Compound Detail
CHEMBL1198
PRAMOXINE 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL1198 |
| Name | PRAMOXINE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | DQKXQSGTHWVTAD-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
3
Targets
5
Activities
2
Assay Types
0
PK Parameters
20
Publications
2
Known Names
2
Indications
Molecular Properties
293.4
MW (Da)
2.97
ALogP
4
HBA
0
HBD
30.9
PSA (Ų)
0.66
QED
0
Ro5 Violations
9
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1976 |
| Availability | Prescription |
| Chirality | Achiral |
Indications
Hemorrhoids Pruritus
ATC Classification
C05AD07
pramocaine
Level 1: CARDIOVASCULAR SYSTEM
Level 2: VASOPROTECTIVES
D04AB07
pramocaine
Level 1: DERMATOLOGICALS
Level 2: ANTIPRURITICS, INCL. ANTIHISTAMINES, ANESTHETICS, ETC.
Activity Summary
IC50 3 meas. best 6.92
Ki 2 meas. best 7.29
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | Ki | 7.29 | 7.29 | 51.0 | 1 |
| Sigma non-opioid intracellular receptor 1 CHEMBL287 | IC50 | 6.92 | 6.92 | 121.0 | 1 |
| Unchecked CHEMBL612545 | Ki | 6.2 | 6.2 | 633.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 5.99 | 5.99 | 1029.0 | 1 |
| Sodium channel alpha subunits; brain (Types I, II, III) CHEMBL2096682 | IC50 | 4.67 | 4.67 | 21200.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Sigma non-opioid intracellular receptor 1 | Ki | = | 51.0 | nM | 7.29 | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | - |
| Sigma non-opioid intracellular receptor 1 | IC50 | = | 121.0 | nM | 6.92 | DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol) | - |
| Unchecked | Ki | = | 633.0 | nM | 6.2 | DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil) | - |
| Unchecked | IC50 | = | 1029.0 | nM | 5.99 | DRUGMATRIX: Sigma2 radioligand binding (ligand: [3H] Ifenprodil) | - |
| Sodium channel alpha subunits; brain (Types I, II, III) | IC50 | = | 21200.0 | nM | 4.67 | Inhibition of binding of Batrachotoxinin [3H]BTX-B to high affinity sites on vol... | 2579237 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| - | 10.6019/CHEMBL3885881 | Rattus norvegicus | 295 |
| 37468498 | 10.1038/s41467-023-40064-9 | Estrogen receptor | 3 |
| 2579237 | 10.1021/jm00381a019 | Sodium channel alpha subunits; brain (Types I, II, III) | 3 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 1A | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2A | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | 5-hydroxytryptamine receptor 2B | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Amine oxidase [flavin-containing] A | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Muscarinic acetylcholine receptor M1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Thromboxane A2 receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Prostaglandin G/H synthase 1 | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Alpha-1A adrenergic receptor | 2 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent dopamine transporter | 1 |
| 38318365 | 10.1016/j.isci.2024.108907 | Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 | 1 |
| 37468498 | 10.1038/s41467-023-40064-9 | Sodium-dependent serotonin transporter | 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 | D(1A) dopamine receptor | 1 |
| - | 10.1101/2020.04.21.054387 | SARS-CoV-2 | 1 |
Data from ChEMBL 36 via Core Engine