Compound Detail
CHEMBL3120215
OSI-027 🧪 Phase II
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🧪 Phase II
COc1cccc2cc(-c3nc([C@H]4CC[C@H](C(=O)O)CC4)n4ncnc(N)c34)[nH]c12
Basic Information
| ChEMBL ID | CHEMBL3120215 |
| Name | OSI-027 |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | JROFGZPOBKIAEW-HAQNSBGRSA-N |
28
Targets
32
Activities
2
Assay Types
0
PK Parameters
20
Publications
10
Known Names
2
Indications
1
Mechanisms
Molecular Properties
406.4
MW (Da)
3.22
ALogP
7
HBA
3
HBD
131.4
PSA (Ų)
0.47
QED
0
Ro5 Violations
4
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Single Enantiomer |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Serine/threonine-protein kinase mTOR inhibitor | INHIBITOR | Serine/threonine-protein kinase mTOR | ✓ | ✓ |
Indications
Lymphedema Lymphoma
Activity Summary
IC50 19 meas. best 8.4
Kd 13 meas. best 7.24
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Serine/threonine-protein kinase mTOR CHEMBL2842 | IC50 | 8.4 | 7.6 | 4.0 | 3 |
| mTORC1 CHEMBL4296661 | IC50 | 7.66 | 7.66 | 22.0 | 1 |
| Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041 | Kd | 7.24 | 7.24 | 57.0 | 1 |
| mTORC2 CHEMBL4523999 | IC50 | 7.19 | 7.19 | 65.0 | 1 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform CHEMBL3267 | IC50 | 6.38 | 6.38 | 420.0 | 1 |
| Activin receptor type-1B CHEMBL5310 | Kd | 6.26 | 6.26 | 549.0 | 1 |
| TGF-beta receptor type-1 CHEMBL4439 | Kd | 6.11 | 6.11 | 780.0 | 1 |
| DNA-dependent protein kinase catalytic subunit CHEMBL3142 | IC50 | 6.0 | 5.26 | 1000.0 | 2 |
| Receptor-interacting serine/threonine-protein kinase 2 CHEMBL5014 | Kd | 5.93 | 5.93 | 1163.0 | 1 |
| SQ20B CHEMBL614939 | IC50 | 5.89 | 5.89 | 1300.0 | 1 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform CHEMBL4005 | IC50 | 5.89 | 5.89 | 1300.0 | 1 |
| Ribosyldihydronicotinamide dehydrogenase [quinone] CHEMBL3959 | Kd | 5.86 | 5.86 | 1390.0 | 1 |
| Unchecked CHEMBL612545 | Kd | 5.83 | 5.83 | 1478.0 | 1 |
| Casein kinase II subunit alpha' CHEMBL4070 | Kd | 5.79 | 5.79 | 1604.0 | 1 |
| Mitogen-activated protein kinase 10 CHEMBL2637 | Kd | 5.79 | 5.79 | 1617.0 | 1 |
| CAKI-1 CHEMBL614067 | IC50 | 5.72 | 5.72 | 1900.0 | 1 |
| Bone morphogenetic protein receptor type-2 CHEMBL5467 | Kd | 5.68 | 5.68 | 2097.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 5.5 | 5.37 | 3200.0 | 2 |
| Serine/threonine-protein kinase NLK CHEMBL5364 | Kd | 5.48 | 5.48 | 3331.0 | 1 |
| DU-145 CHEMBL613508 | IC50 | 5.39 | 5.39 | 4100.0 | 1 |
| Dual specificity mitogen-activated protein kinase kinase 5 CHEMBL4948 | Kd | 5.31 | 5.31 | 4914.0 | 1 |
| Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma CHEMBL1770034 | Kd | 5.3 | 5.3 | 4974.0 | 1 |
| HCT-116 CHEMBL394 | IC50 | 5.25 | 5.25 | 5600.0 | 1 |
| COLO 205 CHEMBL614561 | IC50 | 5.24 | 5.24 | 5800.0 | 1 |
| OVCAR-3 CHEMBL614213 | IC50 | 5.09 | 5.09 | 8100.0 | 1 |
| Ferrochelatase, mitochondrial CHEMBL3879831 | Kd | 4.9 | 4.9 | 12611.0 | 1 |
| HOP-62 CHEMBL614643 | IC50 | 4.39 | 4.39 | 41000.0 | 1 |
| HT-29 CHEMBL384 | IC50 | 4.26 | 4.26 | 55000.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine