Compound Detail
CHEMBL3301622
GILTERITINIB 💊 Approved Drug
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💊 Approved Drug
CCc1nc(C(N)=O)c(Nc2ccc(N3CCC(N4CCN(C)CC4)CC3)c(OC)c2)nc1NC1CCOCC1
Basic Information
| ChEMBL ID | CHEMBL3301622 |
| Name | GILTERITINIB |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | GYQYAJJFPNQOOW-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
97
Targets
171
Activities
4
Assay Types
0
PK Parameters
20
Publications
3
Known Names
8
Indications
2
Mechanisms
Molecular Properties
552.7
MW (Da)
2.70
ALogP
10
HBA
3
HBD
121.1
PSA (Ų)
0.43
QED
1
Ro5 Violations
9
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2018 |
| Availability | Prescription |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Tyrosine-protein kinase receptor FLT3 inhibitor | INHIBITOR | Receptor-type tyrosine-protein kinase FLT3 | ✓ | ✓ |
| Tyrosine-protein kinase receptor UFO inhibitor | INHIBITOR | Tyrosine-protein kinase receptor UFO | ✓ | ✓ |
Indications
Neoplasms Leukemia, Myeloid Leukemia, Myeloid, Acute Myelodysplastic Syndromes Carcinoma, Non-Small-Cell Lung Kidney Diseases Leukemia Liver Diseases
ATC Classification
L01EX13
gilteritinib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS
Activity Summary
IC50 85 meas. best 9.8
Kd 82 meas. best 8.22
Ki 3 meas. best 8.7
EC50 1 meas. best 6.65
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974 | IC50 | 9.8 | 8.6988 | 0.2 | 25 |
| Leukocyte tyrosine kinase receptor CHEMBL5627 | IC50 | 9.46 | 9.46 | 0.3 | 1 |
| BaF3 CHEMBL614524 | IC50 | 9.32 | 8.94 | 0.5 | 10 |
| Tyrosine-protein kinase receptor UFO CHEMBL4895 | IC50 | 9.14 | 8.5033 | 0.7 | 18 |
| MOLM-13 CHEMBL3706572 | IC50 | 9.11 | 6.7175 | 0.8 | 4 |
| MV4-11 CHEMBL613835 | IC50 | 9.05 | 8.482 | 0.9 | 5 |
| ALK tyrosine kinase receptor CHEMBL4247 | IC50 | 8.92 | 8.8867 | 1.2 | 3 |
| Unchecked CHEMBL612545 | IC50 | 8.85 | 7.0633 | 1.4 | 3 |
| EML4-ALK CHEMBL3883330 | IC50 | 8.82 | 8.53 | 1.5 | 2 |
| MOLM-14 CHEMBL3706570 | IC50 | 8.74 | 8.085 | 1.8 | 4 |
| Proto-oncogene tyrosine-protein kinase ROS CHEMBL5568 | IC50 | 8.72 | 8.72 | 1.9 | 1 |
| Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974 | Ki | 8.7 | 8.35 | 2.0 | 2 |
| Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041 | IC50 | 8.47 | 8.47 | 3.4 | 1 |
| Serine/threonine-protein kinase ULK3 CHEMBL5047 | Kd | 8.22 | 8.22 | 6.0 | 1 |
| Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974 | Kd | 8.15 | 8.15 | 7.0 | 1 |
| Interleukin-1 receptor-associated kinase 3 CHEMBL5081 | Kd | 8.15 | 8.15 | 7.0 | 1 |
| TEL/AXL CHEMBL4523666 | IC50 | 8.07 | 8.07 | 8.5 | 1 |
| Cyclin-G-associated kinase CHEMBL4355 | Kd | 8.05 | 8.05 | 9.0 | 1 |
| Uncharacterized protein FLJ45252 CHEMBL4105933 | Kd | 7.96 | 7.96 | 11.0 | 1 |
| Serine/threonine-protein kinase PLK4 CHEMBL3788 | Kd | 7.75 | 7.75 | 18.0 | 1 |
| AP2-associated protein kinase 1 CHEMBL3830 | Kd | 7.6 | 7.6 | 25.0 | 1 |
| Non-receptor tyrosine-protein kinase TNK1 CHEMBL5334 | Kd | 7.41 | 7.41 | 39.0 | 1 |
| Activin receptor type-1 CHEMBL5903 | Kd | 7.41 | 7.41 | 39.0 | 1 |
| BMP-2-inducible protein kinase CHEMBL4522 | Kd | 7.34 | 7.34 | 46.0 | 1 |
| Phosphorylase b kinase gamma catalytic chain, liver/testis isoform CHEMBL2349 | Kd | 7.32 | 7.32 | 48.0 | 1 |
| Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041 | Kd | 7.3 | 7.3 | 50.0 | 1 |
| STE20-like serine/threonine-protein kinase CHEMBL4202 | Kd | 7.17 | 7.17 | 68.0 | 1 |
| Mitogen-activated protein kinase kinase kinase kinase 1 CHEMBL5749 | Kd | 6.97 | 6.97 | 108.0 | 1 |
| Bone morphogenetic protein receptor type-1A CHEMBL5275 | Kd | 6.92 | 6.92 | 121.0 | 1 |
| Serine/threonine-protein kinase 10 CHEMBL3981 | Kd | 6.83 | 6.83 | 149.0 | 1 |
| AarF domain-containing protein kinase 1 CHEMBL4105885 | Kd | 6.82 | 6.82 | 152.0 | 1 |
| Calcium/calmodulin-dependent protein kinase type II subunit gamma CHEMBL3829 | Kd | 6.77 | 6.77 | 169.0 | 1 |
| Aurora kinase A CHEMBL4722 | Kd | 6.74 | 6.74 | 184.0 | 1 |
| Myosin light chain kinase, smooth muscle CHEMBL2428 | Kd | 6.73 | 6.73 | 188.0 | 1 |
| Tyrosine-protein kinase Fer CHEMBL3982 | Kd | 6.73 | 6.73 | 188.0 | 1 |
| Mitotic checkpoint serine/threonine-protein kinase BUB1 CHEMBL1772932 | Kd | 6.72 | 6.72 | 191.0 | 1 |
| Cytochrome c1, heme protein, mitochondrial CHEMBL4105975 | Kd | 6.7 | 6.7 | 202.0 | 1 |
| Mitogen-activated protein kinase kinase kinase kinase 4 CHEMBL6166 | Kd | 6.7 | 6.7 | 202.0 | 1 |
| MM1.S CHEMBL4296471 | IC50 | 6.69 | 6.69 | 203.5 | 1 |
| Calcium/calmodulin-dependent protein kinase type II subunit delta CHEMBL2801 | Kd | 6.68 | 6.68 | 207.0 | 1 |
| Long-chain-fatty-acid--CoA ligase 5 CHEMBL4105818 | Kd | 6.68 | 6.68 | 208.0 | 1 |
| Serine/threonine-protein kinase LATS1 CHEMBL6167 | Kd | 6.66 | 6.66 | 221.0 | 1 |
| SARS-CoV-2 CHEMBL4303835 | EC50 | 6.65 | 6.65 | 225.0 | 1 |
| SARS-CoV-2 CHEMBL4303835 | IC50 | 6.65 | 5.97 | 225.0 | 3 |
| Serine/threonine-protein kinase 24 CHEMBL5082 | Kd | 6.64 | 6.64 | 230.0 | 1 |
| Ephrin type-B receptor 6 CHEMBL5836 | Kd | 6.62 | 6.62 | 241.0 | 1 |
| Serine/threonine-protein kinase Nek2 CHEMBL3835 | Kd | 6.61 | 6.61 | 247.0 | 1 |
| Mitogen-activated protein kinase kinase kinase kinase 2 CHEMBL5330 | Kd | 6.61 | 6.61 | 244.0 | 1 |
| Mitogen-activated protein kinase 15 CHEMBL5198 | Kd | 6.58 | 6.58 | 263.0 | 1 |
| Serine/threonine-protein kinase 16 CHEMBL3938 | Kd | 6.53 | 6.53 | 295.0 | 1 |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine