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Assay Detail

CHEMBL4040970

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Binding
Inhibition of PDE2A (unknown origin)
3
Total Activities
3
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

Discovery of an Orally Bioavailable, Brain-Penetrating, in Vivo Active Phosphodiesterase 2A Inhibitor Lead Series for the Treatment of Cognitive Disorders.
Mikami S, Sasaki S, Asano Y, Ujikawa O, Fukumoto S, Nakashima K, Oki H, Kamiguchi N, Imada H, Iwashita H, Taniguchi T.
J Med Chem (2017) 60 : 7658 -7676
PubMed 28759228 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 3 8.69 9.07

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL370962 1 9.07
CHEMBL3092562 PF-05180999 1.0 1 9.00
CHEMBL3331521 1 8.00

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL370962 IC50 = 0.86 nM 9.07
CHEMBL3092562 PF-05180999 IC50 = 1.0 nM 9.00
CHEMBL3331521 IC50 = 10.0 nM 8.00