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Assay Detail

CHEMBL646709

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

Binding
Affinity for adenosine A1 receptor was determined, in the absence of GTP in rat cortical membrane.
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Confidence 8 — Homologous single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL318)
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 19 6.24 7.63

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL52648 1 7.63
CHEMBL2112630 1 7.49
CHEMBL122746 1 7.08
CHEMBL2112627 1 6.96
CHEMBL2112619 1 6.96
CHEMBL2112626 1 6.89
CHEMBL338399 1 6.72
CHEMBL340299 1 6.70
CHEMBL2112632 1 6.62
CHEMBL2112625 1 6.43
CHEMBL2112620 1 6.40
CHEMBL2112631 1 6.09
CHEMBL121997 1 6.07
CHEMBL2112622 1 5.45
CHEMBL305686 CORDYCEPIN 1.0 1 5.15
CHEMBL122345 1 5.11
CHEMBL2112633 1 5.07
CHEMBL2112612 1 4.96
CHEMBL2112623 1 4.77

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL52648 Ki = 23.6 nM 7.63
CHEMBL2112630 Ki = 32.5 nM 7.49
CHEMBL122746 Ki = 83.0 nM 7.08
CHEMBL2112627 Ki = 110.0 nM 6.96
CHEMBL2112619 Ki = 110.0 nM 6.96
CHEMBL2112626 Ki = 130.0 nM 6.89
CHEMBL338399 Ki = 190.0 nM 6.72
CHEMBL340299 Ki = 200.0 nM 6.70
CHEMBL2112632 Ki = 240.0 nM 6.62
CHEMBL2112625 Ki = 370.0 nM 6.43
CHEMBL2112620 Ki = 400.0 nM 6.40
CHEMBL2112631 Ki = 820.0 nM 6.09
CHEMBL121997 Ki = 850.0 nM 6.07
CHEMBL2112622 Ki = 3590.0 nM 5.45
CHEMBL305686 CORDYCEPIN Ki = 7120.0 nM 5.15
CHEMBL122345 Ki = 7840.0 nM 5.11
CHEMBL2112633 Ki = 8470.0 nM 5.07
CHEMBL2112612 Ki = 10900.0 nM 4.96
CHEMBL2112623 Ki = 16900.0 nM 4.77