Compound Detail
CHEMBL524
METHOXAMINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL524 |
| Name | METHOXAMINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | WJAJPNHVVFWKKL-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
20
Publications
4
Known Names
3
Indications
Molecular Properties
211.3
MW (Da)
1.08
ALogP
4
HBA
2
HBD
64.7
PSA (Ų)
0.78
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1982 |
| Availability | Discontinued |
| Chirality | Racemic |
Indications
Cardiovascular Diseases Fecal Incontinence Urinary Incontinence
ATC Classification
C01CA10
methoxamine
Level 1: CARDIOVASCULAR SYSTEM
Level 2: CARDIAC THERAPY
Activity Summary
EC50 2 meas. best 6.14
IC50 2 meas. best 5.44
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Alpha-1A adrenergic receptor CHEMBL229 | EC50 | 6.14 | 6.14 | 720.0 | 1 |
| Unchecked CHEMBL612545 | EC50 | 6.14 | 6.14 | 720.0 | 1 |
| Adrenergic receptor alpha-2 CHEMBL2093864 | IC50 | 5.44 | 5.44 | 3600.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Alpha-1A adrenergic receptor | EC50 | = | 720.0 | nM | 6.14 | Alpha-1 adrenergic receptor agonist activity in rabbit ear artery | 6118438 |
| Unchecked | EC50 | = | 720.0 | nM | 6.14 | Alpha-1 adrenergic receptor activation causing vasoconstriction in the isolated ... | 6120238 |
| Adrenergic receptor alpha-2 | IC50 | = | 3600.0 | nM | 5.44 | 50% inhibition of specific [3H]clonidine binding (0.4 nM) to Alpha-2 adrenergic ... | 6142954 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 37468498 | 10.1038/s41467-023-40064-9 | Thromboxane A2 receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Prostaglandin G/H synthase 1 | 2 |
| 2884315 | 10.1021/jm00389a023 | Adrenergic receptor alpha-2 | 2 |
| 6827543 | 10.1021/jm00356a026 | Adrenergic receptor alpha-1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 2 |
| 191614 | 10.1021/jm00214a028 | Unchecked | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| 22961681 | 10.1124/dmd.112.047068 | Bile salt export pump | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent noradrenaline transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Acetylcholinesterase | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent dopamine transporter | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Voltage-gated inwardly rectifying potassium channel KCNH2 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | D(1A) dopamine receptor | 1 |
| - | 10.1101/2020.04.21.054387 | SARS-CoV-2 | 1 |
| 6142954 | 10.1021/jm00370a011 | Oryctolagus cuniculus | 1 |
| 38318365 | 10.1016/j.isci.2024.108907 | Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 | 1 |
| 6120238 | 10.1021/jm00344a009 | Unchecked | 1 |
| 6118438 | 10.1021/jm00144a012 | Oryctolagus cuniculus | 1 |
| 6118438 | 10.1021/jm00144a012 | Alpha-1A adrenergic receptor | 1 |
| 6142954 | 10.1021/jm00370a011 | Adrenergic receptor alpha-2 | 1 |
Data from ChEMBL 36 via Core Engine