Compound Detail
CHEMBL119625
ZONAMPANEL 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL119625 |
| Name | ZONAMPANEL |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | SPXYHZRWPRQLNS-UHFFFAOYSA-N |
4
Targets
7
Activities
2
Assay Types
3
PK Parameters
14
Publications
9
Known Names
2
Indications
1
Mechanisms
Molecular Properties
331.2
MW (Da)
-0.13
ALogP
8
HBA
2
HBD
153.1
PSA (Ų)
0.38
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Glutamate receptor ionotropic AMPA antagonist | ANTAGONIST | Glutamate receptor ionotropic AMPA | ✓ | ✓ |
Indications
Ischemic Stroke Stroke
Activity Summary
IC50 4 meas. best 5.52
Ki 3 meas. best 7.21
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Glutamate receptor ionotropic, AMPA CHEMBL2093871 | Ki | 7.21 | 7.21 | 62.0 | 2 |
| Unchecked CHEMBL612545 | Ki | 7.02 | 7.02 | 96.0 | 1 |
| Solute carrier family 22 member 6 CHEMBL1641347 | IC50 | 5.52 | 5.52 | 3000.0 | 1 |
| Unchecked CHEMBL612545 | IC50 | 5.34 | 5.34 | 4600.0 | 1 |
| Organic anion transporter 3 CHEMBL1641348 | IC50 | 5.18 | 5.18 | 6600.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 5.3 | mL.min-1.kg-1 | Homo sapiens |
| MRT | 0.6 | hr | Homo sapiens |
| T1/2 | 0.78 | hr | Homo sapiens |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Glutamate receptor ionotropic, AMPA | Ki | = | 62.0 | nM | 7.21 | Binding affinity for ionotropic glutamate receptor AMPA using [3H]AMPA as radiol... | 14505662 |
| Glutamate receptor ionotropic, AMPA | Ki | = | 62.0 | nM | 7.21 | Displacement of [3H]AMPA (5 nM) from ionotropic glutamate receptor AMPA of rat c... | 15380209 |
| Unchecked | Ki | = | 96.0 | nM | 7.02 | Displacement of [3H]AMPA from AMPA receptor in rat cortical membrane | 20356304 |
| Solute carrier family 22 member 6 | IC50 | = | 3000.0 | nM | 5.52 | Inhibition of human OAT1 | 20356304 |
| Unchecked | IC50 | = | 4600.0 | nM | 5.34 | Displacement of [3H]kainate from kainate receptor in rat cortical membrane | 20356304 |
| Organic anion transporter 3 | IC50 | = | 6600.0 | nM | 5.18 | Inhibition of human OAT3 | 20356304 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 18426954 | 10.1124/dmd.108.020479 | ADMET | 4 |
| 20356304 | 10.1021/jm901688m | Rattus norvegicus | 3 |
| 14505662 | 10.1016/s0960-894x(03)00740-6 | Rattus norvegicus | 2 |
| 20356304 | 10.1021/jm901688m | Unchecked | 2 |
| 20356304 | 10.1021/jm901688m | Glutamate NMDA receptor | 2 |
| 14505662 | 10.1016/s0960-894x(03)00740-6 | Glutamate receptor ionotropic, AMPA | 1 |
| 14505662 | 10.1016/s0960-894x(03)00740-6 | Glutamate receptors; NMDA/AMPA | 1 |
| 15380209 | 10.1016/j.bmcl.2004.07.093 | Glutamate receptor ionotropic, AMPA | 1 |
| 15380209 | 10.1016/j.bmcl.2004.07.093 | Glutamate receptors; NMDA/AMPA | 1 |
| 15380209 | 10.1016/j.bmcl.2004.07.093 | Rattus norvegicus | 1 |
| 15380209 | 10.1016/j.bmcl.2004.07.093 | No relevant target | 1 |
| 20356304 | 10.1021/jm901688m | Solute carrier family 22 member 6 | 1 |
| 20356304 | 10.1021/jm901688m | Organic anion transporter 3 | 1 |
| 20356304 | 10.1021/jm901688m | Solute carrier family 22 member 11 | 1 |
Data from ChEMBL 36 via Core Engine