Target's General Information
Target ID T47094
Target Name Substance-P receptor (TACR1)
Synonyms Tachykinin receptor 1; Tachykinin neurokinin 1 receptor; Tachykinin 1 receptor; TACR1; Substance P receptor; SPR; Neurokinin 1 receptor; NK-1R; NK-1 receptor
Target Type Successful
Gene Name TACR1
Biochemical Class GPCR rhodopsin
UniProt ID NK1R_HUMAN
Target's Expression Profile in Disease Related Tissue between Patients and Normal People
Disease Asthma
Example drug Nolpitantium besilate Discontinued in Phase 2 [1], [2], [3], [4]
Tissue Nasal and bronchial airway
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 0.02
Z-score: 0.09
P-value: 9.91E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Chronic obstructive pulmonary disease
Example drug CS-003 Discontinued in Phase 2 [5], [3], [4]
Tissue Lung tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.05
Z-score: -0.28
P-value: 9.59E-02
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Chronic obstructive pulmonary disease
Example drug CS-003 Discontinued in Phase 2 [5], [3], [4]
Tissue Small airway epithelium
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 0.05
Z-score: 0.3
P-value: 1.38E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Irritable bowel syndrome
Example drug DNK-333 Discontinued in Phase 2 [5], [3], [4]
Tissue Rectal colon tissue
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 0.04
Z-score: 0.2
P-value: 1.94E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Depression
Example drug Aprepitant Approved [3], [4], [6], [7]
Tissue Pre-frontal cortex
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 0.02
Z-score: 0.11
P-value: 7.24E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Schizophrenia
Example drug GSK1144814 Phase 1 [8], [3], [4]
Tissue Pre-frontal cortex
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: 0.02
Z-score: 0.07
P-value: 7.40E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Disease Schizophrenia
Example drug GSK1144814 Phase 1 [8], [3], [4]
Tissue Superior temporal cortex
Level of differential expression between the patients in the disease section of the tissue and the tissues of healthy individual Fold-change: -0.02
Z-score: -0.18
P-value: 8.57E-01
Target gene expression profiles of the patients in the disease section of the tissue
Target gene expression profiles in the tissue of healthy individual
Target's Expression Profile across Various Tissues of Healthy Individual
References
REF 1 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 2107).
REF 2 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800003930)
REF 3 Interpreting expression profiles of cancers by genome-wide survey of breadth of expression in normal tissues. Genomics 2005 Aug;86(2):127-41.
REF 4 NCBI GEO: archive for functional genomics data sets--update. Nucleic Acids Res. 2013 Jan;41(Database issue):D991-5.
REF 5 Emerging drugs for the treatment of chronic obstructive pulmonary disease. Expert Opin Emerg Drugs. 2006 May;11(2):275-91.
REF 6 Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
REF 7 Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800009602)
REF 8 ClinicalTrials.gov (NCT01090440) Pharmacokinetics, Effect of Food, Safety and Tolerability of a New Tablet Formulation of GSK1144814 in Healthy Subjects. U.S. National Institutes of Health.

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