Compound Detail
CHEMBL3545154
POZIOTINIB 🧪 Phase III
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🧪 Phase III
Basic Information
| ChEMBL ID | CHEMBL3545154 |
| Name | POZIOTINIB |
| Phase | Phase III |
| Structure Type | MOL |
| InChI Key | LPFWVDIFUFFKJU-UHFFFAOYSA-N |
19
Targets
66
Activities
3
Assay Types
4
PK Parameters
20
Publications
8
Known Names
9
Indications
1
Mechanisms
Molecular Properties
491.4
MW (Da)
5.38
ALogP
6
HBA
1
HBD
76.6
PSA (Ų)
0.37
QED
1
Ro5 Violations
6
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Epidermal growth factor receptor inhibitor | INHIBITOR | Epidermal growth factor receptor | ✓ | ✓ |
Indications
Carcinoma, Non-Small-Cell Lung Adenocarcinoma of Lung Breast Neoplasms Esophageal Neoplasms Head and Neck Neoplasms Lung Neoplasms Neoplasms Neoplasms Stomach Neoplasms
Activity Summary
IC50 52 meas. best 10.21
Kd 11 meas. best 8.7
EC50 3 meas. best 8.15
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Epidermal growth factor receptor CHEMBL203 | IC50 | 10.21 | 8.9861 | 0.1 | 23 |
| Unchecked CHEMBL612545 | IC50 | 10.09 | 8.5669 | 0.1 | 16 |
| BaF3 CHEMBL614524 | IC50 | 9.68 | 9.3 | 0.2 | 5 |
| A-431 CHEMBL614069 | IC50 | 9.05 | 9.05 | 0.9 | 1 |
| SK-BR-3 CHEMBL613834 | IC50 | 9.0 | 9.0 | 1.0 | 1 |
| Receptor tyrosine-protein kinase erbB-2 CHEMBL1824 | IC50 | 8.88 | 8.36 | 1.3 | 3 |
| Epidermal growth factor receptor CHEMBL203 | Kd | 8.7 | 8.7 | 2.0 | 1 |
| NON-PROTEIN TARGET CHEMBL3879801 | IC50 | 8.57 | 8.57 | 2.7 | 1 |
| Tyrosine-protein kinase BTK CHEMBL5251 | Kd | 8.52 | 8.52 | 3.0 | 1 |
| NCI-H1975 CHEMBL614348 | IC50 | 8.24 | 8.24 | 5.7 | 1 |
| Unchecked CHEMBL612545 | EC50 | 8.15 | 8.15 | 7.0 | 1 |
| BaF3 CHEMBL614524 | EC50 | 7.92 | 7.92 | 12.0 | 1 |
| Receptor-interacting serine/threonine-protein kinase 2 CHEMBL5014 | Kd | 7.32 | 7.32 | 48.0 | 1 |
| Tyrosine-protein kinase Tec CHEMBL4246 | Kd | 7.16 | 7.16 | 69.0 | 1 |
| Ephrin type-B receptor 4 CHEMBL5147 | Kd | 6.47 | 6.47 | 340.0 | 1 |
| Receptor-interacting serine/threonine-protein kinase 3 CHEMBL1795199 | Kd | 6.41 | 6.41 | 392.0 | 1 |
| Hepatocyte growth factor receptor CHEMBL3717 | Kd | 6.1 | 6.1 | 794.0 | 1 |
| Voltage-gated inwardly rectifying potassium channel KCNH2 CHEMBL240 | IC50 | 6.04 | 6.04 | 915.0 | 1 |
| Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041 | Kd | 5.93 | 5.93 | 1185.0 | 1 |
| A-431 CHEMBL614069 | EC50 | 5.84 | 5.84 | 1445.0 | 1 |
| Non-receptor tyrosine-protein kinase TNK1 CHEMBL5334 | Kd | 5.77 | 5.77 | 1682.0 | 1 |
| Ephrin type-B receptor 2 CHEMBL3290 | Kd | 5.65 | 5.65 | 2236.0 | 1 |
| Ephrin type-A receptor 4 CHEMBL3988 | Kd | 5.15 | 5.15 | 7057.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 35.4 | mL.min-1.g-1 | Mus musculus |
| CL | 22.0 | mL.min-1.g-1 | Homo sapiens |
| CL | 44.0 | mL.min-1.g-1 | Homo sapiens |
| T1/2 | 15.63 | hr | - |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine