Histamine receptor H1. Every medicine in our data that ChEMBL or the Guide to Pharmacology records as acting on this protein, with the source for each and its current clinical trials on this site.
| Medicine | How it acts | Source | Current trials here |
|---|---|---|---|
| Diphenhydramine CHEMBL657 |
Histamine H1 receptor antagonist Antagonist Small molecule |
✓ Both | 10 |
| Desloratadine CHEMBL1172 |
Histamine H1 receptor antagonist Antagonist Small molecule |
✓ Both | 5 |
| Fexofenadine CHEMBL914 |
Histamine H1 receptor antagonist Antagonist Small molecule |
✓ Both | 5 |
| Rupatadine CHEMBL91397 |
Histamine H1 receptor antagonist Antagonist Small molecule |
✓ Both | 3 |
| Amitriptyline CHEMBL629 |
Antagonist at HRH1 Primary target Small molecule |
Guide to Pharmacology only | 2 |
| Cetirizine Hydrochloride CHEMBL1607273 |
Histamine H1 receptor antagonist Antagonist Small molecule |
✓ Both | 2 |
| Chlorpheniramine CHEMBL505 |
Histamine H1 receptor antagonist Antagonist Small molecule |
✓ Both | 2 |
| Ebastine CHEMBL305660 |
Histamine H1 receptor inverse agonist Inverse agonist Small molecule |
ChEMBL only | 2 |
| Levocetirizine CHEMBL1201191 |
Histamine H1 receptor antagonist Antagonist Small molecule |
✓ Both | 2 |
| Loratadine CHEMBL998 |
Histamine H1 receptor antagonist Antagonist Small molecule |
✓ Both | 2 |
“Both” means ChEMBL and the Guide to Pharmacology each record this medicine acting on this protein; “only” means one source records it and the other does not (often because it lists fewer secondary targets). The Guide to Pharmacology adds a medicine here only when this protein is its primary target. Medicines without a link have no page on this site yet.
| Disease | Medicines tested | Furthest trial phase |
|---|---|---|
| Asthma | 4 | Phase 3 |
| Chronic idiopathic urticaria | 3 | Phase 3 |
| Non-small cell lung carcinoma | 3 | Phase 3 |
| Rheumatoid arthritis | 3 | Phase 3 |
| Seasonal allergic rhinitis | 3 | Phase 3 |
| Nasal congestion | 2 | Phase 3 |
| Pruritus | 2 | Phase 3 |
| Atopic eczema | 2 | Phase 3 |
| Common cold | 2 | Phase 3 |
| Diabetic kidney disease | 2 | Phase 3 |
| Neuropathy | 2 | Phase 3 |
| Perennial allergic rhinitis | 2 | Phase 3 |
| Urticaria | 2 | Phase 3 |
| Ulcerative colitis | 2 | Phase 2 |
| Headache | 1 | Phase 3 |
From ChEMBL's drug-disease records, which draw on trial registries. A trial phase is not an approval; approved uses are on each medicine's page from the regulators' own records.
Which medicines act on this protein comes from two independent, expert-curated sources: ChEMBL's mechanism-of-action records (via the Open Targets Platform) and the IUPHAR/BPS Guide to PHARMACOLOGY. Each row says which of them lists it. Data from them is shared here under their share-alike licences (CC BY-SA 3.0 and 4.0).
A job re-reads both sources every 30 days. Medicines are matched to our pages by exact name or a ChEMBL-curated synonym, and to the Guide to Pharmacology by ChEMBL ID or exact name, never by a close spelling. No AI drafting. See our methodology. The Open Targets data on this page was last retrieved on 30 Sep 2026. How every register is built: methodology · fixes we have made: corrections log.
