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Assay Detail

CHEMBL641723

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Binding
Evaluated for the binding affinity towards the Adenosine A1 receptor in corpora striata of rats using [3H]CHA as radioligand.
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

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

Publication

4-Amino[1,2,4]triazolo[4,3-a]quinoxalines. A novel class of potent adenosine receptor antagonists and potential rapid-onset antidepressants.
Sarges R, Howard HR, Browne RG, Lebel LA, Seymour PA, Koe BK.
J Med Chem (1990) 33 : 2240 -2254
PubMed 2374150 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 8.19 9.23

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE 1 9.23
CHEMBL139000 (R)-PIA 1 8.52
CHEMBL262083 N6-PHENYLADENOSINE 1 8.52
CHEMBL477 ADENOSINE 4.0 1 8.00
CHEMBL420705 (S)-PIA 1 6.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL68738 N6-CYCLOPENTYLADENOSINE Ki = 0.589 nM 9.23
CHEMBL139000 (R)-PIA Ki = 3.0 nM 8.52
CHEMBL262083 N6-PHENYLADENOSINE Ki = 3.0 nM 8.52
CHEMBL477 ADENOSINE Ki = 10.0 nM 8.00
CHEMBL420705 (S)-PIA Ki = 200.0 nM 6.70