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Assay Detail

CHEMBL839688

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

Binding
Inhibition of [3H]NECA binding to human adenosine A3 receptor expressed in HeLa cells
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

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

Publication

Synthesis and biological activity of new potential agonists for the human adenosine A2A receptor.
Bosch MP, Campos F, Niubó I, Rosell G, Díaz JL, Brea J, Loza MI, Guerrero A.
J Med Chem (2004) 47 : 4041 -4053
PubMed 15267242 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 9 7.04 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL464859 NECA 1 8.40
CHEMBL331372 CGS-21680 1 7.17
CHEMBL361925 1 7.08
CHEMBL186113 GW-328267 1.0 1 7.04
CHEMBL2096798 1 7.00
CHEMBL368880 1 6.89
CHEMBL360837 1 6.85
CHEMBL360646 1 6.54
CHEMBL186403 1 6.40

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL464859 NECA Ki = 4.0 nM 8.40
CHEMBL331372 CGS-21680 Ki = 68.0 nM 7.17
CHEMBL361925 Ki = 83.0 nM 7.08
CHEMBL186113 GW-328267 Ki = 92.0 nM 7.04
CHEMBL2096798 Ki = 100.0 nM 7.00
CHEMBL368880 Ki = 130.0 nM 6.89
CHEMBL360837 Ki = 140.0 nM 6.85
CHEMBL360646 Ki = 288.0 nM 6.54
CHEMBL186403 Ki = 400.0 nM 6.40