ROLAPITANT

ROLAPITANT : Antagonist of TACR1

Structure

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Information

TACR1

Antagonist

up to 100 nM

In Vitro Validations

Uniprot ID: P25103

Target Class: GPCR

Target SubClass: NK-1 Receptor

Potency: Ki

Potency Value: 0.66 nM

Potency Assay: Radio ligand binding assay

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

Target aliases:

Substance-P receptor, TAC1R, NK1R, TACR1, NK1R_HUM ...

DOI Reference: 10.1016/j.pbb.2012.03.021

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family: >1000-fold for the human NK1 receptor compared to the human NK2 and NK3 receptors. Selectivity outside target family: The affinity of rolapitant for a panel of over 100 receptors, transporters, enzymes and ion channels was also tested. Rolapitant did not show activity to any of these targets, further confirming its selectivity for the NK1 receptor.

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