> Trialight public data. Index of pages: https://trialight.com/llms.txt
> Web page: https://trialight.com/data/target/hcrtr1-fe2b8b6d-e646-5d68-8fcc-5f3c29444e6b
> Record changed: 2026-10-13

# HCRTR1

ENSG00000121764

Target class

GPCR

Chromosome

1

Approved drugs

4

Clinical candidates (approved and in development)

8

## Clinical evidence

**Approved drugs**

4

**Clinical candidates (approved and in development)**

8

## Druggability

**Chemical probe available**

Yes

## Names

**Target name**

HCRTR1

**Gene name**

Hypocretin receptor 1

**Gene symbol**

HCRTR1

**Protein name**

Orexin/Hypocretin receptor type 1 (Hypocretin receptor type 1) (Orexin receptor type 1) (Ox-1-R) (Ox1-R) (Ox1R)

### Other names (3)

- OX1R
- OXR1
- ORXR1

## Classification

**Gene biotype**

Protein coding

**Gene family**

Hypocretin receptors

**Target class**

GPCR

**Target type**

Human gene

## Expression and localisation

**Tissues expressed in**

2

**Highest tissue expression**

1.32

**Tissue specificity (Gini)**

0.571

**Tissue specificity (tau)**

0.847

## Pathways and interactions

**KEGG gene identifiers**

- hsa:3061

**Protein interaction confidence**

0.799571

**Protein interaction partners**

7

### Reactome pathways (2)

- R-HSA-389397
- R-HSA-416476

## Genomic location

**End position**

31632518

**Start position**

31617660

**Chromosome**

1

**Strand**

Forward

## Identifiers

**Ensembl gene ID**

ENSG00000121764

**HGNC ID**

HGNC:4848

Source: [www.genenames.org](https://www.genenames.org/data/gene-symbol-report/#!/hgnc%5Fid/HGNC:4848)

**NCBI Gene ID**

3061

**UniProt ID**

O43613

## Cellular location

- Cell membrane
- Multi-pass membrane protein .

### Publication evidence (2)

- PubMed 26950369  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/26950369/)
- PubMed 9491897  
Source: [pubmed.ncbi.nlm.nih.gov](https://pubmed.ncbi.nlm.nih.gov/9491897/)

## Tissue expression

**Tissue specificity (tau)**

0.846913

**Expression inequality (Gini)**

0.570534

### Highest expression

Expression in transcripts per million

**Thyroid**

1.32

**Kidney - Medulla**

1.05

**Brain - Hypothalamus**

0.98

**Pituitary**

0.95

**Esophagus - Muscularis**

0.63

### All tissues (54)

Expression in transcripts per million

- Thyroid1.32
- Kidney - Medulla1.05
- Brain - Hypothalamus0.98
- Pituitary0.95
- Esophagus - Muscularis0.63
- Artery - Aorta0.52
- Breast - Mammary Tissue0.44
- Esophagus - Gastroesophageal Junction0.43
- Adipose - Visceral (Omentum)0.42
- Brain - Cortex0.41
- Adipose - Subcutaneous0.4
- Artery - Coronary0.32
- Brain - Frontal Cortex (BA9)0.3
- Heart - Left Ventricle0.24
- Testis0.21
- Artery - Tibial0.21
- Muscle - Skeletal0.2
- Brain - Anterior cingulate cortex (BA24)0.18
- Fallopian Tube0.18
- Brain - Cerebellum0.17
- Brain - Substantia nigra0.16
- Colon - Sigmoid0.15
- Brain - Cerebellar Hemisphere0.14
- Uterus0.14
- Brain - Hippocampus0.14

And 29 more, listed on the interactive page.

## Biological functions

### Biological processes (5)

- GO:0007200  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007200)
- GO:0007218  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007218)
- GO:0007268  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007268)
- GO:0007631  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0007631)
- GO:0051480  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0051480)

### Cellular components

- GO:0005886  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005886)

### Molecular functions (3)

- GO:0004930  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0004930)
- GO:0005515  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0005515)
- GO:0016499  
Source: [www.ebi.ac.uk](https://www.ebi.ac.uk/QuickGO/term/GO:0016499)

## Related records

### Trials (203)

- 15-Day Repeated-Dose Study With SB-649868 And Its Interaction With CYP3A4 Isoenzyme In Healthy Male Subjects.
- 2-Part Multiple Ascending Dose Study for Safety and Pharmacokinetics in Healthy and Elderly Subjects
- A 2-Part Single Dose Study to Assess the Safety, Tolerability, Pharmacokinetics, and Pharmacodynamics of E2006
- A 2-Part Study to Assess Potential Metabolism-Based Drug-Drug Interactions of E2006 When Coadministered With Itraconazole, Rifampin, Midazolam, or Bupropion
- A Clinical Pharmacology Study of TS-142 in Patients with Obstructive Sleep Apnea Hypopnea.
- A Clinical Study to Assess Next-day Driving Performance Following Administration of ACT-541468 in Middle-aged and Elderly Subjects
- A Clinical Study to Evaluate the Pharmacokinetic Profile of SB-649868 in Elderly and Female Population
- A Clinical Study to Investigate the Food Effect on the Pharmacokinetics of ACT-541468 in Healthy Male Subjects
- A Clinical Study to Investigate the Potential Interactions Between Food and ACT-541468 and Between ACT-541468 and Midazolam
- A Comparison of the Physiological and Behavioral Effects of Suvorexant and Zolpidem in Healthy Volunteers: A Randomized, Double-blind, Placebo Controlled Study
- A Dual Orexin Receptor Antagonist to Reduce Biomarkers of Neurodegeneration in Adults With Insomnia.
- A Food Effect Study of TS-142 in Healthy Subjects
- A Long Term Safety Study of Suvorexant in Participants With Primary Insomnia (MK-4305-009 AM3)
- A Multicenter Observational Study of Lemborexant on Insomnia Patients With Psychiatric Disorders
- A Multicenter, Randomized, Double-blind, Placebo-controlled, Parallel-group, Bayesian Adaptive Randomization Design, Dose Response Study of the Efficacy of E2006 in Adults and Elderly Subjects With Chronic Insomnia
- A Pharmacokinetic Study of TS-142 in Patients with Hepatic Impairment
- A Phase 1 Trial to Investigate the Biological Equivalence of 5 × 10 mg Tablets and 2 × 25 mg Tablets of Daridorexant in Healthy Male and Female Japanese Participants
- A Phase I Study of TS-142 in Healthy Participants (Repeated Doses)
- A Phase I Study of TS-142 in Healthy Participants (Single Doses)
- A Pilot Study of Suvorexant for Insomnia in Parkinson Disease

### Drugs (8)

- Almorexant Orexin receptor antagonist
- Daridorexant Orexin receptor antagonist
- Daridorexant hydrochloride Orexin receptor 1 antagonist
- Filorexant Orexin receptor antagonist
- Lemborexant Orexin receptor 1 antagonist
- [Orn-0829 hydrate](https://trialight.com/data/asset/orn-0829-hydrate-92f99085-a773-43bb-b77b-07a441e66c94.md) Orexin receptor antagonist
- SB-649868 Orexin receptor 1 antagonist
- Suvorexant Orexin receptor antagonist

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