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Assay Detail

CHEMBL4373381

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ADMET
Inhibition of human GST-tagged PDE3A (484 to end residues) using cAMP as substrate measured after 60 mins
14
Total Activities
14
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-inhibited 3',5'-cyclic phosphodiesterase 3A (CHEMBL241)
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 14 5.13 5.96

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4534373 1 5.96
CHEMBL4569753 1 5.31
CHEMBL4542237 1 5.15
CHEMBL4535938 1 5.13
CHEMBL4544877 1 5.11
CHEMBL4542820 1 5.11
CHEMBL4456157 1 5.07
CHEMBL1086110 1 5.07
CHEMBL4464637 1 4.78
CHEMBL4556703 1 4.63
CHEMBL4585428 1 -
CHEMBL4580449 1 -
CHEMBL4437406 1 -
CHEMBL4472846 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4534373 IC50 = 1110.0 nM 5.96
CHEMBL4569753 IC50 = 4940.0 nM 5.31
CHEMBL4542237 IC50 = 7070.0 nM 5.15
CHEMBL4535938 IC50 = 7470.0 nM 5.13
CHEMBL4544877 IC50 = 7850.0 nM 5.11
CHEMBL4542820 IC50 = 7840.0 nM 5.11
CHEMBL4456157 IC50 = 8520.0 nM 5.07
CHEMBL1086110 IC50 = 8500.0 nM 5.07
CHEMBL4464637 IC50 = 16500.0 nM 4.78
CHEMBL4556703 IC50 = 23600.0 nM 4.63
CHEMBL4585428 IC50 > 20000.0 nM -
CHEMBL4580449 IC50 > 20000.0 nM -
CHEMBL4437406 IC50 > 20000.0 nM -
CHEMBL4472846 IC50 = 111900.0 nM -