Compound Detail
CHEMBL2364611
GALUNISERTIB 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL2364611 |
| Name | GALUNISERTIB |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | IVRXNBXKWIJUQB-UHFFFAOYSA-N |
16
Targets
40
Activities
2
Assay Types
0
PK Parameters
20
Publications
3
Known Names
12
Indications
1
Mechanisms
Molecular Properties
369.4
MW (Da)
3.51
ALogP
5
HBA
1
HBD
86.7
PSA (Ų)
0.60
QED
0
Ro5 Violations
3
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| TGF-beta receptor type I inhibitor | INHIBITOR | TGF-beta receptor type-1 | ✓ | ✓ |
Indications
Carcinoma, Hepatocellular Glioblastoma Myelodysplastic Syndromes Nasopharyngeal Carcinoma Prostatic Neoplasms, Castration-Resistant Rectal Neoplasms Neoplasm Metastasis Neoplasms Pancreatic Neoplasms Pancreatic Neoplasms Paraganglioma Triple Negative Breast Neoplasms
Activity Summary
IC50 28 meas. best 8.39
Kd 12 meas. best 7.96
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| TGF-beta receptor type-1 CHEMBL4439 | IC50 | 8.39 | 7.1327 | 4.1 | 15 |
| Receptor-interacting serine/threonine-protein kinase 3 CHEMBL1795199 | Kd | 7.96 | 7.96 | 11.0 | 1 |
| Activin receptor type-1B CHEMBL5310 | Kd | 7.8 | 7.8 | 16.0 | 1 |
| Misshapen-like kinase 1 CHEMBL5518 | Kd | 7.75 | 7.75 | 18.0 | 1 |
| Receptor-interacting serine/threonine-protein kinase 2 CHEMBL5014 | Kd | 7.42 | 7.42 | 38.0 | 1 |
| Receptor-interacting serine/threonine-protein kinase 2 CHEMBL5014 | IC50 | 7.36 | 7.36 | 44.0 | 1 |
| Transforming growth factor beta-2 proprotein CHEMBL3217393 | IC50 | 7.25 | 7.25 | 56.0 | 1 |
| TGF-beta receptor type-1 CHEMBL4439 | Kd | 7.1 | 7.1 | 79.0 | 1 |
| Activin receptor type-1B CHEMBL5310 | IC50 | 6.7 | 6.7 | 199.0 | 1 |
| Mitogen-activated protein kinase kinase kinase kinase 4 CHEMBL6166 | IC50 | 6.58 | 6.565 | 263.1 | 2 |
| Mitogen-activated protein kinase 14 CHEMBL260 | IC50 | 6.39 | 6.3233 | 405.0 | 6 |
| Vascular endothelial growth factor receptor 2 CHEMBL279 | IC50 | 6.36 | 6.36 | 442.0 | 1 |
| Cyclin-G-associated kinase CHEMBL4355 | Kd | 6.3 | 6.3 | 495.0 | 1 |
| TRAF2 and NCK-interacting protein kinase CHEMBL4527 | Kd | 5.92 | 5.92 | 1208.0 | 1 |
| TGF-beta receptor type-2 CHEMBL4267 | IC50 | 5.89 | 5.89 | 1300.0 | 1 |
| Mitogen-activated protein kinase kinase kinase kinase 4 CHEMBL6166 | Kd | 5.77 | 5.77 | 1693.0 | 1 |
| Casein kinase I isoform epsilon CHEMBL4937 | Kd | 5.1 | 5.1 | 7903.0 | 1 |
| Atypical kinase COQ8A, mitochondrial CHEMBL5550 | Kd | 4.91 | 4.91 | 12248.0 | 1 |
| Casein kinase I isoform delta CHEMBL2828 | Kd | 4.79 | 4.79 | 16150.0 | 1 |
| Casein kinase I isoform alpha CHEMBL2793 | Kd | 4.71 | 4.71 | 19352.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine