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Assay Detail

CHEMBL641302

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

Binding
Displacement of [3H]CGS-21680 from Adenosine A2A receptor of rat striatal membrane at 10e-4 uM
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Chiral resolution and stereospecificity of 6-phenyl-4-phenylethynyl- 1,4-dihydropyridines as selective A(3) adenosine receptor antagonists.
Jiang J, Li AH, Jang SY, Chang L, Melman N, Moro S, Ji X, Lobkovsky EB, Clardy JC, Jacobson KA.
J Med Chem (1999) 42 : 3055 -3065
PubMed 10447949 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 5 4.61 5.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL315984 1 5.32
CHEMBL105672 1 4.46
CHEMBL283013 1 4.06
CHEMBL405355 NIGULDIPINE 2.0 1 -
CHEMBL2051956 DEXNIGULDIPINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL315984 Ki = 4770.0 nM 5.32
CHEMBL105672 Ki = 35100.0 nM 4.46
CHEMBL283013 Ki = 86300.0 nM 4.06
CHEMBL405355 NIGULDIPINE Ki > 100000.0 nM -
CHEMBL2051956 DEXNIGULDIPINE Ki > 100000.0 nM -