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Assay Detail

CHEMBL1073402

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

Binding
Displacement of radioligand from human adenosine A3 receptor expressed in cells by topcount microplate scintillation counting
7
Total Activities
7
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Antagonists of the human A(2A) receptor. Part 6: Further optimization of pyrimidine-4-carboxamides.
Gillespie RJ, Bamford SJ, Clay A, Gaur S, Haymes T, Jackson PS, Jordan AM, Klenke B, Leonardi S, Liu J, Mansell HL, Ng S, Saadi M, Simmonite H, Stratton GC, Todd RS, Williamson DS, Yule IA.
Bioorg Med Chem (2009) 17 : 6590 -6605
PubMed 19695884 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 7 5.87 6.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL609578 1 6.44
CHEMBL603748 1 6.13
CHEMBL608383 1 6.05
CHEMBL594136 1 5.94
CHEMBL594455 1 5.79
CHEMBL594363 1 5.68
CHEMBL596308 1 5.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL609578 Ki = 366.0 nM 6.44
CHEMBL603748 Ki = 741.0 nM 6.13
CHEMBL608383 Ki = 896.0 nM 6.05
CHEMBL594136 Ki = 1150.0 nM 5.94
CHEMBL594455 Ki = 1627.0 nM 5.79
CHEMBL594363 Ki = 2104.0 nM 5.68
CHEMBL596308 Ki = 9090.0 nM 5.04