Compound Detail
CHEMBL677
LEVONORDEFRIN 💊 Approved Drug
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💊 Approved Drug
Basic Information
| ChEMBL ID | CHEMBL677 |
| Name | LEVONORDEFRIN |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | GEFQWZLICWMTKF-CDUCUWFYSA-N |
| Therapeutic | ✓ Yes |
3
Targets
8
Activities
2
Assay Types
0
PK Parameters
17
Publications
13
Known Names
1
Mechanisms
Molecular Properties
183.2
MW (Da)
0.48
ALogP
4
HBA
4
HBD
86.7
PSA (Ų)
0.50
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 1960 |
| Availability | Discontinued |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Adrenergic receptor alpha-2 agonist | AGONIST | Adrenergic receptor alpha-2 | ✓ | ✓ |
Activity Summary
Ki 6 meas. best 8.11
EC50 2 meas. best 7.72
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Adrenergic receptor alpha-2 CHEMBL2093864 | Ki | 8.11 | 7.4 | 7.7 | 2 |
| Unchecked CHEMBL612545 | EC50 | 7.72 | 7.72 | 19.0 | 1 |
| Adrenergic receptor alpha-1 CHEMBL1907610 | EC50 | 6.11 | 6.11 | 776.0 | 1 |
| Adrenergic receptor alpha-1 CHEMBL1907610 | Ki | 5.44 | 5.2067 | 3600.0 | 3 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Adrenergic receptor alpha-2 | Ki | = | 7.7 | nM | 8.11 | Displacement of [3H]clonidine from Alpha-2 adrenergic receptor of rat brain memb... | 6296387 |
| Unchecked | EC50 | = | 19.0 | nM | 7.72 | Effective concentration for inhibition of neurotransmission in field-stimulated,... | 7562902 |
| Adrenergic receptor alpha-2 | Ki | = | 205.0 | nM | 6.69 | Alpha-2 adrenergic receptor binding affinity was tested against membrane prepara... | 8709134 |
| Adrenergic receptor alpha-1 | EC50 | = | 776.0 | nM | 6.11 | Effective dose for contraction of reserpine-pretreated rat vas deferens. | 7562902 |
| Adrenergic receptor alpha-1 | Ki | = | 3600.0 | nM | 5.44 | Compound was evaluated for inhibition of [3H]prazosin binding to Alpha-1 adrener... | 7328589 |
| Adrenergic receptor alpha-1 | Ki | = | 7300.0 | nM | 5.14 | Compound was evaluated for inhibition of [3H]prazosin binding to Alpha-1 adrener... | 7328589 |
| Adrenergic receptor alpha-1 | Ki | = | 9221.0 | nM | 5.04 | Alpha-1 adrenergic receptor binding affinity in rat brain membranes | 8709134 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 7328589 | 10.1021/jm00142a027 | Adrenergic receptor alpha-1 | 3 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 23571415 | 10.1124/mol.112.084152 | Solute carrier organic anion transporter family member 1B1 | 1 |
| 38318365 | 10.1016/j.isci.2024.108907 | Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| - | 10.1101/2020.04.03.023846 | SARS-CoV-2 | 1 |
| 23571415 | 10.1124/mol.112.084152 | Solute carrier organic anion transporter family member 1B3 | 1 |
| 3005570 | 10.1021/jm00152a017 | Erythrocyte beta receptor | 1 |
| 8709134 | 10.1021/jm9506074 | Adrenergic receptor alpha | 1 |
| 8709134 | 10.1021/jm9506074 | Adrenergic receptor alpha-2 | 1 |
| 8709134 | 10.1021/jm9506074 | Adrenergic receptor alpha-1 | 1 |
| 6296387 | 10.1021/jm00354a001 | Adrenergic receptor alpha-2 | 1 |
| 7562902 | 10.1021/jm00019a001 | Unchecked | 1 |
| 7562902 | 10.1021/jm00019a001 | Adrenergic receptor alpha-1 | 1 |
Data from ChEMBL 36 via Core Engine