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Assay Detail

CHEMBL642192

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

Binding
Displacement of [3H]R-PIA from Adenosine A1 receptor of rat brain membrane
4
Total Activities
4
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 A1 (CHEMBL318)
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 4 4.79 5.17

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112436 1 5.17
CHEMBL2111655 1 4.83
CHEMBL2051956 DEXNIGULDIPINE 2.0 1 4.38
CHEMBL405355 NIGULDIPINE 2.0 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112436 Ki = 6830.0 nM 5.17
CHEMBL2111655 Ki = 14800.0 nM 4.83
CHEMBL2051956 DEXNIGULDIPINE Ki = 41300.0 nM 4.38
CHEMBL405355 NIGULDIPINE Ki > 100000.0 nM -