Assay Detail

CHEMBL4028062

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

Binding

Displacement of radiolabeled 4-(azetidin-1-yl)-3-[5-[4-(trifluoromethyl)phenyl]-1H-pyrazol-4-yl]-1-(tritritiomethyl)pyrazolo[3,4-d]pyrimidine from PDE2A in rat striatal membranes after 30 mins by liquid scintillation counting method

ChEMBL ↗

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Target

cGMP-dependent 3',5'-cyclic phosphodiesterase (CHEMBL4650) ↗

Open DB target context

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Loading context

cGMP-dependent 3',5'-cyclic phosphodiesterase (CHEMBL4650) is the working anchor for this assay review. Loading the live Open DB target snapshot…

Primary target cGMP-dependent 3',5'-cyclic phosphodiesterase

CHEMBL4650

Anchored from Assay target.

Protein identity cGMP-dependent 3',5'-cyclic phosphodiesterase

Disease frame Disease evidence pending

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Review focus Open DB context pending

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Total Activities

Compounds Tested

Activity Types

Assay Parameters

Assay Information

Assay Type	Binding
Organism	Rattus norvegicus
Tissue	Striatum
Subcellular	Membrane
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

cGMP-dependent 3',5'-cyclic phosphodiesterase (CHEMBL4650) ↗

Type	SINGLE PROTEIN
Organism	Rattus norvegicus

Publication

Identification of a Potent, Highly Selective, and Brain Penetrant Phosphodiesterase 2A Inhibitor Clinical Candidate.

Helal CJ, Arnold E, Boyden T, Chang C, Chappie TA, Fisher E, Hajos M, Harms JF, Hoffman WE, Humphrey JM, Pandit J, Kang Z, Kleiman RJ, Kormos BL, Lee CW, Lu J, Maklad N, McDowell L, McGinnis D, O'Connor RE, O'Donnell CJ, Ogden A, Piotrowski M, Schmidt CJ, Seymour PA, Ueno H, Vansell N, Verhoest PR, Yang EX.
J Med Chem (2018) 61 : 1001 -1018
PubMed 29293004 · DOI

Activity Statistics

Type	Count	Avg pChEMBL	Best pChEMBL
Ki	1	8.38	8.38

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL3092562	PF-05180999	1.0	1	8.38

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL3092562	PF-05180999	Ki	=	4.2	nM	8.38