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Assay Detail

CHEMBL4373082

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

Binding
Inhibition of PDE2 (unknown origin) using [3H]cAMP or [3H]cGMP as substrate measured after 30 mins by liquid scintillation counting method
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

cGMP-dependent 3',5'-cyclic phosphodiesterase (CHEMBL2652)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Design, synthesis of novel purin-6-one derivatives as phosphodiesterase 2 (PDE2) inhibitors: The neuroprotective and anxiolytic-like effects.
Huang XF, Cao YJ, Zhen J, Zhang DW, Kong R, Jiang WT, Xu Y, Song GQ, Ke HM, Liu L.
Bioorg Med Chem Lett (2019) 29 : 481 -486
PubMed 30554955 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 5.72 8.32

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370962 1 8.32
CHEMBL4580973 1 7.14
CHEMBL4591047 1 7.09
CHEMBL4453746 1 6.51
CHEMBL4458207 1 6.24
CHEMBL4437158 1 5.91
CHEMBL4448676 1 5.71
CHEMBL4458316 1 5.58
CHEMBL4578464 1 5.42
CHEMBL4518682 1 5.41
CHEMBL4443594 1 5.40
CHEMBL4516467 1 5.37
CHEMBL4533780 1 5.37
CHEMBL4453022 1 5.26
CHEMBL4539824 1 5.24
CHEMBL4473227 1 5.23
CHEMBL4467295 1 5.14
CHEMBL4446592 1 4.96
CHEMBL4562875 1 4.77
CHEMBL4463360 1 4.39
CHEMBL4569293 1 -
CHEMBL4475675 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370962 IC50 = 4.8 nM 8.32
CHEMBL4580973 IC50 = 72.0 nM 7.14
CHEMBL4591047 IC50 = 81.0 nM 7.09
CHEMBL4453746 IC50 = 310.0 nM 6.51
CHEMBL4458207 IC50 = 570.0 nM 6.24
CHEMBL4437158 IC50 = 1240.0 nM 5.91
CHEMBL4448676 IC50 = 1940.0 nM 5.71
CHEMBL4458316 IC50 = 2630.0 nM 5.58
CHEMBL4578464 IC50 = 3790.0 nM 5.42
CHEMBL4518682 IC50 = 3910.0 nM 5.41
CHEMBL4443594 IC50 = 3990.0 nM 5.40
CHEMBL4516467 IC50 = 4280.0 nM 5.37
CHEMBL4533780 IC50 = 4320.0 nM 5.37
CHEMBL4453022 IC50 = 5460.0 nM 5.26
CHEMBL4539824 IC50 = 5800.0 nM 5.24
CHEMBL4473227 IC50 = 5940.0 nM 5.23
CHEMBL4467295 IC50 = 7270.0 nM 5.14
CHEMBL4446592 IC50 = 11020.0 nM 4.96
CHEMBL4562875 IC50 = 16980.0 nM 4.77
CHEMBL4463360 IC50 = 40350.0 nM 4.39
CHEMBL4569293 IC50 > 50000.0 nM -
CHEMBL4475675 IC50 > 50000.0 nM -