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Assay Detail

CHEMBL4373380

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

ADMET
Inhibition of human PDE2A using cAMP as substrate measured after 60 mins
11
Total Activities
11
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
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

Novel, potent, selective, and brain penetrant phosphodiesterase 10A inhibitors.
Geneste H, Drescher K, Jakob C, Laplanche L, Ochse M, Torrent M.
Bioorg Med Chem Lett (2019) 29 : 406 -412
PubMed 30587449 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 11 5.56 6.04

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4580449 1 6.04
CHEMBL4569753 1 5.88
CHEMBL4556703 1 5.88
CHEMBL4535938 1 5.73
CHEMBL1086110 1 5.67
CHEMBL4542237 1 5.52
CHEMBL4456157 1 5.45
CHEMBL4464637 1 5.31
CHEMBL4472846 1 5.27
CHEMBL4437406 1 4.89
CHEMBL4534373 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4580449 IC50 = 923.0 nM 6.04
CHEMBL4569753 IC50 = 1310.0 nM 5.88
CHEMBL4556703 IC50 = 1320.0 nM 5.88
CHEMBL4535938 IC50 = 1860.0 nM 5.73
CHEMBL1086110 IC50 = 2160.0 nM 5.67
CHEMBL4542237 IC50 = 3010.0 nM 5.52
CHEMBL4456157 IC50 = 3520.0 nM 5.45
CHEMBL4464637 IC50 = 4890.0 nM 5.31
CHEMBL4472846 IC50 = 5390.0 nM 5.27
CHEMBL4437406 IC50 = 12900.0 nM 4.89
CHEMBL4534373 IC50 > 100000.0 nM -