Molecular Target Synopsis
Overview
Domains and Structures
Drugs and Clinical Candidates
Druggability
Chemistry
Ligand Efficiency Plot
Pathways
Family Cladogram
Interaction Network
Gene Expression
Gene Copy Number Variation
RNAi
Mutations
Germline Genetics

TACR1 (P25103) - Overview - Molecular Target Synopsis

Protein


TACR1, Substance-P receptor
UniProt P25103

Also Known as NK1R_HUMAN, TACR1, NK1R, TAC1R

This is a receptor for the tachykinin neuropeptide substance P. It is probably associated with G proteins that activate a phosphatidylinositol-calcium second messenger system. The rank order of affinity of this receptor to tachykinins is: substance P > substance K > neuromedin-K. Interacts with ARRB1.

6J20
CRYSTAL STRUCTURE OF THE HUMAN NK1 SUBSTANCE P RECEPTOR
RCSB/PDB
Inspect Structure
See all 3D Structures for TACR1

Isoforms / Transcripts (Protein Coding)


Protein Length Ensembl Gene Ensembl Transcript Ensembl Protein Uniprot Isoform
407ENSG00000115353ENST00000305249ENSP00000303522P25103-1
311ENSG00000115353ENST00000409848ENSP00000386448P25103-3

Drugs


TACR1 is targeted by Approved Drugs Netupitant, Aprepitant, Rolapitant Hydrochloride. (see details)
Netupitant
Aprepitant
Rolapitant Hydrochloride

Sub-cellular localization


UniProt: TACR1 is active in the following subcellular-locations: cell membrane.
GO terms: TACR1 is active in the following subcellular-locations: integral component of plasma membrane, plasma membrane, sperm flagellum, sperm head, sperm midpiece.



UniProt
GO terms

Gene Copy Number Variation


In COSMIC - Cell Lines Project TACR1 has gain in 1 cell-lines, loss in 0 cell-lines and no signal in 1004 cell-lines. (see details)

Gene Expression


In NCI60, the highest expressing cell lines are: MCF7, TK_10, SK_OV_3

In Array Express (RNA-seq of 675 commonly used human cancer cell lines), the highest expressing cell lines are: NCI-H1623, G28T, G124

In Array Express (RNA-seq of long poly adenylated RNA and long non poly adenylated RNA from ENCODE cell lines), the highest expressing cell lines are: SK-N-SH, NHLF, HSMM

(see details)

3D Structures


For TACR1 there are:
9 structures (9 chains) solved
6 are solved in complex with at least one small molecule ligand



(see details)
Molecular Target 3D Synopsis

Screening and Chemistry


TACR1 has been screened with 3805 compounds (5751 bioactivities), 2226 compounds have bioactivities that show binding affinity of <= 500nM (2849 bioactivities). (see details)