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Assay Detail

CHEMBL642892

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

Binding
GTP-induced shift at rat Adenosine A1 receptor (A1AR)
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 8.97 9.16

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL54334 1 9.16
CHEMBL296399 1 9.15
CHEMBL293371 1 9.15
CHEMBL52648 1 9.14
CHEMBL53795 1 9.14
CHEMBL299238 1 9.13
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 9.11
CHEMBL55195 1 9.08
CHEMBL48278 1 9.03
CHEMBL299504 1 8.37
CHEMBL54468 1 8.19

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL54334 Ki = 0.69 nM 9.16
CHEMBL296399 Ki = 0.7 nM 9.15
CHEMBL293371 Ki = 0.7 nM 9.15
CHEMBL52648 Ki = 0.73 nM 9.14
CHEMBL53795 Ki = 0.72 nM 9.14
CHEMBL299238 Ki = 0.74 nM 9.13
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 0.77 nM 9.11
CHEMBL55195 Ki = 0.84 nM 9.08
CHEMBL48278 Ki = 0.94 nM 9.03
CHEMBL299504 Ki = 4.3 nM 8.37
CHEMBL54468 Ki = 6.4 nM 8.19