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Assay Detail

CHEMBL4008549

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

Binding
Inhibition of human full length PDE2a using cGMP as substrate by Scintillation proximity assay
1
Total Activities
1
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

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

Publication

Design and Synthesis of Novel and Selective Phosphodiesterase 2 (PDE2a) Inhibitors for the Treatment of Memory Disorders.
Gomez L, Massari ME, Vickers T, Freestone G, Vernier W, Ly K, Xu R, McCarrick M, Marrone T, Metz M, Yan YG, Yoder ZW, Lemus R, Broadbent NJ, Barido R, Warren N, Schmelzer K, Neul D, Lee D, Andersen CB, Sebring K, Aertgeerts K, Zhou X, Tabatabaei A, Peters M, Breitenbucher JG.
J Med Chem (2017) 60 : 2037 -2051
PubMed 28165743 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 1 9.00 9.00

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL3092562 PF-05180999 1.0 1 9.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL3092562 PF-05180999 IC50 = 1.0 nM 9.00