APREPITANT

APREPITANT : Antagonist of TACR1

Structure

SERP Rating

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Information

TACR1

Antagonist

up to 10 nM

Probe Availability:

In Vitro Validations

Uniprot ID: P25103

Target Class: GPCR

Target SubClass: NK-1 Receptor

Potency: Kd

Potency Value: 0.2 nM

Potency Assay: Saturation binding analysis with increasing concentrations of [3H]-Aprepitant using Sf9 membranes

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

Target aliases:

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

DOI Reference: 10.1021/jm980299k

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Selectivity within target family (DOI: 10.1016/S0028-3908(99)00172-0) hNK2 IC50 4500 nM hNK3 IC50 300 nM Outside target family: Ca2+ IC50 8000 nM Na+ IC50 > 10000 nM

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