Compound Detail
CHEMBL1956285
DSM-265 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL1956285 |
| Name | DSM-265 |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | OIZSVTOIBNSVOS-UHFFFAOYSA-N |
7
Targets
56
Activities
2
Assay Types
30
PK Parameters
20
Publications
2
Known Names
3
Indications
1
Mechanisms
Molecular Properties
415.3
MW (Da)
5.95
ALogP
5
HBA
1
HBD
55.1
PSA (Ų)
0.54
QED
1
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Dihydroorotate dehydrogenase inhibitor | INHIBITOR | Dihydroorotate dehydrogenase | ✓ | ✓ |
Indications
Malaria, Falciparum Malaria, Vivax Malaria
Activity Summary
EC50 31 meas. best 8.37
IC50 25 meas. best 8.74
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Plasmodium falciparum CHEMBL364 | IC50 | 8.74 | 8.1667 | 1.8 | 6 |
| Plasmodium falciparum CHEMBL364 | EC50 | 8.37 | 7.54 | 4.3 | 26 |
| Unchecked CHEMBL612545 | IC50 | 8.05 | 6.8808 | 8.9 | 12 |
| Dihydroorotate dehydrogenase CHEMBL3486 | IC50 | 8.0 | 7.74 | 10.0 | 2 |
| Unchecked CHEMBL612545 | EC50 | 7.7 | 7.7 | 20.0 | 1 |
| Plasmodium vivax CHEMBL613013 | EC50 | 6.72 | 6.5 | 190.0 | 2 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | EC50 | 5.8 | 5.48 | 1600.0 | 2 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 5.8 | 5.8 | 1600.0 | 1 |
| Dihydroorotate dehydrogenase (quinone), mitochondrial CHEMBL2991 | IC50 | 5.68 | 5.66 | 2100.0 | 2 |
| Dihydroorotate dehydrogenase (quinone), mitochondrial CHEMBL2383 | IC50 | 5.58 | 5.47 | 2600.0 | 2 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| AUC | 186.9 | ng.hr.mL-1 | Mus musculus |
| AUC | 1128.48 | ng.hr.mL-1 | Mus musculus |
| AUC | 9394.99 | ng.hr.mL-1 | Mus musculus |
| AUC | 14038.49 | ng.hr.mL-1 | Mus musculus |
| AUC | 6429.46 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 50476.27 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 133635.64 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 24014.96 | ng.hr.mL-1 | Mus musculus |
| AUC | 23724.22 | ng.hr.mL-1 | Mus musculus |
| AUC | 16700.0 | ng.hr.mL-1 | Canis lupus familiaris |
| AUC | 16700.0 | ng.hr.mL-1 | Macaca mulatta |
| AUC | 107000.0 | ng.hr.mL-1 | Homo sapiens |
| AUC | 12335.6 | ng.hr.mL-1 | Mus musculus |
| AUC | 6479.3 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 50671.48 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 50671.48 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 7226.92 | ng.hr.mL-1 | Rattus norvegicus |
| AUC | 9386.68 | ng.hr.mL-1 | Mus musculus |
| CL | 8.1 | mL.min-1.g-1 | Mus musculus |
| CL | 5.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 3.6 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 6.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 0.3667 | mL.min-1.kg-1 | Canis lupus familiaris |
| CL | 0.3667 | mL.min-1.kg-1 | Macaca mulatta |
| CL | 6500.0 | mL.min-1.g-1 | Rattus norvegicus |
| CL | 6.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 263.0 | mL.min-1.kg-1 | Rattus norvegicus |
| Cmax | 60.0 | nM | Mus musculus |
| Cmax | 440.0 | nM | Mus musculus |
| Cmax | 3100.0 | nM | Mus musculus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine