Compound Detail
CHEMBL220808
SARIZOTAN 🧪 Phase III
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🧪 Phase III
Basic Information
| ChEMBL ID | CHEMBL220808 |
| Name | SARIZOTAN |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | HKFMQJUJWSFOLY-OAQYLSRUSA-N |
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
8
Publications
2
Known Names
2
Indications
Molecular Properties
348.4
MW (Da)
4.37
ALogP
3
HBA
1
HBD
34.1
PSA (Ų)
0.74
QED
0
Ro5 Violations
5
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Indications
Movement Disorders Rett Syndrome
Activity Summary
Ki 3 meas. best 8.65
EC50 1 meas. best 7.11
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A CHEMBL273 | Ki | 8.65 | 8.65 | 2.2 | 1 |
| D(2) dopamine receptor CHEMBL339 | Ki | 7.72 | 7.72 | 19.1 | 1 |
| 5-hydroxytryptamine receptor 1A CHEMBL214 | EC50 | 7.11 | 7.11 | 77.6 | 1 |
| 5-hydroxytryptamine receptor 2A CHEMBL322 | Ki | 5.67 | 5.67 | 2138.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
| Target | Type | Rel. | Value | Units | pChEMBL | Assay | PubMed |
|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 1A | Ki | = | 2.239 | nM | 8.65 | Displacement of [3H]OH-DPAT from rat cortex 5HT1A receptor | 17300168 |
| D(2) dopamine receptor | Ki | = | 19.05 | nM | 7.72 | Displacement of [3H]YM-09151-2 from rat striatum D2 receptor | 17300168 |
| 5-hydroxytryptamine receptor 1A | EC50 | = | 77.62 | nM | 7.11 | Agonist activity at human 5HT1A receptor in HeLa cells assessed as stimulation o... | 17300168 |
| 5-hydroxytryptamine receptor 2A | Ki | = | 2137.96 | nM | 5.67 | Displacement of [3H]ketanserin from rat cortex 5HT2A receptor | 17300168 |
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 17300168 | 10.1021/jm061180b | 5-hydroxytryptamine receptor 1A | 3 |
| 17300168 | 10.1021/jm061180b | 5-hydroxytryptamine receptor 2A | 1 |
| 17300168 | 10.1021/jm061180b | D(2) dopamine receptor | 1 |
| 18181565 | 10.1021/jm7009364 | 5-hydroxytryptamine receptor 3A | 1 |
| 18181565 | 10.1021/jm7009364 | D(2) dopamine receptor | 1 |
| 18181565 | 10.1021/jm7009364 | D(3) dopamine receptor | 1 |
| 18181565 | 10.1021/jm7009364 | D(4) dopamine receptor | 1 |
| 18181565 | 10.1021/jm7009364 | 5-hydroxytryptamine receptor 1A | 1 |
Data from ChEMBL 36 via Core Engine