BIIE0246

Protein target name:

NPY2R

Mechanism of action:

Antagonist

Recommended Concentration for use in cells:

up to 1 uM

Probe Information

Target and Probe Information

Target Details

Target class:

GPCR

Subclass:

Neuropeptide Y receptor Y2

HUGO ID:

HGNC:7957

Entrez gene ID:

4887

UNIPROT ID:

P49146

Target alias:

NPY2-R

Probe Details

Chemical Probes Portal ID:

CPP2256

PubChem CID:

5311024

ChEMBL ID:

CHEMBL540989

SMILES string:

NC(=NCCC[C@@H](C(=O)NCCn1c(=O)n(n(c1=O)c1ccccc1)c1ccccc1)NC(=O)CC1(CCCC1)CC(=O)N1CCN(CC1)C1c2ccccc2NC(=O)c2c1cccc2)N

InChi Key:

RSJAXPUYVJKAAA-JPGJPTAESA-N

Control compound:

BIIE0212

Validation in Cells and Model Organisms

In vitro validation

On target activity

Structure-activity relationship:

In cell validation

On target activity in cells

Potency in cells:

IC50

3.3 nM

Potency assay (cells):

Radioligand binding Assay

Off target activity in cells

Probe Selectivity in Cell:

Selectivity vs family members was assessed on rat homologs using radioligand binding assay in HEK293T cells expressing respective receptor: rY2R 15 nM, rY1R, rY4R and rY5R >10 uM IC50; no cross-reactivity with 60 other receptors.

In vivo validation

Organism:

Mouse, Rat, Rabbit

Dose:

3 mg/Kg

Route of delivery:

Intraperitoneal

Plasma half life:

<3h

Primary Reference

Reference (doi):

10.1038/sj.bjp.0703162 10.1016/s0014-2999(99)00650-0

Reference (PMID):

10725255 10611450

External Resources

Available data:

opnME | Boehringer Ingelheim Open Innovation Portal

BIIE0246

Probe Information

Target Details

NPY2-R

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

External Resources

Supporting Organizations

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BIIE0246

Probe Information

Target Details

NPY2-R

Probe Details

In vitro validation

In cell validation

In vivo validation

Primary Reference

External Resources

Supporting Organizations

Interested in supporting the portal?