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Assay Detail

CHEMBL939482

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

Binding
Displacement of [3H]DPCPX form human adenosine A1 receptor expressed in HEK293 cells
3
Total Activities
3
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Cell Type HEK293
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A1 (CHEMBL226)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

2,6-Diaryl-4-acylaminopyrimidines as potent and selective adenosine A(2A) antagonists with improved solubility and metabolic stability.
Moorjani M, Luo Z, Lin E, Vong BG, Chen Y, Zhang X, Rueter JK, Gross RS, Lanier MC, Tellew JE, Williams JP, Lechner SM, Malany S, Santos M, Crespo MI, Díaz JL, Saunders J, Slee DH.
Bioorg Med Chem Lett (2008) 18 : 5402 -5405
PubMed 18835161 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 3 6.79 8.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL401321 1 8.04
CHEMBL251975 1 6.57
CHEMBL270761 1 5.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL401321 Ki = 9.2 nM 8.04
CHEMBL251975 Ki = 270.0 nM 6.57
CHEMBL270761 Ki = 1700.0 nM 5.77