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Assay Detail

CHEMBL3419487

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

Functional
Agonist activity at human adenosine A2B receptor expressed in CHO cells assessed as stimulation of [3H]cAMP levels by scintillation counting method
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type CHO
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Adenosine receptor A2b (CHEMBL255)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis, and biological evaluation of novel 2-((2-(4-(substituted)phenylpiperazin-1-yl)ethyl)amino)-5'-N-ethylcarboxamidoadenosines as potent and selective agonists of the A2A adenosine receptor.
Preti D, Baraldi PG, Saponaro G, Romagnoli R, Aghazadeh Tabrizi M, Baraldi S, Cosconati S, Bruno A, Novellino E, Vincenzi F, Ravani A, Borea PA, Varani K.
J Med Chem (2015) 58 : 3253 -3267
PubMed 25780876 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
EC50 40 5.62 6.41

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3416810 1 6.41
CHEMBL3416808 1 6.06
CHEMBL3416806 1 6.03
CHEMBL3416782 1 5.15
CHEMBL3416780 1 5.03
CHEMBL3416781 1 5.03
CHEMBL3416805 1 -
CHEMBL3416783 1 -
CHEMBL3416807 1 -
CHEMBL3416809 1 -
CHEMBL3416811 1 -
CHEMBL3416785 1 -
CHEMBL3416777 1 -
CHEMBL3416776 1 -
CHEMBL3416775 1 -
CHEMBL464859 NECA 1 -
CHEMBL331372 CGS-21680 1 -
CHEMBL3416779 1 -
CHEMBL3416793 1 -
CHEMBL3416803 1 -
CHEMBL3416802 1 -
CHEMBL3416801 1 -
CHEMBL3416800 1 -
CHEMBL3416799 1 -
CHEMBL3416798 1 -
CHEMBL3416797 1 -
CHEMBL3414573 1 -
CHEMBL3416796 1 -
CHEMBL3416795 1 -
CHEMBL3416804 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3416810 EC50 = 389.0 nM 6.41
CHEMBL3416808 EC50 = 866.0 nM 6.06
CHEMBL3416806 EC50 = 927.0 nM 6.03
CHEMBL3416782 EC50 = 7130.0 nM 5.15
CHEMBL3416780 EC50 = 9287.0 nM 5.03
CHEMBL3416781 EC50 = 9352.0 nM 5.03
CHEMBL3416777 EC50 > 10000.0 nM -
CHEMBL3416778 EC50 > 10000.0 nM -
CHEMBL3416776 EC50 > 10000.0 nM -
CHEMBL3416775 EC50 > 10000.0 nM -
CHEMBL464859 NECA EC50 > 10000.0 nM -
CHEMBL331372 CGS-21680 EC50 > 10000.0 nM -
CHEMBL3416779 EC50 > 10000.0 nM -
CHEMBL3416783 EC50 > 10000.0 nM -
CHEMBL3416784 EC50 > 10000.0 nM -
CHEMBL3416794 EC50 > 10000.0 nM -
CHEMBL3416786 EC50 > 10000.0 nM -
CHEMBL3416787 EC50 > 10000.0 nM -
CHEMBL3416788 EC50 > 10000.0 nM -
CHEMBL3416789 EC50 > 10000.0 nM -
CHEMBL3416790 EC50 > 10000.0 nM -
CHEMBL3416791 EC50 > 10000.0 nM -
CHEMBL3416792 EC50 > 10000.0 nM -
CHEMBL3416801 EC50 > 10000.0 nM -
CHEMBL3416804 EC50 > 10000.0 nM -
CHEMBL3416795 EC50 > 10000.0 nM -
CHEMBL3416796 EC50 > 10000.0 nM -
CHEMBL3414573 EC50 > 10000.0 nM -
CHEMBL3416797 EC50 > 10000.0 nM -
CHEMBL3416798 EC50 > 10000.0 nM -
CHEMBL3416799 EC50 > 10000.0 nM -
CHEMBL3416800 EC50 > 10000.0 nM -
CHEMBL3416785 EC50 > 10000.0 nM -
CHEMBL3416802 EC50 > 10000.0 nM -
CHEMBL3416803 EC50 > 10000.0 nM -
CHEMBL3416793 EC50 > 10000.0 nM -
CHEMBL3416805 EC50 > 10000.0 nM -
CHEMBL3416807 EC50 > 10000.0 nM -
CHEMBL3416809 EC50 > 10000.0 nM -
CHEMBL3416811 EC50 > 10000.0 nM -