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Assay Detail

CHEMBL2187828

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

Binding
Inhibition of recombinant PDE2A expressed in baculovirus infected SF21 cells using [3H]cAMP as substrate after 30 mins by liquid scintillation counting
9
Total Activities
9
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Cell Type Sf21
Confidence 8 — Homologous single protein target
Curated By Autocuration

Target

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

Publication

Current landscape of phosphodiesterase 10A (PDE10A) inhibition.
Chappie TA, Helal CJ, Hou X.
J Med Chem (2012) 55 : 7299 -7331
PubMed 22834877 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 7.31 8.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2180771 1 8.48
CHEMBL2180772 1 8.28
CHEMBL2180773 1 8.03
CHEMBL2069321 1 7.52
CHEMBL2180774 1 7.41
CHEMBL2180775 1 7.09
CHEMBL1086110 1 6.62
CHEMBL2070666 1 6.46
CHEMBL2070659 1 5.94

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2180771 IC50 = 3.31 nM 8.48
CHEMBL2180772 IC50 = 5.31 nM 8.28
CHEMBL2180773 IC50 = 9.3 nM 8.03
CHEMBL2069321 IC50 = 30.3 nM 7.52
CHEMBL2180774 IC50 = 39.4 nM 7.41
CHEMBL2180775 IC50 = 80.6 nM 7.09
CHEMBL1086110 IC50 = 239.0 nM 6.62
CHEMBL2070666 IC50 = 346.5 nM 6.46
CHEMBL2070659 IC50 = 1150.0 nM 5.94