Skip to main content
Free research Free research Free assay review with research home and workspace preview
Quick search ChEMBL 36
Assay Detail

CHEMBL642334

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

Binding
Inhibition of the stimulation by 5'-(N-ethylcarbamoyl) adenosine of adenyl cyclase via adenosine A2 receptor in human platelet membranes.
38
Total Activities
38
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Adenosine A2 receptor (CHEMBL2094257)
Type PROTEIN FAMILY
Organism Homo sapiens

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 38 5.79 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL158507 1 8.00
CHEMBL274855 1 7.70
CHEMBL22042 1 7.07
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] 1 6.85
CHEMBL106265 8-CYCLOPENTYLTHEOPHYLLINE 1 6.85
CHEMBL321505 1 6.82
CHEMBL160369 1 6.72
CHEMBL281811 1 6.72
CHEMBL22099 1 6.66
CHEMBL423239 1 6.50
CHEMBL279688 1 6.28
CHEMBL9069 1 6.07
CHEMBL21449 1 5.96
CHEMBL11048 1 5.82
CHEMBL1250 1-METHYLXANTHINE 1 5.72
CHEMBL418333 1 5.72
CHEMBL62350 8-PHENYL THEOPHYLLINE 1 5.72
CHEMBL20483 1 5.68
CHEMBL20402 1 5.64
CHEMBL418375 1 5.62
CHEMBL22178 1 5.62
CHEMBL281633 1 5.57
CHEMBL278332 1 5.55
CHEMBL8488 1 5.26
CHEMBL20613 1 5.19
CHEMBL157655 1 5.13
CHEMBL20806 1 4.96
CHEMBL278104 1 4.89
CHEMBL280367 1 4.85
CHEMBL1355736 THEOPHYLLINE 4.0 1 4.85

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL158507 Ki = 10.0 nM 8.00
CHEMBL274855 Ki = 20.0 nM 7.70
CHEMBL22042 Ki = 85.0 nM 7.07
CHEMBL183 1,3-DIPROPYL-8-CYCLOPENTYLXANTHINE [DPCPX] Ki = 140.0 nM 6.85
CHEMBL106265 8-CYCLOPENTYLTHEOPHYLLINE Ki = 140.0 nM 6.85
CHEMBL321505 Ki = 150.0 nM 6.82
CHEMBL160369 Ki = 190.0 nM 6.72
CHEMBL281811 Ki = 190.0 nM 6.72
CHEMBL22099 Ki = 220.0 nM 6.66
CHEMBL423239 Ki = 320.0 nM 6.50
CHEMBL279688 Ki = 520.0 nM 6.28
CHEMBL9069 Ki = 860.0 nM 6.07
CHEMBL21449 Ki = 1100.0 nM 5.96
CHEMBL11048 Ki = 1500.0 nM 5.82
CHEMBL62350 8-PHENYL THEOPHYLLINE Ki = 1900.0 nM 5.72
CHEMBL1250 1-METHYLXANTHINE Ki = 1900.0 nM 5.72
CHEMBL418333 Ki = 1900.0 nM 5.72
CHEMBL20483 Ki = 2100.0 nM 5.68
CHEMBL20402 Ki = 2300.0 nM 5.64
CHEMBL418375 Ki = 2400.0 nM 5.62
CHEMBL22178 Ki = 2400.0 nM 5.62
CHEMBL281633 Ki = 2700.0 nM 5.57
CHEMBL278332 Ki = 2800.0 nM 5.55
CHEMBL8488 Ki = 5500.0 nM 5.26
CHEMBL20613 Ki = 6500.0 nM 5.19
CHEMBL157655 Ki = 7400.0 nM 5.13
CHEMBL20806 Ki = 11000.0 nM 4.96
CHEMBL278104 Ki = 13000.0 nM 4.89
CHEMBL1355736 THEOPHYLLINE Ki = 14000.0 nM 4.85
CHEMBL21053 Ki = 14000.0 nM 4.85
CHEMBL280367 Ki = 14000.0 nM 4.85
CHEMBL21172 Ki = 25000.0 nM 4.60
CHEMBL21554 Ki = 26000.0 nM 4.58
CHEMBL113 CAFFEINE Ki = 30000.0 nM 4.52
CHEMBL20993 Ki = 57000.0 nM 4.24
CHEMBL279898 ENPROFYLLINE Ki = 130000.0 nM -
CHEMBL20844 Ki = 150000.0 nM -
CHEMBL619 3-METHYLXANTHINE Ki = 240000.0 nM -