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Assay Detail

CHEMBL648802

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Binding
Binding affinity against adenosine A2 receptor in rat brain using [3H]- CGS 21680 as radioligand
ChEMBL ↗
72
Total Activities
72
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Tissue Brain
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

Adenosine A2 receptor (CHEMBL2094117) ↗
Type PROTEIN FAMILY
Organism Rattus norvegicus

Publication

Structure-activity relationships of 8-styrylxanthines as A2-selective adenosine antagonists.
Jacobson KA, Gallo-Rodriguez C, Melman N, Fischer B, Maillard M, van Bergen A, van Galen PJ, Karton Y.
J Med Chem (1993) 36 : 1333 -1342
PubMed 8496902 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 72 6.61 7.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL283939 — — 1 7.85
CHEMBL25906 — — 1 7.72
CHEMBL27215 — — 1 7.62
CHEMBL27508 — — 1 7.51
CHEMBL28258 — — 1 7.48
CHEMBL25859 — — 1 7.41
CHEMBL283908 — — 1 7.36
CHEMBL27496 — — 1 7.31
CHEMBL27260 — — 1 7.28
CHEMBL26138 — — 1 7.27
CHEMBL26938 — — 1 7.25
CHEMBL26668 — — 1 7.24
CHEMBL25964 — — 1 7.21
CHEMBL27140 — — 1 7.19
CHEMBL281468 — — 1 7.19
CHEMBL283896 — — 1 7.17
CHEMBL283937 — — 1 7.16
CHEMBL27318 — — 1 7.12
CHEMBL422399 — — 1 7.09
CHEMBL283906 — — 1 7.08
CHEMBL281657 — — 1 7.07
CHEMBL26897 — — 1 7.03
CHEMBL25799 — — 1 6.92
CHEMBL27203 — — 1 6.88
CHEMBL27714 — — 1 6.88
CHEMBL28267 — — 1 6.87
CHEMBL28052 — — 1 6.86
CHEMBL25976 — — 1 6.84
CHEMBL284571 — — 1 6.82
CHEMBL28233 — — 1 6.76

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL283939 — Ki = 14.0 nM 7.85
CHEMBL25906 — Ki = 18.9 nM 7.72
CHEMBL27215 — Ki = 24.0 nM 7.62
CHEMBL27508 — Ki = 31.1 nM 7.51
CHEMBL28258 — Ki = 33.0 nM 7.48
CHEMBL25859 — Ki = 39.0 nM 7.41
CHEMBL283908 — Ki = 44.0 nM 7.36
CHEMBL27496 — Ki = 48.5 nM 7.31
CHEMBL27260 — Ki = 53.0 nM 7.28
CHEMBL26138 — Ki = 54.0 nM 7.27
CHEMBL26938 — Ki = 56.2 nM 7.25
CHEMBL26668 — Ki = 57.0 nM 7.24
CHEMBL25964 — Ki = 61.3 nM 7.21
CHEMBL281468 — Ki = 65.0 nM 7.19
CHEMBL27140 — Ki = 64.0 nM 7.19
CHEMBL283896 — Ki = 68.0 nM 7.17
CHEMBL283937 — Ki = 68.5 nM 7.16
CHEMBL27318 — Ki = 75.3 nM 7.12
CHEMBL422399 — Ki = 81.0 nM 7.09
CHEMBL283906 — Ki = 83.0 nM 7.08
CHEMBL281657 — Ki = 84.8 nM 7.07
CHEMBL26897 — Ki = 94.0 nM 7.03
CHEMBL25799 — Ki = 120.0 nM 6.92
CHEMBL27203 — Ki = 131.0 nM 6.88
CHEMBL27714 — Ki = 131.0 nM 6.88
CHEMBL28267 — Ki = 134.0 nM 6.87
CHEMBL28052 — Ki = 139.0 nM 6.86
CHEMBL25976 — Ki = 143.0 nM 6.84
CHEMBL284571 — Ki = 153.0 nM 6.82
CHEMBL28233 — Ki = 173.0 nM 6.76
CHEMBL26070 — Ki = 195.0 nM 6.71
CHEMBL280982 — Ki = 197.0 nM 6.71
CHEMBL26069 — Ki = 202.0 nM 6.70
CHEMBL26887 — Ki = 206.0 nM 6.69
CHEMBL447777 — Ki = 210.0 nM 6.68
CHEMBL280796 — Ki = 216.0 nM 6.67
CHEMBL28395 — Ki = 216.0 nM 6.67
CHEMBL283406 — Ki = 228.0 nM 6.64
CHEMBL286959 — Ki = 265.0 nM 6.58
CHEMBL282864 — Ki = 267.0 nM 6.57
CHEMBL280839 — Ki = 269.0 nM 6.57
CHEMBL282993 — Ki = 291.0 nM 6.54
CHEMBL283184 — Ki = 303.0 nM 6.52
CHEMBL26837 — Ki = 323.0 nM 6.49
CHEMBL26963 — Ki = 327.0 nM 6.49
CHEMBL283847 — Ki = 327.0 nM 6.49
CHEMBL283258 — Ki = 343.0 nM 6.46
CHEMBL27261 — Ki = 346.0 nM 6.46
CHEMBL282206 — Ki = 353.0 nM 6.45
CHEMBL26979 — Ki = 360.0 nM 6.44