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Assay Detail

CHEMBL875247

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

Binding
Displacement of specific [3H]-CGS- 21680 binding at human adenosine A2A receptor expressed in HEK293 cells
45
Total Activities
45
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type HEK293
Confidence 8 — Homologous single protein target
Curated By Intermediate

Target

Adenosine receptor A2a (CHEMBL251)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-activity relationships of adenosine A3 receptor ligands: new potential therapy for the treatment of glaucoma.
Okamura T, Kurogi Y, Hashimoto K, Sato S, Nishikawa H, Kiryu K, Nagao Y.
Bioorg Med Chem Lett (2004) 14 : 3775 -3779
PubMed 15203160 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 45 6.16 7.15

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL122512 1 7.15
CHEMBL421611 1 6.89
CHEMBL340221 1 6.51
CHEMBL124900 1 6.12
CHEMBL126061 1 5.58
CHEMBL340262 1 5.57
CHEMBL338057 1 5.28
CHEMBL125147 1 -
CHEMBL122230 1 -
CHEMBL339066 1 -
CHEMBL123705 1 -
CHEMBL125340 1 -
CHEMBL123346 1 -
CHEMBL122163 1 -
CHEMBL124138 1 -
CHEMBL340182 1 -
CHEMBL125288 1 -
CHEMBL121339 1 -
CHEMBL434639 1 -
CHEMBL339529 1 -
CHEMBL124724 1 -
CHEMBL331837 1 -
CHEMBL124659 1 -
CHEMBL340657 1 -
CHEMBL125062 1 -
CHEMBL124725 1 -
CHEMBL123669 1 -
CHEMBL332800 1 -
CHEMBL124897 1 -
CHEMBL341259 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL122512 IC50 = 71.0 nM 7.15
CHEMBL421611 IC50 = 130.0 nM 6.89
CHEMBL340221 IC50 = 310.0 nM 6.51
CHEMBL124900 IC50 = 760.0 nM 6.12
CHEMBL126061 IC50 = 2600.0 nM 5.58
CHEMBL340262 IC50 = 2700.0 nM 5.57
CHEMBL338057 IC50 = 5300.0 nM 5.28
CHEMBL341041 IC50 > 10000.0 nM -
CHEMBL340182 IC50 > 10000.0 nM -
CHEMBL340580 IC50 > 10000.0 nM -
CHEMBL339218 IC50 > 10000.0 nM -
CHEMBL332577 IC50 > 10000.0 nM -
CHEMBL126150 IC50 > 10000.0 nM -
CHEMBL122230 IC50 > 650.0 nM -
CHEMBL121339 IC50 > 2600.0 nM -
CHEMBL125288 IC50 > 10000.0 nM -
CHEMBL124137 IC50 > 120.0 nM -
CHEMBL122037 IC50 > 10000.0 nM -
CHEMBL339556 IC50 > 10000.0 nM -
CHEMBL124887 IC50 > 10000.0 nM -
CHEMBL338837 IC50 > 10000.0 nM -
CHEMBL125339 IC50 > 10000.0 nM -
CHEMBL340093 IC50 > 10000.0 nM -
CHEMBL121890 IC50 > 10000.0 nM -
CHEMBL339019 IC50 > 10000.0 nM -
CHEMBL123694 IC50 > 10000.0 nM -
CHEMBL124724 IC50 > 10000.0 nM -
CHEMBL341259 IC50 > 10000.0 nM -
CHEMBL124897 IC50 > 10000.0 nM -
CHEMBL332800 IC50 > 10000.0 nM -
CHEMBL123669 IC50 > 10000.0 nM -
CHEMBL124725 IC50 > 10000.0 nM -
CHEMBL125062 IC50 > 10000.0 nM -
CHEMBL340657 IC50 > 190.0 nM -
CHEMBL124659 IC50 > 10000.0 nM -
CHEMBL331837 IC50 > 10000.0 nM -
CHEMBL124138 IC50 > 10000.0 nM -
CHEMBL339529 IC50 > 10000.0 nM -
CHEMBL434639 IC50 > 10000.0 nM -
CHEMBL125147 IC50 > 10000.0 nM -
CHEMBL339066 IC50 > 10000.0 nM -
CHEMBL123705 IC50 > 10000.0 nM -
CHEMBL125340 IC50 > 10000.0 nM -
CHEMBL123346 IC50 > 10000.0 nM -
CHEMBL122163 IC50 > 10000.0 nM -