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Assay Detail

CHEMBL839608

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

Binding
Inhibition of [3H]DPCPX binding to human adenosine A2B receptor expressed in HEK293 cells
9
Total Activities
9
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 Expert

Target

Adenosine receptor A2b (CHEMBL255)
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 5.80 6.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL360837 1 6.21
CHEMBL464859 NECA 1 6.12
CHEMBL368880 1 5.93
CHEMBL186113 GW-328267 1.0 1 5.89
CHEMBL361925 1 5.65
CHEMBL360646 1 5.57
CHEMBL2096798 1 5.56
CHEMBL186403 1 5.44
CHEMBL331372 CGS-21680 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL360837 Ki = 624.0 nM 6.21
CHEMBL464859 NECA Ki = 760.0 nM 6.12
CHEMBL368880 Ki = 1183.0 nM 5.93
CHEMBL186113 GW-328267 Ki = 1300.0 nM 5.89
CHEMBL361925 Ki = 2261.0 nM 5.65
CHEMBL360646 Ki = 2715.0 nM 5.57
CHEMBL2096798 Ki = 2780.0 nM 5.56
CHEMBL186403 Ki = 3660.0 nM 5.44
CHEMBL331372 CGS-21680 Ki > 10000.0 nM -