JNJ-31020028

JNJ-31020028 : Antagonist of NPY2R

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe JNJ-31020028 is in the process of SERP review.

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Information

NPY2R

Antagonist

up to 1 uM

In Vitro Validations

Uniprot ID: P49146

Target Class: GPCR

Target SubClass: Neuropeptide Y receptor

PDB ID for probe-target interaction (3D structure): 7DDZ

Target aliases:

Neuropeptide Y receptor type 2, NPY2R, NPY2R_HUMAN ...

DOI Reference: 10.1007/s00213-009-1726-x

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay, off target (cells): >100-fold selective versus human Y1, Y4, and Y5 receptors in radioligand binding assays

Potency assay (off target): The selectivity of JNJ-31020028 was evaluated in a large variety of ion channels, transporters, receptor binding, and kinase assays. These assays were performed by CEREP and Millipore, respectively.

Probe Selectivity in Vitro:

JNJ-31020028 was assayed by binding in a panel of 50 receptors, ion channels, and transporters assays including adenosine (A1, A2A, A3), adrenergic (α1, α2, β1), angioten- sin (AT1), dopamine (D1, D2), bradykinin (B2), cholecysto- kinin (CCKA), galanin (GAL 2 ), melatonin (ML 1 ), muscarinic (M1, M2, M3), neurotensin (NT1), neurokinin (NK2, NK3), opiate (μ, κ, δ), serotonin (5-HT1A, 5-HT1B, 5-HT 2A , 5-HT 3 , 5-HT 5A , 5-HT 6 , 5-HT 7 ), somatostatin, vasopressin (V 1a), norepinephrine transporter, dopamine transporter, and ion channels (sodium, calcium, potassium, and chloride). The Y2 antagonist at concentrations up to 10μM had no significant affinity for any receptor/transport- er/ion channel (<50% inhibition at 10μM) other than the Y2 receptor. Selectivity of Y2 antagonist was further evaluated in a panel comprised of 65 kinases. JNJ-31020028 (10μM) did not inhibit any of the kinase included in the panel

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 8 Dec 2025 )

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

JNJ 31020028 is a high quality, potent and selective antagonist of the NPYY2 receptor. Although it was found to be ineffective in a variety of anxiety models, receptor occupancy and pharmacodynamic marker modulation in the brain have been demonstrated in the rat. It can be confidently used to study the biology of this receptor in vitro and in vivo in the rat, using subcutaneous dosing.

(last updated: 11 Dec 2025 )