Compound Detail
CHEMBL46286
OMACETAXINE MEPESUCCINATE 💊 Approved Drug
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💊 Approved Drug
COC(=O)C[C@](O)(CCCC(C)(C)O)C(=O)O[C@@H]1C(OC)=C[C@]23CCCN2CCc2cc4c(cc2[C@H]13)OCO4
Basic Information
| ChEMBL ID | CHEMBL46286 |
| Name | OMACETAXINE MEPESUCCINATE |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | HYFHYPWGAURHIV-JFIAXGOJSA-N |
| Therapeutic | ✓ Yes |
25
Targets
36
Activities
3
Assay Types
0
PK Parameters
20
Publications
11
Known Names
6
Indications
1
Mechanisms
Molecular Properties
545.6
MW (Da)
2.58
ALogP
10
HBA
2
HBD
124.0
PSA (Ų)
0.45
QED
1
Ro5 Violations
9
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2009 |
| Availability | Discontinued |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Protein synthesis inhibitor | - | - | ✓ | ✓ |
Indications
Neoplasms Neoplasms Leukemia Leukemia, Myeloid, Acute Leukemia, Myelogenous, Chronic, BCR-ABL Positive Myelodysplastic Syndromes
ATC Classification
L01XX40
omacetaxine mepesuccinate
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS
Activity Summary
IC50 32 meas. best 9.06
EC50 3 meas. best 8.31
Kd 1 meas. best 4.77
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| MCF7 CHEMBL387 | IC50 | 9.06 | 9.06 | 0.9 | 1 |
| A204 CHEMBL614514 | IC50 | 8.4 | 8.4 | 4.0 | 1 |
| KB CHEMBL398 | IC50 | 8.4 | 8.4 | 4.0 | 1 |
| BJ CHEMBL614358 | EC50 | 8.31 | 8.31 | 4.9 | 1 |
| MV4-11 CHEMBL613835 | IC50 | 8.3 | 8.3 | 5.0 | 1 |
| OCI-Ly3 CHEMBL4523565 | IC50 | 8.3 | 8.3 | 5.0 | 1 |
| MOLT-4 CHEMBL614177 | IC50 | 8.15 | 8.15 | 7.0 | 1 |
| U-937 CHEMBL612794 | IC50 | 7.92 | 7.92 | 12.0 | 1 |
| HL-60 CHEMBL383 | IC50 | 7.89 | 7.7367 | 13.0 | 3 |
| HCT-116 CHEMBL394 | IC50 | 7.89 | 7.89 | 13.0 | 1 |
| K562 CHEMBL385 | IC50 | 7.85 | 7.765 | 14.0 | 2 |
| Unchecked CHEMBL612545 | IC50 | 7.74 | 7.74 | 18.3 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 7.7 | 6.995 | 20.0 | 2 |
| MDA-MB-453 CHEMBL614334 | IC50 | 7.68 | 7.68 | 21.0 | 1 |
| NCI-H1299 CHEMBL612255 | IC50 | 7.66 | 7.66 | 22.0 | 1 |
| NCI-H1975 CHEMBL614348 | IC50 | 7.66 | 7.66 | 22.0 | 1 |
| A549 CHEMBL392 | IC50 | 7.52 | 7.51 | 30.0 | 2 |
| HepG2 CHEMBL395 | IC50 | 7.46 | 7.46 | 34.5 | 1 |
| Huh-7 CHEMBL614039 | IC50 | 7.4 | 7.4 | 40.0 | 1 |
| SARS-CoV-2 CHEMBL4303835 | EC50 | 7.22 | 6.45 | 60.0 | 2 |
| 4T1 CHEMBL612589 | IC50 | 7.22 | 7.22 | 60.0 | 1 |
| L02 CHEMBL4296457 | IC50 | 7.19 | 7.19 | 64.0 | 1 |
| NCI-H716 CHEMBL2366106 | IC50 | 7.19 | 7.19 | 65.0 | 1 |
| BaF3 CHEMBL614524 | IC50 | 7.09 | 7.09 | 81.0 | 1 |
| HeLa CHEMBL399 | IC50 | 6.4 | 6.085 | 400.0 | 2 |
| SARS-CoV-2 CHEMBL4303835 | IC50 | 5.33 | 5.33 | 4710.0 | 1 |
| Unchecked CHEMBL612545 | Kd | 4.77 | 4.77 | 16970.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine