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Assay Detail

CHEMBL643485

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Binding
Binding affinity at rat Adenosine A1 receptor in the absence of GTP
18
Total Activities
18
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

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 18 7.00 8.84

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 8.84
CHEMBL52648 1 7.62
CHEMBL296399 1 7.26
CHEMBL54334 1 7.17
CHEMBL54468 1 7.16
CHEMBL293371 1 7.11
CHEMBL53795 1 7.01
CHEMBL294675 1 6.99
CHEMBL299504 1 6.96
CHEMBL55099 1 6.95
CHEMBL55195 1 6.86
CHEMBL443741 1 6.77
CHEMBL54505 1 6.63
CHEMBL53387 1 6.62
CHEMBL416117 1 6.57
CHEMBL48278 1 6.55
CHEMBL299238 1 6.54
CHEMBL301116 1 6.33

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 1.46 nM 8.84
CHEMBL52648 Ki = 24.0 nM 7.62
CHEMBL296399 Ki = 55.0 nM 7.26
CHEMBL54334 Ki = 67.0 nM 7.17
CHEMBL54468 Ki = 70.0 nM 7.16
CHEMBL293371 Ki = 78.0 nM 7.11
CHEMBL53795 Ki = 98.0 nM 7.01
CHEMBL294675 Ki = 102.0 nM 6.99
CHEMBL299504 Ki = 110.0 nM 6.96
CHEMBL55099 Ki = 112.0 nM 6.95
CHEMBL55195 Ki = 138.0 nM 6.86
CHEMBL443741 Ki = 171.0 nM 6.77
CHEMBL54505 Ki = 236.0 nM 6.63
CHEMBL53387 Ki = 240.0 nM 6.62
CHEMBL416117 Ki = 270.0 nM 6.57
CHEMBL48278 Ki = 279.0 nM 6.55
CHEMBL299238 Ki = 286.0 nM 6.54
CHEMBL301116 Ki = 473.0 nM 6.33