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Assay Detail

CHEMBL641041

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Binding
Affinity against Adenosine A1 receptor in rat brain using [3H]- PIA as radioligand
ChEMBL ↗
65
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine receptor A1 (CHEMBL318) ↗
Type SINGLE PROTEIN
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 65 5.76 7.50

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL283939 — — 1 7.50
CHEMBL283908 — — 1 7.26
CHEMBL27496 — — 1 7.15
CHEMBL284571 — — 1 7.11
CHEMBL27140 — — 1 7.01
CHEMBL25906 — — 1 6.95
CHEMBL26837 — — 1 6.84
CHEMBL27261 — — 1 6.84
CHEMBL28395 — — 1 6.78
CHEMBL26938 — — 1 6.57
CHEMBL26069 — — 1 6.54
CHEMBL28258 — — 1 6.52
CHEMBL27260 — — 1 6.42
CHEMBL283937 — — 1 6.42
CHEMBL27508 — — 1 6.24
CHEMBL447777 — — 1 6.20
CHEMBL282993 — — 1 6.18
CHEMBL283847 — — 1 6.16
CHEMBL283184 — — 1 6.15
CHEMBL280839 — — 1 6.07
CHEMBL281958 — — 1 6.07
CHEMBL25964 — — 1 6.06
CHEMBL283258 — — 1 6.05
CHEMBL285339 — — 1 5.97
CHEMBL281305 — — 1 5.80
CHEMBL26668 — — 1 5.77
CHEMBL28046 — — 1 5.76
CHEMBL28346 — — 1 5.75
CHEMBL27032 — — 1 5.74
CHEMBL26070 — — 1 5.67

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL283939 — Ki = 32.0 nM 7.50
CHEMBL283908 — Ki = 55.0 nM 7.26
CHEMBL27496 — Ki = 71.0 nM 7.15
CHEMBL284571 — Ki = 78.0 nM 7.11
CHEMBL27140 — Ki = 97.0 nM 7.01
CHEMBL25906 — Ki = 113.0 nM 6.95
CHEMBL26837 — Ki = 143.0 nM 6.84
CHEMBL27261 — Ki = 146.0 nM 6.84
CHEMBL28395 — Ki = 167.0 nM 6.78
CHEMBL26938 — Ki = 272.0 nM 6.57
CHEMBL26069 — Ki = 288.0 nM 6.54
CHEMBL28258 — Ki = 301.0 nM 6.52
CHEMBL27260 — Ki = 382.0 nM 6.42
CHEMBL283937 — Ki = 379.0 nM 6.42
CHEMBL27508 — Ki = 577.0 nM 6.24
CHEMBL447777 — Ki = 632.0 nM 6.20
CHEMBL282993 — Ki = 654.0 nM 6.18
CHEMBL283847 — Ki = 689.0 nM 6.16
CHEMBL283184 — Ki = 702.0 nM 6.15
CHEMBL280839 — Ki = 852.0 nM 6.07
CHEMBL281958 — Ki = 858.0 nM 6.07
CHEMBL25964 — Ki = 874.0 nM 6.06
CHEMBL283258 — Ki = 881.0 nM 6.05
CHEMBL285339 — Ki = 1060.0 nM 5.97
CHEMBL281305 — Ki = 1600.0 nM 5.80
CHEMBL26668 — Ki = 1690.0 nM 5.77
CHEMBL28046 — Ki = 1730.0 nM 5.76
CHEMBL28346 — Ki = 1770.0 nM 5.75
CHEMBL27032 — Ki = 1830.0 nM 5.74
CHEMBL26070 — Ki = 2140.0 nM 5.67
CHEMBL282599 — Ki = 2190.0 nM 5.66
CHEMBL26698 — Ki = 2330.0 nM 5.63
CHEMBL27215 — Ki = 2630.0 nM 5.58
CHEMBL281885 — Ki = 2720.0 nM 5.57
CHEMBL422399 — Ki = 2790.0 nM 5.55
CHEMBL26899 — Ki = 3030.0 nM 5.52
CHEMBL25799 — Ki = 3044.0 nM 5.52
CHEMBL28267 — Ki = 3330.0 nM 5.48
CHEMBL26897 — Ki = 3890.0 nM 5.41
CHEMBL26792 — Ki = 4040.0 nM 5.39
CHEMBL28052 — Ki = 4120.0 nM 5.38
CHEMBL282864 — Ki = 4760.0 nM 5.32
CHEMBL286285 — Ki = 5390.0 nM 5.27
CHEMBL285589 — Ki = 5340.0 nM 5.27
CHEMBL281657 — Ki = 5430.0 nM 5.26
CHEMBL28233 — Ki = 6170.0 nM 5.21
CHEMBL25914 — Ki = 6290.0 nM 5.20
CHEMBL283406 — Ki = 6280.0 nM 5.20
CHEMBL283896 — Ki = 6330.0 nM 5.20
CHEMBL26887 — Ki = 6920.0 nM 5.16