Compound Detail
CHEMBL4303596
AMG-319 🧪 Phase II
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🧪 Phase II
Basic Information
| ChEMBL ID | CHEMBL4303596 |
| Name | AMG-319 |
| Phase | Phase II |
| Structure Type | MOL |
| InChI Key | KWRYMZHCQIOOEB-LBPRGKRZSA-N |
6
Targets
7
Activities
1
Assay Types
7
PK Parameters
15
Publications
3
Known Names
5
Indications
1
Mechanisms
Molecular Properties
385.4
MW (Da)
4.28
ALogP
6
HBA
2
HBD
92.3
PSA (Ų)
0.48
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 |
|---|---|---|---|---|
| PI3-kinase p110-delta subunit inhibitor | INHIBITOR | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform | ✓ | ✓ |
Indications
Carcinoma, Squamous Cell Leukemia, Lymphocytic, Chronic, B-Cell Lymphoma, Large B-Cell, Diffuse Lymphoma, Mantle-Cell Neoplasms
Activity Summary
IC50 7 meas. best 8.82
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform CHEMBL2216745 | IC50 | 8.82 | 8.82 | 1.5 | 1 |
| B cell CHEMBL5314312 | IC50 | 8.07 | 8.07 | 8.6 | 1 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform CHEMBL3130 | IC50 | 7.96 | 7.855 | 10.9 | 2 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform CHEMBL3267 | IC50 | 6.07 | 6.07 | 850.0 | 1 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform CHEMBL3145 | IC50 | 5.57 | 5.57 | 2700.0 | 1 |
| Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform CHEMBL4005 | IC50 | 4.48 | 4.48 | 33000.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 14.0 | mL.min-1.g-1 | Rattus norvegicus |
| CL | 14.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 5.0 | mL.min-1.kg-1 | Rattus norvegicus |
| CL | 45.0 | mL.min-1.kg-1 | Rattus norvegicus |
| F | 54.0 | % | Rattus norvegicus |
| Fu | 0.16 | - | Homo sapiens |
| Fu | 0.12 | - | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
| PubMed | DOI | Target Context | # Activities |
|---|---|---|---|
| 27411843 | 10.1021/acs.jmedchem.6b00827 | ADMET | 8 |
| 27411843 | 10.1021/acs.jmedchem.6b00827 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform | 4 |
| - | 10.6019/CHEMBL4495565 | SARS-CoV-2 | 4 |
| - | 10.6019/CHEMBL4808148 | Histone deacetylase 6 | 4 |
| 27411843 | 10.1021/acs.jmedchem.6b00827 | Unchecked | 3 |
| - | 10.21203/rs.3.rs-23951/v1 | SARS-CoV-2 | 2 |
| 27411843 | 10.1021/acs.jmedchem.6b00827 | Nuclear receptor subfamily 1 group I member 2 | 2 |
| - | 10.6019/CHEMBL4495564 | Replicase polyprotein 1ab | 2 |
| 27411843 | 10.1021/acs.jmedchem.6b00827 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform | 1 |
| 27411843 | 10.1021/acs.jmedchem.6b00827 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform | 1 |
| 27411843 | 10.1021/acs.jmedchem.6b00827 | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | 1 |
| 27411843 | 10.1021/acs.jmedchem.6b00827 | B cell | 1 |
| 27411843 | 10.1021/acs.jmedchem.6b00827 | Cytochrome P450 3A4 | 1 |
| 27411843 | 10.1021/acs.jmedchem.6b00827 | Cytochrome P450 2D6 | 1 |
| 27411843 | 10.1021/acs.jmedchem.6b00827 | No relevant target | 1 |
Data from ChEMBL 36 via Core Engine