Compound Detail
CHEMBL452461
PERZINFOTEL 🧪 Phase II
Enter ChEMBL ID:
Free Research Context
This compound will appear in recent viewed items on the research home for this browser.
Research home
View demo workspace
🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL452461 |
| Name | PERZINFOTEL |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | BDABGOLMYNHHTR-UHFFFAOYSA-N |
2
Targets
5
Activities
1
Assay Types
5
PK Parameters
17
Publications
2
Known Names
1
Mechanisms
Molecular Properties
260.2
MW (Da)
-0.92
ALogP
5
HBA
3
HBD
106.9
PSA (Ų)
0.48
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Glutamate [NMDA] receptor antagonist | ANTAGONIST | Glutamate [NMDA] receptor | ✓ | ✓ |
Activity Summary
IC50 5 meas. best 8.12
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Glutamate NMDA receptor CHEMBL1907608 | IC50 | 8.12 | 7.76 | 7.6 | 3 |
| Glutamate [NMDA] receptor CHEMBL2094124 | IC50 | 7.52 | 6.32 | 30.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 342.0 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 342.0 | ng.hr.mL-1 | Rattus norvegicus |
| Cmax | 837.85 | nM | Rattus norvegicus |
| T1/2 | 1.3 | hr | Rattus norvegicus |
| Tmax | 0.5 | hr | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Glutamate NMDA receptor | IC50 | = | 7.6 | nM | 8.12 | Tested in vitro for antagonistic activity at N-methyl-D-aspartate glutamate rece... | 9457246 |
| Glutamate NMDA receptor | IC50 | = | 23.0 | nM | 7.64 | Displacement of [3H]CGP-39653 from rat brain NMDA receptor | 19146418 |
| Glutamate NMDA receptor | IC50 | = | 30.0 | nM | 7.52 | Displacement of [3H]CPP from rat brain synaptic membrane N-methyl-D-aspartate gl... | 9457246 |
| Glutamate [NMDA] receptor | IC50 | = | 30.0 | nM | 7.52 | Binding affinity to NMDA receptor (unknown origin) | 33035923 |
| Glutamate [NMDA] receptor | IC50 | = | 7600.0 | nM | 5.12 | Binding affinity to TCP-stimulated NMDA (unknown origin) | 33035923 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 19146418 | 10.1021/jm8011799 | No relevant target | 12 |
| 19146418 | 10.1021/jm8011799 | Rattus norvegicus | 7 |
| 9457246 | 10.1021/jm970504g | Glutamate NMDA receptor | 2 |
| 33035923 | 10.1016/j.ejmech.2020.112872 | Glutamate [NMDA] receptor | 2 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 19146418 | 10.1021/jm8011799 | Unchecked | 2 |
| 19146418 | 10.1021/jm8011799 | Blood | 2 |
| 19146418 | 10.1021/jm8011799 | Plasma | 2 |
| 19146418 | 10.1021/jm8011799 | Brain | 2 |
| 33035923 | 10.1016/j.ejmech.2020.112872 | ADMET | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| 19146418 | 10.1021/jm8011799 | Glycine receptor subunit alpha-1 | 1 |
| 19146418 | 10.1021/jm8011799 | Glutamate NMDA receptor | 1 |
| 9457246 | 10.1021/jm970504g | Rattus norvegicus | 1 |
| 9457246 | 10.1021/jm970504g | Mus musculus | 1 |
Data from ChEMBL 36 via Core Engine