Compound Detail
CHEMBL296522
RENZAPRIDE 🧪 Phase III
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🧪 Phase III
Basic Information
| ChEMBL ID | CHEMBL296522 |
| Name | RENZAPRIDE |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | GZSKEXSLDPEFPT-UHFFFAOYSA-N |
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
20
Publications
6
Known Names
1
Indications
2
Mechanisms
Molecular Properties
323.8
MW (Da)
2.14
ALogP
4
HBA
2
HBD
67.6
PSA (Ų)
0.84
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Racemic |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Serotonin 3 (5-HT3) receptor antagonist | ANTAGONIST | Serotonin 3 (5-HT3) receptor | ✓ | ✓ |
| Serotonin 4 (5-HT4) receptor agonist | AGONIST | 5-hydroxytryptamine receptor 4 | ✓ | ✓ |
Indications
Irritable Bowel Syndrome
Activity Summary
Ki 4 meas. best 8.3
EC50 2 meas. best 7.2
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Serotonin 3 (5-HT3) receptor CHEMBL2094116 | Ki | 8.3 | 8.29 | 5.0 | 2 |
| 5-hydroxytryptamine receptor 3A CHEMBL2411 | Ki | 8.25 | 8.25 | 5.6 | 1 |
| 5-hydroxytryptamine receptor 4 CHEMBL5017 | Ki | 7.39 | 7.39 | 40.4 | 1 |
| 5-hydroxytryptamine receptor 4 CHEMBL4317 | EC50 | 7.2 | 7.105 | 63.1 | 2 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| Serotonin 3 (5-HT3) receptor | Ki | = | 5.012 | nM | 8.3 | Tested for its binding affinity by measuring its ability to displace [3H]granise... | - |
| Serotonin 3 (5-HT3) receptor | Ki | = | 5.3 | nM | 8.28 | Inhibition of [3H]GR-65630 binding to rat cortical membrane serotonin 5-hydroxyt... | 12593651 |
| 5-hydroxytryptamine receptor 3A | Ki | = | 5.6 | nM | 8.25 | Compound was evaluated in vivo for the antagonistic activity towards 5-hydroxytr... | - |
| 5-hydroxytryptamine receptor 4 | Ki | = | 40.4 | nM | 7.39 | Inhibition of [3H]GR-113808 binding to guinea pig striatum 5-hydroxytryptamine 4... | 12593651 |
| 5-hydroxytryptamine receptor 4 | EC50 | = | 63.1 | nM | 7.2 | Tested for its agonist potency against the 5-hydroxytryptamine 4 receptor locate... | - |
| 5-hydroxytryptamine receptor 4 | EC50 | = | 98.0 | nM | 7.01 | Compound was evaluated for the agonistic activity towards 5-hydroxytryptamine 4 ... | - |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 8459397 | 10.1021/jm00058a004 | 5-hydroxytryptamine receptor 4 | 5 |
| 8459397 | 10.1021/jm00058a004 | Canis familiaris | 3 |
| 8459397 | 10.1021/jm00058a004 | Serotonin 3 (5-HT3) receptor | 3 |
| - | 10.6019/CHEMBL4651402 | SARS-CoV-2 | 2 |
| - | 10.1016/S0960-894X(01)81243-9 | 5-hydroxytryptamine receptor 4 | 2 |
| 12593651 | 10.1021/jm020270n | D(2) dopamine receptor | 1 |
| 1573641 | 10.1021/jm00086a019 | Adrenergic receptor alpha-2 | 1 |
| 1573641 | 10.1021/jm00086a019 | Alpha-1A adrenergic receptor | 1 |
| 1573641 | 10.1021/jm00086a019 | D(2) dopamine receptor | 1 |
| 1573641 | 10.1021/jm00086a019 | D(1A) dopamine receptor | 1 |
| 1573641 | 10.1021/jm00086a019 | Serotonin 2 (5-HT2) receptor | 1 |
| 1573641 | 10.1021/jm00086a019 | Serotonin 1 (5-HT1) receptor | 1 |
| 1573641 | 10.1021/jm00086a019 | Unchecked | 1 |
| 1573641 | 10.1021/jm00086a019 | Serotonin 3 (5-HT3) receptor | 1 |
| 1573641 | 10.1021/jm00086a019 | 5-hydroxytryptamine receptor 4 | 1 |
| - | 10.1016/S0960-894X(00)80441-2 | 5-hydroxytryptamine receptor 4 | 1 |
| 12593651 | 10.1021/jm020270n | 5-hydroxytryptamine receptor 4 | 1 |
| 12593651 | 10.1021/jm020270n | Serotonin 3 (5-HT3) receptor | 1 |
| - | 10.1016/S0960-894X(01)81243-9 | Serotonin 3 (5-HT3) receptor | 1 |
| - | 10.1016/S0960-894X(00)80441-2 | Rattus norvegicus | 1 |
Data from ChEMBL 36 via Core Engine