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Assay Detail

CHEMBL642987

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

Binding
Binding affinity towards adenosine A1 receptor in rat whole brain membranes using N6-[3H]cyclohexyladenosine
4
Total Activities
4
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Adenosine A1 antagonists. 2. Structure-activity relationships on diuretic activities and protective effects against acute renal failure.
Suzuki F, Shimada J, Mizumoto H, Karasawa A, Kubo K, Nonaka H, Ishii A, Kawakita T.
J Med Chem (1992) 35 : 3066 -3075
PubMed 1501234 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 4 8.06 9.34

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 9.34
CHEMBL268071 1 8.14
CHEMBL16687 CGS-15943 1 7.69
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 7.07

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 0.46 nM 9.34
CHEMBL268071 Ki = 7.3 nM 8.14
CHEMBL16687 CGS-15943 Ki = 20.5 nM 7.69
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 86.0 nM 7.07