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Assay Detail

CHEMBL644555

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Binding
Binding affinity for human adenosine A3 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 A3 (CHEMBL256)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Facile synthesis of fused 1,2,4-triazolo[1,5-c]pyrimidine derivatives as human adenosine A3 receptor ligands.
Okamura T, Kurogi Y, Hashimoto K, Nishikawa H, Nagao Y.
Bioorg Med Chem Lett (2004) 14 : 2443 -2446
PubMed 15109629 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.72 9.60

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122512 1 9.60
CHEMBL123705 1 9.21
CHEMBL340657 1 8.68
CHEMBL332577 1 6.89
CHEMBL341041 1 6.80
CHEMBL340580 1 6.58
CHEMBL125288 1 6.31
CHEMBL126061 1 -
CHEMBL331111 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122512 IC50 = 0.25 nM 9.60
CHEMBL123705 IC50 = 0.61 nM 9.21
CHEMBL340657 IC50 = 2.1 nM 8.68
CHEMBL332577 IC50 = 130.0 nM 6.89
CHEMBL341041 IC50 = 160.0 nM 6.80
CHEMBL340580 IC50 = 260.0 nM 6.58
CHEMBL125288 IC50 = 490.0 nM 6.31
CHEMBL126061 IC50 < 10.0 nM -
CHEMBL331111 IC50 < 0.1 nM -