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Assay Detail

CHEMBL768653

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

Binding
Inhibition of human platelet PDE by inhibiting cyclic Adenosine monophosphate (cAMP) hydrolysis
76
Total Activities
76
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

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

Target

Phosphodiesterase 3 (CHEMBL2094125)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Inhibitors of blood platelet cAMP phosphodiesterase. 2. Structure-activity relationships associated with 1,3-dihydro-2H-imidazo[4,5-b]quinolin-2-ones substituted with functionalized side chains.
Meanwell NA, Pearce BC, Roth HR, Smith EC, Wedding DL, Wright JJ, Buchanan JO, Baryla UM, Gamberdella M, Gillespie E.
J Med Chem (1992) 35 : 2672 -2687
PubMed 1321910 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 76 7.39 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL88108 1 9.52
CHEMBL431799 1 9.40
CHEMBL90804 1 9.30
CHEMBL92264 1 9.00
CHEMBL88245 1 9.00
CHEMBL90237 1 8.70
CHEMBL91368 1 8.70
CHEMBL90677 1 8.70
CHEMBL88444 1 8.70
CHEMBL88835 1 8.52
CHEMBL69139 LIXAZINONE 2.0 1 8.52
CHEMBL91527 1 8.52
CHEMBL89679 1 8.40
CHEMBL91295 1 8.40
CHEMBL91224 1 8.30
CHEMBL313463 1 8.30
CHEMBL328149 1 8.30
CHEMBL88799 1 8.22
CHEMBL91478 1 8.22
CHEMBL92269 1 8.22
CHEMBL90168 1 8.15
CHEMBL330280 1 8.10
CHEMBL330677 1 8.05
CHEMBL93688 1 8.00
CHEMBL88583 1 8.00
CHEMBL90120 1 8.00
CHEMBL314763 1 7.70
CHEMBL88265 1 7.70
CHEMBL90195 1 7.70
CHEMBL91570 1 7.70

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL88108 IC50 = 0.3 nM 9.52
CHEMBL431799 IC50 = 0.4 nM 9.40
CHEMBL90804 IC50 = 0.5 nM 9.30
CHEMBL92264 IC50 = 1.0 nM 9.00
CHEMBL88245 IC50 = 1.0 nM 9.00
CHEMBL90237 IC50 = 2.0 nM 8.70
CHEMBL91368 IC50 = 2.0 nM 8.70
CHEMBL90677 IC50 = 2.0 nM 8.70
CHEMBL88444 IC50 = 2.0 nM 8.70
CHEMBL88835 IC50 = 3.0 nM 8.52
CHEMBL69139 LIXAZINONE IC50 = 3.0 nM 8.52
CHEMBL91527 IC50 = 3.0 nM 8.52
CHEMBL91295 IC50 = 4.0 nM 8.40
CHEMBL89679 IC50 = 4.0 nM 8.40
CHEMBL328149 IC50 = 5.0 nM 8.30
CHEMBL91224 IC50 = 5.0 nM 8.30
CHEMBL313463 IC50 = 5.0 nM 8.30
CHEMBL88799 IC50 = 6.0 nM 8.22
CHEMBL91478 IC50 = 6.0 nM 8.22
CHEMBL92269 IC50 = 6.0 nM 8.22
CHEMBL90168 IC50 = 7.0 nM 8.15
CHEMBL330280 IC50 = 8.0 nM 8.10
CHEMBL330677 IC50 = 9.0 nM 8.05
CHEMBL90120 IC50 = 10.0 nM 8.00
CHEMBL93688 IC50 = 10.0 nM 8.00
CHEMBL88583 IC50 = 10.0 nM 8.00
CHEMBL314763 IC50 = 20.0 nM 7.70
CHEMBL88265 IC50 = 20.0 nM 7.70
CHEMBL90195 IC50 = 20.0 nM 7.70
CHEMBL91570 IC50 = 20.0 nM 7.70
CHEMBL90414 IC50 = 20.0 nM 7.70
CHEMBL91259 IC50 = 20.0 nM 7.70
CHEMBL423864 IC50 = 20.0 nM 7.70
CHEMBL91843 IC50 = 30.0 nM 7.52
CHEMBL88218 IC50 = 30.0 nM 7.52
CHEMBL88955 IC50 = 30.0 nM 7.52
CHEMBL89876 IC50 = 30.0 nM 7.52
CHEMBL313609 IC50 = 40.0 nM 7.40
CHEMBL88708 IC50 = 40.0 nM 7.40
CHEMBL90958 IC50 = 40.0 nM 7.40
CHEMBL89660 IC50 = 40.0 nM 7.40
CHEMBL92158 IC50 = 40.0 nM 7.40
CHEMBL91899 IC50 = 50.0 nM 7.30
CHEMBL760 ANAGRELIDE IC50 = 54.0 nM 7.27
CHEMBL88224 IC50 = 60.0 nM 7.22
CHEMBL91204 IC50 = 60.0 nM 7.22
CHEMBL91837 IC50 = 60.0 nM 7.22
CHEMBL88525 IC50 = 70.0 nM 7.16
CHEMBL90477 IC50 = 70.0 nM 7.16
CHEMBL314093 IC50 = 80.0 nM 7.10