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Assay Detail

CHEMBL2187458

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Binding
Inhibition of recombinant PDE10A1 expressed in baculovirus infected SF21 cells using [3H]cAMP as substrate after 30 mins by liquid scintillation counting
10
Total Activities
10
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

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 10 8.24 9.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL2069321 1 9.55
CHEMBL2180775 1 9.15
CHEMBL2070666 1 8.83
CHEMBL2070659 1 8.45
CHEMBL1086110 1 8.15
CHEMBL1085374 1 8.15
CHEMBL2180773 1 8.02
CHEMBL2180771 1 7.62
CHEMBL2180774 1 7.34
CHEMBL2180772 1 7.11

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL2069321 IC50 = 0.28 nM 9.55
CHEMBL2180775 IC50 = 0.7 nM 9.15
CHEMBL2070666 IC50 = 1.48 nM 8.83
CHEMBL2070659 IC50 = 3.55 nM 8.45
CHEMBL1086110 IC50 = 7.0 nM 8.15
CHEMBL1085374 IC50 = 7.0 nM 8.15
CHEMBL2180773 IC50 = 9.6 nM 8.02
CHEMBL2180771 IC50 = 23.7 nM 7.62
CHEMBL2180774 IC50 = 45.5 nM 7.34
CHEMBL2180772 IC50 = 77.2 nM 7.11