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Assay Detail

CHEMBL821993

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

Binding
Inhibition of platelet cAMP phosphodiesterase
24
Total Activities
24
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 5 — Multiple protein complex / RNA
Curated By Autocuration

Target

Phosphodiesterase 3 (CHEMBL2094125)
Type PROTEIN FAMILY
Organism Homo sapiens

Publication

Inhibitors of cyclic AMP phosphodiesterase. 3. Synthesis and biological evaluation of pyrido and imidazolyl analogues of 1,2,3,5-tetrahydro-2-oxoimidazo[2,1-b]quinazoline.
Venuti MC, Stephenson RA, Alvarez R, Bruno JJ, Strosberg AM.
J Med Chem (1988) 31 : 2136 -2145
PubMed 2846839 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 24 6.01 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69139 LIXAZINONE 2.0 1 8.00
CHEMBL66522 1 7.16
CHEMBL760 ANAGRELIDE 4.0 1 7.10
CHEMBL440593 CI-930 1 6.82
CHEMBL31580 1 6.82
CHEMBL320341 QUAZINONE 2.0 1 6.62
CHEMBL67513 1 6.54
CHEMBL66978 1 6.28
CHEMBL66447 1 6.25
CHEMBL66153 1 6.22
CHEMBL66061 1 6.16
CHEMBL189 MILRINONE 4.0 1 6.07
CHEMBL65882 1 5.82
CHEMBL66212 1 5.82
CHEMBL70033 1 5.70
CHEMBL69286 1 5.48
CHEMBL65700 1 5.06
CHEMBL302575 1 4.75
CHEMBL66935 1 4.58
CHEMBL69940 1 4.52
CHEMBL428866 1 4.43
CHEMBL307996 1 -
CHEMBL58355 PIROXIMONE 2.0 1 -
CHEMBL68833 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69139 LIXAZINONE IC50 = 10.0 nM 8.00
CHEMBL66522 IC50 = 70.0 nM 7.16
CHEMBL760 ANAGRELIDE IC50 = 80.0 nM 7.10
CHEMBL440593 CI-930 IC50 = 150.0 nM 6.82
CHEMBL31580 IC50 = 150.0 nM 6.82
CHEMBL320341 QUAZINONE IC50 = 240.0 nM 6.62
CHEMBL67513 IC50 = 290.0 nM 6.54
CHEMBL66978 IC50 = 520.0 nM 6.28
CHEMBL66447 IC50 = 560.0 nM 6.25
CHEMBL66153 IC50 = 600.0 nM 6.22
CHEMBL66061 IC50 = 700.0 nM 6.16
CHEMBL189 MILRINONE IC50 = 860.0 nM 6.07
CHEMBL65882 IC50 = 1500.0 nM 5.82
CHEMBL66212 IC50 = 1500.0 nM 5.82
CHEMBL70033 IC50 = 2000.0 nM 5.70
CHEMBL69286 IC50 = 3300.0 nM 5.48
CHEMBL65700 IC50 = 8800.0 nM 5.06
CHEMBL302575 IC50 = 18000.0 nM 4.75
CHEMBL66935 IC50 = 26000.0 nM 4.58
CHEMBL69940 IC50 = 30000.0 nM 4.52
CHEMBL428866 IC50 = 37000.0 nM 4.43
CHEMBL307996 IC50 = 330000.0 nM -
CHEMBL58355 PIROXIMONE IC50 > 100000.0 nM -
CHEMBL68833 IC50 = 250000.0 nM -