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Assay Detail

CHEMBL643486

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Binding
Binding affinity at rat Adenosine A1 receptor in the presence of GTP
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Expert

Target

Adenosine receptor A1 (CHEMBL318)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

5'-Deoxy congeners of 9-(3-amido-3-deoxy-beta-D-xylofuranosyl)-N(6)-cyclopentyladenine: new adenosine A(1) receptor antagonists and inverse agonists.
Van Calenbergh S, Link A, Fujikawa S, de Ligt RA, Vanheusden V, Golisade A, Blaton NM, Rozenski J, IJzerman AP, Herdewijn P.
J Med Chem (2002) 45 : 1845 -1852
PubMed 11960496 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 11 7.16 8.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 8.92
CHEMBL52648 1 7.77
CHEMBL296399 1 7.42
CHEMBL54334 1 7.34
CHEMBL293371 1 7.27
CHEMBL53795 1 7.16
CHEMBL55195 1 6.94
CHEMBL299238 1 6.68
CHEMBL48278 1 6.59
CHEMBL54468 1 6.35
CHEMBL299504 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 1.2 nM 8.92
CHEMBL52648 Ki = 17.0 nM 7.77
CHEMBL296399 Ki = 38.0 nM 7.42
CHEMBL54334 Ki = 46.0 nM 7.34
CHEMBL293371 Ki = 54.0 nM 7.27
CHEMBL53795 Ki = 70.0 nM 7.16
CHEMBL55195 Ki = 114.0 nM 6.94
CHEMBL299238 Ki = 210.0 nM 6.68
CHEMBL48278 Ki = 259.0 nM 6.59
CHEMBL54468 Ki = 450.0 nM 6.35
CHEMBL299504 Ki = 470.0 nM 6.33