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Assay Detail

CHEMBL646276

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

Binding
Affinity for adenosine A2a receptor was determined on rat striatal membrane using [3H]-CGS- 21680 as radioligand
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Striatum
Subcellular Membrane
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A2a (CHEMBL302)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

N6-cyclopentyl-3'-substituted-xylofuranosyladenosines: a new class of non-xanthine adenosine A1 receptor antagonists.
Van Calenbergh S, von Frijtag Drabbe Künzel JK, Blaton NM, Peeters OM, Rozenski J, Van Aerschot A, De Bruyn A, De Keukeleire D, IJzerman AP, Herdewijn P.
J Med Chem (1997) 40 : 3765 -3772
PubMed 9371242 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 16 5.56 6.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2112627 1 6.24
CHEMBL2112626 1 6.19
CHEMBL340299 1 6.11
CHEMBL122746 1 6.10
CHEMBL2112622 1 5.75
CHEMBL2112630 1 5.70
CHEMBL2112633 1 5.62
CHEMBL2112612 1 5.61
CHEMBL2112620 1 5.56
CHEMBL52648 1 5.43
CHEMBL2112632 1 5.37
CHEMBL122345 1 5.33
CHEMBL2112631 1 5.16
CHEMBL2112625 1 5.10
CHEMBL2112623 1 4.93
CHEMBL2112619 1 4.73

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2112627 Ki = 580.0 nM 6.24
CHEMBL2112626 Ki = 650.0 nM 6.19
CHEMBL340299 Ki = 770.0 nM 6.11
CHEMBL122746 Ki = 790.0 nM 6.10
CHEMBL2112622 Ki = 1770.0 nM 5.75
CHEMBL2112630 Ki = 2020.0 nM 5.70
CHEMBL2112633 Ki = 2410.0 nM 5.62
CHEMBL2112612 Ki = 2470.0 nM 5.61
CHEMBL2112620 Ki = 2760.0 nM 5.56
CHEMBL52648 Ki = 3680.0 nM 5.43
CHEMBL2112632 Ki = 4230.0 nM 5.37
CHEMBL122345 Ki = 4660.0 nM 5.33
CHEMBL2112631 Ki = 6850.0 nM 5.16
CHEMBL2112625 Ki = 7940.0 nM 5.10
CHEMBL2112623 Ki = 11800.0 nM 4.93
CHEMBL2112619 Ki = 18600.0 nM 4.73