Assay Detail

CHEMBL4028018

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Binding

Inhibition of PDE5A1 (unknwon origin) using [3H]cGMP as substrate after 30 mins by SPA

ChEMBL ↗

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Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗

Open DB target context

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Loading context

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) is the working anchor for this assay review. Loading the live Open DB target snapshot…

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

CHEMBL1827

Anchored from Assay target.

Protein identity cGMP-specific 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	Homo sapiens
Confidence	9 — Direct single protein target
Curated By	Autocuration

Target

cGMP-specific 3',5'-cyclic phosphodiesterase (CHEMBL1827) ↗

Type	SINGLE PROTEIN
Organism	Homo sapiens

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
IC50	2	8.91	9.77

Compounds Tested

Compound	Name	Phase	Activities	Best pChEMBL
CHEMBL1520	VARDENAFIL	4.0	1	9.77
CHEMBL3769434	—	—	1	8.05

Activity Data

Compound	Name	Type	Rel.	Value	Units	pChEMBL
CHEMBL1520	VARDENAFIL	IC50	=	0.17	nM	9.77
CHEMBL3769434	—	IC50	=	8.9	nM	8.05