Compound Detail
CHEMBL1852688
INFIGRATINIB 💊 Approved Drug
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💊 Approved Drug
CCN1CCN(c2ccc(Nc3cc(N(C)C(=O)Nc4c(Cl)c(OC)cc(OC)c4Cl)ncn3)cc2)CC1
Basic Information
| ChEMBL ID | CHEMBL1852688 |
| Name | INFIGRATINIB |
| Phase | Approved |
| Structure Type | MOL |
| InChI Key | QADPYRIHXKWUSV-UHFFFAOYSA-N |
| Therapeutic | ✓ Yes |
42
Targets
129
Activities
2
Assay Types
2
PK Parameters
20
Publications
5
Known Names
15
Indications
1
Mechanisms
Molecular Properties
560.5
MW (Da)
5.35
ALogP
8
HBA
2
HBD
95.1
PSA (Ų)
0.38
QED
2
Ro5 Violations
8
Rot. Bonds
Drug Information
| Molecule Type | Small molecule |
| First Approval | 2021 |
| Availability | Discontinued |
| Chirality | Achiral |
Mechanism of Action
| Mechanism | Action Type | Target | Direct | Efficacy |
|---|---|---|---|---|
| Fibroblast growth factor receptor inhibitor | INHIBITOR | Fibroblast growth factor receptor | ✓ | ✓ |
Indications
Neoplasms Neoplasms Cholangiocarcinoma Urinary Bladder Neoplasms Achondroplasia Carcinoma, Squamous Cell Glioblastoma Melanoma Osteomalacia Papillomavirus Infections Paraganglioma Squamous Cell Carcinoma of Head and Neck Breast Neoplasms Gastrointestinal Stromal Tumors Uterine Cervical Neoplasms
ATC Classification
L01EN03
infigratinib
Level 1: ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS
Level 2: ANTINEOPLASTIC AGENTS
Activity Summary
IC50 128 meas. best 9.23
Ki 1 meas. best 7.33
Target Activity Profile
| Target | Type | Best pChEMBL | Mean pChEMBL | Best (nM) | # Data |
|---|---|---|---|---|---|
| Fibroblast growth factor receptor 1 CHEMBL3650 | IC50 | 9.23 | 8.2695 | 0.6 | 21 |
| Fibroblast growth factor receptor 3 CHEMBL2742 | IC50 | 9.18 | 7.8678 | 0.7 | 23 |
| Fibroblast growth factor receptor 2 CHEMBL4142 | IC50 | 9.17 | 8.144 | 0.7 | 15 |
| Fibroblast growth factor receptor 4 CHEMBL3973 | IC50 | 9.09 | 7.4329 | 0.8 | 14 |
| RT-112 CHEMBL614145 | IC50 | 8.21 | 7.086 | 6.2 | 5 |
| CC-LP-1 CHEMBL6066762 | IC50 | 8.14 | 7.35 | 7.3 | 3 |
| Unchecked CHEMBL612545 | IC50 | 8.12 | 7.125 | 7.6 | 4 |
| SNU-16 CHEMBL613529 | IC50 | 7.91 | 7.465 | 12.4 | 2 |
| Protein smoothened CHEMBL5971 | Ki | 7.33 | 7.33 | 46.5 | 1 |
| Huh-7 CHEMBL614039 | IC50 | 7.24 | 7.17 | 57.2 | 2 |
| KATO III stomach cancer cell line CHEMBL612700 | IC50 | 7.22 | 7.22 | 60.3 | 1 |
| NCI-H716 CHEMBL2366106 | IC50 | 7.18 | 7.18 | 65.9 | 1 |
| Hep 3B2 CHEMBL4296437 | IC50 | 7.07 | 7.07 | 85.0 | 1 |
| BaF3 CHEMBL614524 | IC50 | 6.88 | 6.18 | 132.6 | 2 |
| Vascular endothelial growth factor receptor 2 CHEMBL279 | IC50 | 6.75 | 6.2067 | 180.0 | 3 |
| Tyrosine-protein kinase Lyn CHEMBL3905 | IC50 | 6.52 | 6.02 | 300.0 | 2 |
| Fibroblast growth factor receptor 4 CHEMBL3839 | IC50 | 6.27 | 6.255 | 541.0 | 2 |
| Mast/stem cell growth factor receptor Kit CHEMBL1936 | IC50 | 6.12 | 5.86 | 750.0 | 2 |
| Tyrosine-protein kinase Yes CHEMBL2073 | IC50 | 5.96 | 5.96 | 1100.0 | 1 |
| Vascular endothelial growth factor receptor 1 CHEMBL1868 | IC50 | 5.82 | 5.82 | 1510.0 | 1 |
| Tyrosine-protein kinase Fyn CHEMBL1841 | IC50 | 5.72 | 5.72 | 1900.0 | 1 |
| Angiopoietin-1 receptor CHEMBL4128 | IC50 | 5.69 | 5.69 | 2051.0 | 1 |
| Vascular endothelial growth factor receptor 3 CHEMBL1955 | IC50 | 5.68 | 5.68 | 2072.0 | 1 |
| Bcr/Abl fusion protein CHEMBL2096618 | IC50 | 5.66 | 5.66 | 2192.0 | 1 |
| Tyrosine-protein kinase ABL1 CHEMBL1862 | IC50 | 5.64 | 5.64 | 2300.0 | 1 |
| Tyrosine-protein kinase Lck CHEMBL258 | IC50 | 5.61 | 5.605 | 2482.0 | 2 |
| Platelet-derived growth factor receptor alpha CHEMBL2007 | IC50 | 5.57 | 5.57 | 2718.0 | 1 |
| Tyrosine-protein kinase JAK2 CHEMBL2971 | IC50 | 5.54 | 5.54 | 2882.0 | 1 |
| Macrophage-stimulating protein receptor CHEMBL2689 | IC50 | 5.54 | 5.54 | 2891.0 | 1 |
| Proto-oncogene tyrosine-protein kinase Src CHEMBL267 | IC50 | 5.53 | 5.53 | 2969.0 | 1 |
| Hepatocyte growth factor receptor CHEMBL3717 | IC50 | 5.52 | 5.52 | 3011.0 | 1 |
| Ephrin type-B receptor 1 CHEMBL5072 | IC50 | 5.52 | 5.52 | 3039.0 | 1 |
| ALK tyrosine kinase receptor CHEMBL4247 | IC50 | 5.51 | 5.51 | 3078.0 | 1 |
| BDNF/NT-3 growth factors receptor CHEMBL4898 | IC50 | 5.5 | 5.5 | 3139.0 | 1 |
| Receptor-type tyrosine-protein kinase FLT3 CHEMBL1974 | IC50 | 5.49 | 5.49 | 3252.0 | 1 |
| Proto-oncogene tyrosine-protein kinase ROS CHEMBL5568 | IC50 | 5.49 | 5.49 | 3263.0 | 1 |
| Non-receptor tyrosine-protein kinase TYK2 CHEMBL3553 | IC50 | 5.48 | 5.48 | 3303.0 | 1 |
| Proto-oncogene tyrosine-protein kinase receptor Ret CHEMBL2041 | IC50 | 5.47 | 5.47 | 3352.0 | 1 |
| Insulin receptor CHEMBL1981 | IC50 | 5.47 | 5.47 | 3371.0 | 1 |
| Cytoplasmic tyrosine-protein kinase BMX CHEMBL3834 | IC50 | 5.47 | 5.47 | 3405.0 | 1 |
| Serine/threonine-protein kinase B-raf CHEMBL5145 | IC50 | 5.38 | 5.38 | 4142.0 | 1 |
| Tyrosine-protein kinase SYK CHEMBL2599 | IC50 | 5.27 | 5.27 | 5358.0 | 1 |
Pharmacokinetic Data
| Parameter | Value | Units | Species |
|---|---|---|---|
| CL | 28.84 | uL.min-1.(10^6cells)-1 | Homo sapiens |
| CL | 87.1 | uL.min-1.(10^6cells)-1 | Rattus norvegicus |
Activity Data Samples
Top measurements by pChEMBL value
Literature References
Data from ChEMBL 36 via Core Engine