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Assay Detail

CHEMBL646360

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Binding
Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via Adenosine A2 receptor in rat PC12 membranes
19
Total Activities
19
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type PC-12
Subcellular Membrane
Confidence 4 — Cell-line / Tissue
Curated By Autocuration

Target

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

Publication

Effects of 8-phenyl and 8-cycloalkyl substituents on the activity of mono-, di-, and trisubstituted alkylxanthines with substitution at the 1-, 3-, and 7-positions.
Shamim MT, Ukena D, Padgett WL, Daly JW.
J Med Chem (1989) 32 : 1231 -1237
PubMed 2724296 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 19 5.65 7.14

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL274855 1 7.14
CHEMBL160369 1 6.68
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.60
CHEMBL9069 1 6.60
CHEMBL321505 1 6.35
CHEMBL22042 1 6.00
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 5.80
CHEMBL158507 1 5.64
CHEMBL418375 1 5.42
CHEMBL281811 1 5.39
CHEMBL8488 1 5.30
CHEMBL278332 1 5.28
CHEMBL157655 1 5.27
CHEMBL20483 1 5.25
CHEMBL418333 1 4.96
CHEMBL281633 1 4.77
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.77
CHEMBL113 CAFFEINE 4.0 1 4.43
CHEMBL20993 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL274855 Ki = 73.0 nM 7.14
CHEMBL160369 Ki = 210.0 nM 6.68
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 250.0 nM 6.60
CHEMBL9069 Ki = 250.0 nM 6.60
CHEMBL321505 Ki = 450.0 nM 6.35
CHEMBL22042 Ki = 1000.0 nM 6.00
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 1600.0 nM 5.80
CHEMBL158507 Ki = 2300.0 nM 5.64
CHEMBL418375 Ki = 3800.0 nM 5.42
CHEMBL281811 Ki = 4100.0 nM 5.39
CHEMBL8488 Ki = 5000.0 nM 5.30
CHEMBL278332 Ki = 5300.0 nM 5.28
CHEMBL157655 Ki = 5400.0 nM 5.27
CHEMBL20483 Ki = 5600.0 nM 5.25
CHEMBL418333 Ki = 11000.0 nM 4.96
CHEMBL281633 Ki = 17000.0 nM 4.77
CHEMBL1355736 THEOPHYLLINE Ki = 17000.0 nM 4.77
CHEMBL113 CAFFEINE Ki = 37000.0 nM 4.43
CHEMBL20993 Ki = 150000.0 nM -