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Assay Detail

CHEMBL5256543

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

Binding
Inhibition of human recombinant PDE3 expressed in Escherichia coli
16
Total Activities
16
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

Anagrelide: A Clinically Effective cAMP Phosphodiesterase 3A Inhibitor with Molecular Glue Properties.
Meanwell NA.
ACS Med Chem Lett (2023) 14 : 350 -361
PubMed 37077378 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 16 6.51 8.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL69139 LIXAZINONE 2.0 1 8.00
CHEMBL34431 CILOSTAMIDE 2.0 1 7.57
CHEMBL760 ANAGRELIDE 4.0 1 7.52
CHEMBL5283704 1 7.50
CHEMBL66522 1 7.16
CHEMBL38224 INDOLIDAN 2.0 1 7.10
CHEMBL299631 1 7.05
CHEMBL799 CILOSTAZOL 4.0 1 6.70
CHEMBL189 MILRINONE 4.0 1 6.35
CHEMBL313842 ZARDAVERINE 2.0 1 6.24
CHEMBL320341 QUAZINONE 2.0 1 6.24
CHEMBL5278813 1 6.22
CHEMBL249856 ENOXIMONE 3.0 1 5.23
CHEMBL12831 IMAZODAN 2.0 1 5.21
CHEMBL17423 VESNARINONE 2.0 1 5.21
CHEMBL12856 INAMRINONE 4.0 1 4.78

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL69139 LIXAZINONE IC50 = 10.0 nM 8.00
CHEMBL34431 CILOSTAMIDE IC50 = 27.0 nM 7.57
CHEMBL760 ANAGRELIDE IC50 = 30.0 nM 7.52
CHEMBL5283704 IC50 = 32.0 nM 7.50
CHEMBL66522 IC50 = 70.0 nM 7.16
CHEMBL38224 INDOLIDAN IC50 = 80.0 nM 7.10
CHEMBL299631 IC50 = 90.0 nM 7.05
CHEMBL799 CILOSTAZOL IC50 = 200.0 nM 6.70
CHEMBL189 MILRINONE IC50 = 450.0 nM 6.35
CHEMBL313842 ZARDAVERINE IC50 = 580.0 nM 6.24
CHEMBL320341 QUAZINONE IC50 = 580.0 nM 6.24
CHEMBL5278813 IC50 = 600.0 nM 6.22
CHEMBL249856 ENOXIMONE IC50 = 5900.0 nM 5.23
CHEMBL12831 IMAZODAN IC50 = 6100.0 nM 5.21
CHEMBL17423 VESNARINONE IC50 = 6200.0 nM 5.21
CHEMBL12856 INAMRINONE IC50 = 16700.0 nM 4.78