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Assay Detail

CHEMBL4011532

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

Binding
Inhibition of N-terminal GST-tagged full length recombinant human PDE11A4 expressed in Baculovirus infected Sf9 insect cells assessed as decrease in FAM-cAMP hydrolysis after 1 hr by fluorescence polarization assay
2
Total Activities
2
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

Dual 3',5'-cyclic-AMP and -GMP phosphodiesterase 11A (CHEMBL2717)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of Selective Phosphodiesterase 1 Inhibitors with Memory Enhancing Properties.
Dyck B, Branstetter B, Gharbaoui T, Hudson AR, Breitenbucher JG, Gomez L, Botrous I, Marrone T, Barido R, Allerston CK, Cedervall EP, Xu R, Sridhar V, Barker R, Aertgeerts K, Schmelzer K, Neul D, Lee D, Massari ME, Andersen CB, Sebring K, Zhou X, Petroski R, Limberis J, Augustin M, Chun LE, Edwards TE, Peters M, Tabatabaei A.
J Med Chem (2017) 60 : 3472 -3483
PubMed 28406621 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.10 6.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4067682 1 6.55
CHEMBL1463540 1 5.64

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4067682 IC50 = 280.0 nM 6.55
CHEMBL1463540 IC50 = 2300.0 nM 5.64