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Assay Detail

CHEMBL641037

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

Binding
Binding of 1 nM [3H]CHA to Adenosine A1 receptor of rat cerebral cortical membranes
6
Total Activities
6
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Benzo[1,2-c:5,4-c']dipyrazoles: non-xanthine adenosine antagonists.
Peet NP, Dickerson GA, Abdallah AH, Daly JW, Ukena D.
J Med Chem (1988) 31 : 2034 -2039
PubMed 3172141 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 6 5.47 6.30

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL26350 1 6.30
CHEMBL157655 1 6.16
CHEMBL416013 1 5.48
CHEMBL1250 1-METHYLXANTHINE 1 5.05
CHEMBL286785 1 5.00
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL26350 Ki = 500.0 nM 6.30
CHEMBL157655 Ki = 700.0 nM 6.16
CHEMBL416013 Ki = 3300.0 nM 5.48
CHEMBL1250 1-METHYLXANTHINE Ki = 9000.0 nM 5.05
CHEMBL286785 Ki = 10000.0 nM 5.00
CHEMBL1355736 THEOPHYLLINE Ki = 14000.0 nM 4.85