Compound Detail
CHEMBL1255582
FIPAMEZOLE 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL1255582 |
| Name | FIPAMEZOLE |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | KXSUAWAUCNFBQJ-UHFFFAOYSA-N |
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
2
Known Names
1
Indications
1
Mechanisms
Molecular Properties
230.3
MW (Da)
3.00
ALogP
1
HBA
1
HBD
28.7
PSA (Ų)
0.84
QED
0
Ro5 Violations
2
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Adrenergic receptor alpha-2 antagonist | ANTAGONIST | Adrenergic receptor alpha-2 | ✓ | ✓ |
Indications
Parkinson Disease
Activity Summary
Ki 4 meas. best 8.17
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Alpha-2B adrenergic receptor CHEMBL1942 | Ki | 8.17 | 8.17 | 6.8 | 1 |
| Alpha-2A adrenergic receptor CHEMBL1867 | Ki | 8.14 | 8.14 | 7.2 | 1 |
| Alpha-2C adrenergic receptor CHEMBL1916 | Ki | 7.86 | 7.86 | 13.8 | 1 |
| Alpha-1B adrenergic receptor CHEMBL232 | Ki | 5.68 | 5.68 | 2089.3 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Alpha-2B adrenergic receptor | Ki | = | 6.761 | nM | 8.17 | Displacement of [3H]-RX821002 from human adrenergic alpha2B receptor expressed i... | 20809632 |
| Alpha-2A adrenergic receptor | Ki | = | 7.244 | nM | 8.14 | Displacement of [3H]-RX821002 from human adrenergic alpha2A receptor expressed i... | 20809632 |
| Alpha-2C adrenergic receptor | Ki | = | 13.8 | nM | 7.86 | Displacement of [3H]-RX821002 from human adrenergic Alpha-2C receptor expressed ... | 20809632 |
| Alpha-1B adrenergic receptor | Ki | = | 2089.3 | nM | 5.68 | Displacement of [3H]-prazosin from human adrenergic alpha-1b receptor expressed ... | 20809632 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 20809632 | 10.1021/jm1006269 | Mus musculus | 4 |
| 20809632 | 10.1021/jm1006269 | Alpha-2A adrenergic receptor | 2 |
| 20809632 | 10.1021/jm1006269 | Alpha-2C adrenergic receptor | 1 |
| 20809632 | 10.1021/jm1006269 | Alpha-2B adrenergic receptor | 1 |
| 20809632 | 10.1021/jm1006269 | Alpha-1B adrenergic receptor | 1 |
Data from ChEMBL 36 via Core Engine