-PIA 1 7.82
CHEMBL275084 ISOBUTYLMETHYLXANTHINE 3 7.30
CHEMBL1355736 THEOPHYLLINE 4.0 2 6.82
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 6.30
CHEMBL113 CAFFEINE 4.0 1 4.82

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL139000 (R)-PIA Ki = 0.6 nM 9.22
CHEMBL261482 Ki = 5.5 nM 8.26
CHEMBL285819 Ki = 10.0 nM 8.00
CHEMBL420705 (S)-PIA Ki = 15.0 nM 7.82
CHEMBL275084 ISOBUTYLMETHYLXANTHINE Ki = 50.0 nM 7.30
CHEMBL1355736 THEOPHYLLINE Ki = 150.0 nM 6.82
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 500.0 nM 6.30
CHEMBL275084 ISOBUTYLMETHYLXANTHINE Ki = 2000.0 nM 5.70
CHEMBL1355736 THEOPHYLLINE Ki = 4500.0 nM 5.35
CHEMBL275084 ISOBUTYLMETHYLXANTHINE Ki = 5000.0 nM 5.30
CHEMBL113 CAFFEINE Ki = 15000.0 nM 4.82