Compound Detail
CHEMBL3360203
PILARALISIB 🧪 Phase II
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🧪 Phase II
COc1ccc(Cl)c(Nc2nc3ccccc3nc2NS(=O)(=O)c2cccc(NC(=O)C(C)(C)N)c2)c1
Basic Information
| ChEMBL ID | CHEMBL3360203 |
| Name | PILARALISIB |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | QINPEPAQOBZPOF-UHFFFAOYSA-N |
7
Targets
18
Activities
1
Assay Types
0
PK Parameters
18
Publications
5
Known Names
9
Indications
1
Mechanisms
Molecular Properties
541.0
MW (Da)
4.51
ALogP
8
HBA
4
HBD
148.3
PSA (Ų)
0.25
QED
1
Ro5 Violations
8
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| PI3-kinase class I inhibitor | INHIBITOR | PI3-kinase class I | ✓ | ✓ |
Indications
Endometrial Neoplasms Endometrial Neoplasms Breast Neoplasms Breast Neoplasms Carcinoma, Non-Small-Cell Lung Glioblastoma Lymphoma Neoplasms Neoplasms
Activity Summary
IC50 18 meas. best 7.64
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform CHEMBL3130 | IC50 | 7.64 | 7.5733 | 23.0 | 3 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform CHEMBL3267 | IC50 | 7.64 | 7.285 | 23.0 | 4 |
| Unchecked CHEMBL612545 | IC50 | 7.64 | 7.64 | 23.0 | 3 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform CHEMBL3145 | IC50 | 7.44 | 6.76 | 36.0 | 3 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform CHEMBL4005 | IC50 | 7.41 | 7.41 | 39.0 | 3 |
| DNA-dependent protein kinase catalytic subunit CHEMBL3142 | IC50 | 5.32 | 5.32 | 4800.0 | 1 |
| Phosphatidylinositol 3-kinase catalytic subunit type 3 CHEMBL1075165 | IC50 | 5.16 | 5.16 | 7000.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 24983663 | 10.1021/jm5006034 | Unchecked | 3 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 2 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 2 |
| 31581005 | 10.1016/j.ejmech.2019.111718 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 1 |
| 20729870 | 10.1038/aps.2010.150 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | 1 |
| 20729870 | 10.1038/aps.2010.150 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform | 1 |
| 20729870 | 10.1038/aps.2010.150 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform | 1 |
| 20729870 | 10.1038/aps.2010.150 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 1 |
| 38157838 | 10.1016/j.bmc.2023.117561 | Unchecked | 1 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 1 |
| 31581005 | 10.1016/j.ejmech.2019.111718 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform | 1 |
| 31581005 | 10.1016/j.ejmech.2019.111718 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform | 1 |
| 31581005 | 10.1016/j.ejmech.2019.111718 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | 1 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 1 |
| 28835805 | 10.1021/acsmedchemlett.7b00222 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | 1 |
| 27644332 | 10.1021/acs.jmedchem.6b00963 | DNA-dependent protein kinase catalytic subunit | 1 |
| 27644332 | 10.1021/acs.jmedchem.6b00963 | Phosphatidylinositol 3-kinase catalytic subunit type 3 | 1 |
| 27644332 | 10.1021/acs.jmedchem.6b00963 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | 1 |
Data from ChEMBL 36 via Core Engine