Co-Target(s) Information
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T17687 | Target Info | |||
| Target Name | Fibroblast growth factor receptor (FGFR) | ||||
| Synonyms |
FGF receptor
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| Target Type | Successful Target | ||||
| Gene Name | NO-GeName | ||||
| UniProt ID | |||||
| Co-Targets of This Target | Top | |||||
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| Co-Target Name | Vascular endothelial growth factor receptor 2 (KDR) | Successful Target | ||||
| UniProt ID | VGFR2_HUMAN | |||||
| Gene Name | KDR | |||||
| Synonyms |
VEGFR2; VEGFR-2; VEGF-2 receptor; Protein-tyrosine kinase receptor flk-1; Kinase insert domain receptor; Fetal liver kinase 1; FLK1; FLK-1; CD309
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| Representative Drug(s) | Erdafitinib | Drug Info | IC50 = 36.8 nM | Click to Show More | [1] | |
| 2 | Drug Info | IC50 = 100 nM | [3] | |||
| 3 | Infigratinib | Drug Info | IC50 = 180 nM | [4] | ||
| 4 | PRN1371 | Drug Info | IC50 = 705 nM | [6] | ||
| Co-Target Name | Smoothened homolog (SMO) | Successful Target | ||||
| UniProt ID | SMO_HUMAN | |||||
| Gene Name | SMO | |||||
| Synonyms |
Smo-D473H; SMOH; Protein Gx
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| Representative Drug(s) | Infigratinib | Drug Info | Ki = 46.5 nM | [2] | ||
| Co-Target Name | Vascular endothelial growth factor receptor (VEGFR) | Successful Target | ||||
| UniProt ID | VGFR1_HUMAN; VGFR2_HUMAN; VGFR3_HUMAN | |||||
| Gene Name | NO-GeName | |||||
| Representative Drug(s) | Drug Info | IC50 = 190 nM | [5] | |||
| Co-Target Name | Janus kinase 3 (JAK-3) | Successful Target | ||||
| UniProt ID | JAK3_HUMAN | |||||
| Gene Name | JAK3 | |||||
| Synonyms |
Tyrosine-protein kinase JAK3; Leukocyte janus kinase; L-JAK
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| Representative Drug(s) | PRN1371 | Drug Info | IC50 = 556 nM | [6] | ||
| Co-Target Name | Tyrosine-protein kinase Kit (KIT) | Successful Target | ||||
| UniProt ID | KIT_HUMAN | |||||
| Gene Name | KIT | |||||
| Synonyms |
v-kit Hardy-Zuckerman 4 feline sarcoma viral oncogene homolog; p145 c-kit; Proto-oncogene tyrosine-protein kinase Kit; Proto-oncogene c-Kit; Piebald trait protein; PBT; Mast/stem cell growth factor receptor Kit; CD117 antigen; CD117; C-kit
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| Representative Drug(s) | Infigratinib | Drug Info | IC50 = 750 nM | [4] | ||
| Co-Target Name | Macrophage colony-stimulating factor 1 receptor (CSF1R) | Clinical trial Target | ||||
| UniProt ID | CSF1R_HUMAN | |||||
| Gene Name | CSF1R | |||||
| Synonyms |
Proto-oncogene c-Fms; M-CSF-R; FMS; CSF-1R; CSF-1-R; CSF-1 receptor; CD115
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| Representative Drug(s) | PRN1371 | Drug Info | IC50 = 8.1 nM | [6] | ||
| Co-Target Name | Tyrosine-protein kinase Lyn (JTK8) | Clinical trial Target | ||||
| UniProt ID | LYN_HUMAN | |||||
| Gene Name | LYN | |||||
| Synonyms |
p56Lyn; p53Lyn; V-yes-1 Yamaguchi sarcoma viral related oncogene homolog; Lck/Yes-related novel protein tyrosine kinase
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| Representative Drug(s) | Infigratinib | Drug Info | IC50 = 300 nM | Click to Show More | [4] | |
| 2 | PRN1371 | Drug Info | IC50 = 631 nM | [6] | ||
| Co-Target Name | Vascular endothelial growth factor receptor 3 (FLT-4) | Clinical trial Target | ||||
| UniProt ID | VGFR3_HUMAN | |||||
| Gene Name | FLT4 | |||||
| Synonyms |
VEGFR3; VEGFR-3; VEGF-3 receptor; Tyrosine-protein kinase receptor FLT4; Fms-like tyrosine kinase 4
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| Representative Drug(s) | PRN1371 | Drug Info | IC50 = 410 nM | [6] | ||
| Co-Target Name | Tyrosine-protein kinase BMX (BMX) | Patented-recorded Target | ||||
| UniProt ID | BMX_HUMAN | |||||
| Gene Name | BMX | |||||
| Synonyms |
NTK38; Epithelial and endothelial tyrosine kinase; ETK; Cytoplasmic tyrosine-protein kinase BMX; Bone marrow tyrosine kinase gene in chromosome X protein
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| Representative Drug(s) | PRN1371 | Drug Info | IC50 = 272 nM | [6] | ||
| Co-Target Name | B lymphocyte kinase (BLK) | Patented-recorded Target | ||||
| UniProt ID | BLK_HUMAN | |||||
| Gene Name | BLK | |||||
| Synonyms |
p55-Blk; Tyrosine-protein kinase Blk
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| Representative Drug(s) | PRN1371 | Drug Info | IC50 = 371 nM | [6] | ||
| Co-Target Name | PRKR-like endoplasmic reticulum kinase (PERK) | Clinical trial Target | ||||
| UniProt ID | E2AK3_HUMAN | |||||
| Gene Name | EIF2AK3 | |||||
| Synonyms |
PEK
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| Representative Drug(s) | PRN1371 | Drug Info | IC50 = 792 nM | [6] | ||
| References | Top | ||||
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| REF 1 | Fibroblast Growth Factor Receptor 4 (FGFR4) Selective Inhibitors as Hepatocellular Carcinoma Therapy: Advances and Prospects. J Med Chem. 2019 Mar 28;62(6):2905-2915. | ||||
| REF 2 | Dual MET and SMO Negative Modulators Overcome Resistance to EGFR Inhibitors in Human Nonsmall Cell Lung Cancer. J Med Chem. 2017 Sep 14;60(17):7447-58. | ||||
| REF 3 | Discovery of Substituted 1H-Pyrazolo[3,4-b]pyridine Derivatives as Potent and Selective FGFR Kinase Inhibitors. ACS Med Chem Lett. 2016 Apr 20;7(6):629-34. | ||||
| REF 4 | Discovery of 3-(2,6-dichloro-3,5-dimethoxy-phenyl)-1-{6-[4-(4-ethyl-piperazin-1-yl)-phenylamino]-pyrimidin-4-yl}-1-methyl-urea (NVP-BGJ398), a potent and selective inhibitor of the fibroblast growth factor receptor family of receptor tyrosine kinase. J Med Chem. 2011 Oct 27;54(20):7066-83. | ||||
| REF 5 | Synthesis and structure-activity relationships of soluble 7-substituted 3-(3,5-dimethoxyphenyl)-1,6-naphthyridin-2-amines and related ureas as dual inhibitors of the fibroblast growth factor receptor-1 and vascular endothelial growth factor receptor-2 tyrosine kinases. J Med Chem. 2005 Jul 14;48(14):4628-53. | ||||
| REF 6 | Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors. J Med Chem. 2017 Aug 10;60(15):6516-27. | ||||
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