Tertatolol
drugOn this page
Also known as ArtexArtexalPrenalexSE-2395Tertatolol hydrochloride
Summary
Tertatolol (CHEMBL434200) is an approved small molecule (ATC C07AA16) targeting ADRB3; indicated across 1 condition including cardiovascular disorder.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Small molecule
- ATC class: C07AA16
- Targets: 1 (ADRB3)
- Indications: 1 condition
- Chemistry: 295.4 Da · C16H25NO2S
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL434200 |
| Name | Tertatolol |
| Type | Small molecule |
| Max phase | 4 |
| FDA approved | no |
| PubChem CID | 36920 |
| ATC | C07AA16 |
| Molecular formula | C16H25NO2S |
| Molecular weight | 295.4 |
| InChIKey | HTWFXPCUFWKXOP-UHFFFAOYSA-N |
SMILES: CC(C)(C)NCC(COC1=CC=CC2=C1SCCC2)O
IUPAC name: 1-(tert-butylamino)-3-(3,4-dihydro-2H-thiochromen-8-yloxy)propan-2-ol
Also known as: Artex, Artexal, Prenalex, SE-2395, Tertatolol, Tertatolol hydrochloride, TERTATOLOL, tertatolol
Patent coverage: 1,064 distinct patent families (4,546 SureChEMBL compound mentions), from 1 matched compound structure(s). Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.
Targets
Targets
Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).
| Gene | Target | Action | pAffinity | Cancer dependency | UniProt |
|---|---|---|---|---|---|
| ADRB3 | β3-adrenoceptor | Antagonist | 8.6 | 0.1% | P13945 |
Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Alpha-2A adrenergic receptor, 5-hydroxytryptamine receptor 1A, Sodium-dependent noradrenaline transporter, Sodium-dependent serotonin transporter, 5-hydroxytryptamine receptor 1A.
Bioactivity
ChEMBL activities: 6 potent at pChembl ≥ 5 of 8 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| P19327 | 8.11 | Ki | 7.71 | nM | CHEMBL_ACT_292028 |
| P19327 | 7.74 | Ki | 18.2 | nM | CHEMBL_ACT_292026 |
| P19327 | 7.73 | Ki | 18.62 | nM | CHEMBL_ACT_840082 |
| P19327 | 7.42 | Ki | 37.6 | nM | CHEMBL_ACT_292027 |
| HTR1A | 7.25 | AC50 | 56.9 | nM | CHEMBL_ACT_25165512 |
| ADRA2A | 5.18 | AC50 | 6599 | nM | CHEMBL_ACT_25156917 |
Target pathways
Aggregated over 1 target gene(s): ADRB3.
Top Reactome pathways
8 total, by targets touching each:
| Pathway | Targets | Genes |
|---|---|---|
| Signal Transduction | 1 | ADRB3 |
| Signaling by GPCR | 1 | ADRB3 |
| Class A/1 (Rhodopsin-like receptors) | 1 | ADRB3 |
| Amine ligand-binding receptors | 1 | ADRB3 |
| GPCR downstream signalling | 1 | ADRB3 |
| Adrenoceptors | 1 | ADRB3 |
| G alpha (s) signalling events | 1 | ADRB3 |
| GPCR ligand binding | 1 | ADRB3 |
Dominant GO biological processes
| GO term | Targets |
|---|---|
| diet induced thermogenesis | 1 |
| norepinephrine-epinephrine-mediated vasodilation involved in regulation of systemic arterial blood pressure | 1 |
| carbohydrate metabolic process | 1 |
| generation of precursor metabolites and energy | 1 |
| energy reserve metabolic process | 1 |
| G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger | 1 |
| adenylate cyclase-modulating G protein-coupled receptor signaling pathway | 1 |
| adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway | 1 |
| response to cold | 1 |
| heat generation | 1 |
| negative regulation of multicellular organism growth | 1 |
| eating behavior | 1 |
| positive regulation of MAPK cascade | 1 |
| negative regulation of smooth muscle contraction | 1 |
| brown fat cell differentiation | 1 |
Indications & clinical
Indications
1 indication (1 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).
| Indication | Trial phase | MONDO | EFO |
|---|---|---|---|
| cardiovascular disorder | 4 | MONDO:0004995 | EFO:0000319 |
Clinical trials
Total trials: 0.
Clinical evidence (CIViC)
No CIViC predictive evidence (expected for non-precision-medicine drugs).
Pharmacology
Pharmacogenomics
No PharmGKB pharmacogenomic data curated for this drug.
Related molecules
Related molecules
Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.
107 molecules share ≥1 primary target. Top 60 by shared-target count:
| Molecule | Source | Status | Shared targets |
|---|---|---|---|
| CRIZOTINIB | ChEMBL + PubChem | Phase 4 (approved) | ADRB3 |
| DIHYDROERGOTAMINE | ChEMBL + PubChem | Phase 4 (approved) | ADRB3 |
| RIFAMPIN | ChEMBL + PubChem | Phase 4 (approved) | ADRB3 |
| TEGASEROD | ChEMBL + PubChem | Phase 4 (approved) | ADRB3 |
| AMIODARONE | ChEMBL | Phase 4 (approved) | ADRB3 |
| AMLODIPINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| ARIPIPRAZOLE | ChEMBL | Phase 4 (approved) | ADRB3 |
| ASTEMIZOLE | ChEMBL | Phase 4 (approved) | ADRB3 |
| BEPRIDIL | ChEMBL | Phase 4 (approved) | ADRB3 |
| BISOPROLOL | ChEMBL | Phase 4 (approved) | ADRB3 |
| BOSUTINIB | ChEMBL | Phase 4 (approved) | ADRB3 |
| BROMOCRIPTINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| CARVEDILOL | ChEMBL | Phase 4 (approved) | ADRB3 |
| CELECOXIB | ChEMBL | Phase 4 (approved) | ADRB3 |
| CHLORPROMAZINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| CLOTRIMAZOLE | ChEMBL | Phase 4 (approved) | ADRB3 |
| DANAZOL | ChEMBL | Phase 4 (approved) | ADRB3 |
| DIETHYLSTILBESTROL | ChEMBL | Phase 4 (approved) | ADRB3 |
| DISOPYRAMIDE | ChEMBL | Phase 4 (approved) | ADRB3 |
| DOXAZOSIN | ChEMBL | Phase 4 (approved) | ADRB3 |
| EBASTINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| ECONAZOLE | ChEMBL | Phase 4 (approved) | ADRB3 |
| EPINEPHRINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| ETHINYL ESTRADIOL | ChEMBL | Phase 4 (approved) | ADRB3 |
| FELODIPINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| FENOFIBRATE | ChEMBL | Phase 4 (approved) | ADRB3 |
| FENOTEROL | ChEMBL | Phase 4 (approved) | ADRB3 |
| FLUPHENAZINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| FORMOTEROL | ChEMBL | Phase 4 (approved) | ADRB3 |
| HALOPERIDOL | ChEMBL | Phase 4 (approved) | ADRB3 |
| IBUPROFEN | ChEMBL | Phase 4 (approved) | ADRB3 |
| ISOPROTERENOL | ChEMBL | Phase 4 (approved) | ADRB3 |
| IVACAFTOR | ChEMBL | Phase 4 (approved) | ADRB3 |
| LABETALOL | ChEMBL | Phase 4 (approved) | ADRB3 |
| LEVOBUNOLOL | ChEMBL | Phase 4 (approved) | ADRB3 |
| LORATADINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| LOVASTATIN | ChEMBL | Phase 4 (approved) | ADRB3 |
| MEMANTINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| MICONAZOLE | ChEMBL | Phase 4 (approved) | ADRB3 |
| MIRABEGRON | ChEMBL | Phase 4 (approved) | ADRB3 |
| MONTELUKAST | ChEMBL | Phase 4 (approved) | ADRB3 |
| NEFAZODONE | ChEMBL | Phase 4 (approved) | ADRB3 |
| NELFINAVIR | ChEMBL | Phase 4 (approved) | ADRB3 |
| NOREPINEPHRINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| OXICONAZOLE | ChEMBL | Phase 4 (approved) | ADRB3 |
| PAMIDRONIC ACID | ChEMBL | Phase 4 (approved) | ADRB3 |
| PERGOLIDE | ChEMBL | Phase 4 (approved) | ADRB3 |
| PHENYLEPHRINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| PIMOZIDE | ChEMBL | Phase 4 (approved) | ADRB3 |
| PINDOLOL | ChEMBL | Phase 4 (approved) | ADRB3 |
| PRACTOLOL | ChEMBL | Phase 4 (approved) | ADRB3 |
| PROCHLORPERAZINE | ChEMBL | Phase 4 (approved) | ADRB3 |
| PROPAFENONE | ChEMBL | Phase 4 (approved) | ADRB3 |
| PROPRANOLOL | ChEMBL | Phase 4 (approved) | ADRB3 |
| RALOXIFENE | ChEMBL | Phase 4 (approved) | ADRB3 |
| RITONAVIR | ChEMBL | Phase 4 (approved) | ADRB3 |
| SALMETEROL | ChEMBL | Phase 4 (approved) | ADRB3 |
| SIMVASTATIN | ChEMBL | Phase 4 (approved) | ADRB3 |
| SIROLIMUS | ChEMBL | Phase 4 (approved) | ADRB3 |
| SOTALOL | ChEMBL | Phase 4 (approved) | ADRB3 |
Related Atlas pages
- Genes: ADRB3
- Diseases: cardiovascular disorder
- Drugs: Crizotinib, Dihydroergotamine, Rifampin, Tegaserod, Amiodarone, Amlodipine, Aripiprazole, Astemizole, Bepridil, Bisoprolol, Bosutinib, Bromocriptine, Carvedilol, Celecoxib, Chlorpromazine, Clotrimazole, Danazol, Diethylstilbestrol, Disopyramide, Doxazosin, Ebastine, Econazole, Epinephrine, Ethinyl Estradiol, Felodipine, Fenofibrate, Fenoterol, Fluphenazine, Formoterol, Haloperidol, Ibuprofen, Isoproterenol, Ivacaftor, Labetalol, Levobunolol, Loratadine, Lovastatin, Memantine, Miconazole, Mirabegron, Montelukast, Nefazodone, Nelfinavir, Norepinephrine, Oxiconazole, Pamidronic Acid, Pergolide, Phenylephrine, Pimozide, Pindolol, Practolol, Prochlorperazine, Propafenone, Propranolol, Raloxifene, Ritonavir, Salmeterol, Simvastatin, Sirolimus, Sotalol