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Assay Detail

CHEMBL3419482

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

Binding
Displacement of [3H]CCPA from human adenosine A1 receptor expressed in CHO cell membranes incubated for 120 mins by scintillation counting method
40
Total Activities
40
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL226)
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
Ki 40 7.61 8.44

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3416810 1 8.44
CHEMBL3416808 1 8.35
CHEMBL3416806 1 8.09
CHEMBL464859 NECA 1 8.06
CHEMBL3416807 1 7.35
CHEMBL3416811 1 7.12
CHEMBL3416804 1 6.83
CHEMBL3416805 1 6.61
CHEMBL3416809 1 -
CHEMBL3416792 1 -
CHEMBL3416791 1 -
CHEMBL3416799 1 -
CHEMBL3416798 1 -
CHEMBL3416797 1 -
CHEMBL3414573 1 -
CHEMBL3416796 1 -
CHEMBL3416795 1 -
CHEMBL3416794 1 -
CHEMBL3416793 1 -
CHEMBL3416803 1 -
CHEMBL3416802 1 -
CHEMBL3416801 1 -
CHEMBL3416775 1 -
CHEMBL3416776 1 -
CHEMBL3416777 1 -
CHEMBL3416778 1 -
CHEMBL331372 CGS-21680 1 -
CHEMBL3416779 1 -
CHEMBL3416781 1 -
CHEMBL3416780 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3416810 Ki = 3.63 nM 8.44
CHEMBL3416808 Ki = 4.52 nM 8.35
CHEMBL3416806 Ki = 8.12 nM 8.09
CHEMBL464859 NECA Ki = 8.62 nM 8.06
CHEMBL3416807 Ki = 45.0 nM 7.35
CHEMBL3416811 Ki = 75.0 nM 7.12
CHEMBL3416804 Ki = 147.0 nM 6.83
CHEMBL3416805 Ki = 243.0 nM 6.61
CHEMBL3414573 Ki > 10000.0 nM -
CHEMBL3416782 Ki > 10000.0 nM -
CHEMBL3416796 Ki > 10000.0 nM -
CHEMBL3416795 Ki > 10000.0 nM -
CHEMBL3416794 Ki > 10000.0 nM -
CHEMBL3416793 Ki > 10000.0 nM -
CHEMBL3416792 Ki > 10000.0 nM -
CHEMBL3416800 Ki > 10000.0 nM -
CHEMBL3416790 Ki > 10000.0 nM -
CHEMBL3416789 Ki > 10000.0 nM -
CHEMBL3416788 Ki > 10000.0 nM -
CHEMBL3416787 Ki > 10000.0 nM -
CHEMBL3416786 Ki > 10000.0 nM -
CHEMBL3416785 Ki > 10000.0 nM -
CHEMBL3416784 Ki > 10000.0 nM -
CHEMBL3416783 Ki > 10000.0 nM -
CHEMBL3416797 Ki > 10000.0 nM -
CHEMBL3416798 Ki > 10000.0 nM -
CHEMBL3416799 Ki > 10000.0 nM -
CHEMBL3416791 Ki > 10000.0 nM -
CHEMBL3416809 Ki > 10000.0 nM -
CHEMBL3416803 Ki > 10000.0 nM -
CHEMBL3416802 Ki > 10000.0 nM -
CHEMBL3416801 Ki > 10000.0 nM -
CHEMBL3416775 Ki > 10000.0 nM -
CHEMBL3416776 Ki > 10000.0 nM -
CHEMBL3416777 Ki > 10000.0 nM -
CHEMBL3416778 Ki > 10000.0 nM -
CHEMBL331372 CGS-21680 Ki > 10000.0 nM -
CHEMBL3416779 Ki > 10000.0 nM -
CHEMBL3416781 Ki > 10000.0 nM -
CHEMBL3416780 Ki > 10000.0 nM -