Target Binding Site Detail
| Target General Information | Top | ||||
|---|---|---|---|---|---|
| Target ID | T74312 | Target Info | |||
| Target Name | Fms-like tyrosine kinase 3 (FLT-3) | ||||
| Synonyms | Stem cell tyrosine kinase 1; STK1; STK-1; Receptor-type tyrosine-protein kinase FLT3; Fetal liver kinase-2; FLT-3; FLK2; FLK-2; FL cytokine receptor; CD135 | ||||
| Target Type | Successful Target | ||||
| Gene Name | FLT3 | ||||
| Biochemical Class | Kinase | ||||
| UniProt ID | |||||
| Ligand General Information | Top | ||||
|---|---|---|---|---|---|
| Ligand Name | 3-Cyclohexyl-1-propylsulfonic acid | Ligand Info | |||
| Canonical SMILES | C1CCC(CC1)NCCCS(=O)(=O)O | ||||
| InChI | 1S/C9H19NO3S/c11-14(12,13)8-4-7-10-9-5-2-1-3-6-9/h9-10H,1-8H2,(H,11,12,13) | ||||
| InChIKey | PJWWRFATQTVXHA-UHFFFAOYSA-N | ||||
| PubChem Compound ID | 70815 | ||||
| Drug Binding Sites of Target | Top | |||||
|---|---|---|---|---|---|---|
| PDB ID: 6IL3 Crystal structure of the FLT3 kinase bound to a small molecule inhibitor | ||||||
| Method | X-ray diffraction | Resolution | 2.50 Å | Mutation | No | [1] |
| PDB Sequence |
QFRYESQLQM
578 VQVTGSSDNE588 YFYVDFREYE598 YDLKWEFPRE608 NLEFGKVLGS618 GAFGKVMNAT 628 AYGISKTGVS638 IQVAVKMLKE648 KADSSEREAL658 MSELKMMTQL668 GSHENIVNLL 678 GACTLSGPIY688 LIFEYCCYGD698 LLNYLRSKRE708 KFSNVLTFED787 LLCFAYQVAK 797 GMEFLEFKSC807 VHRDLAARNV817 LVTHGKVVKI827 CDFGLARDIM837 SDSNYVVRGN 847 ARLPVKWMAP857 ESLFEGIYTI867 KSDVWSYGIL877 LWEIFSLGVN887 PYPGIPVDAN 897 FYKLIQNGFK907 MDQPFYATEE917 IYIIMQSCWA927 FDSRKRPSFP937 NLTSFLGCQL 947
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| PDB ID: 6JQR Crystal structure of FLT3 in complex with gilteritinib | ||||||
| Method | X-ray diffraction | Resolution | 2.20 Å | Mutation | No | [2] |
| PDB Sequence |
RYESQLQMVQ
580 VTGSSDNEYF590 YVDFREYEYD600 LKWEFPRENL610 EFGKVLGSGA620 FGKVMNATAY 630 GISVSIQVAV643 KMLKEDSSER655 EALMSELKMM665 TQLGSHENIV675 NLLGACTLSG 685 PIYLIFEYCC695 YGDLLNYLRS705 KREKFSNVLT784 FEDLLCFAYQ794 VAKGMEFLEF 804 KSCVHRDLAA814 RNVLVTHGKV824 VKICDFMSDS840 NYVVRGNARL850 PVKWMAPESL 860 FEGIYTIKSD870 VWSYGILLWE880 IFSLGVNPYP890 GIPVDANFYK900 LIQNGFKMDQ 910 PFYATEEIYI920 IMQSCWAFDS930 RKRPSFPNLT940 SFLGCQLADA950 E |
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| References | Top | ||||
|---|---|---|---|---|---|
| REF 1 | Crystal structure of the FLT3 kinase bound to a small molecule inhibitor | ||||
| REF 2 | Effect of Fms-like tyrosine kinase 3 (FLT3) ligand (FL) on antitumor activity of gilteritinib, a FLT3 inhibitor, in mice xenografted with FL-overexpressing cells. Oncotarget. 2019 Oct 22;10(58):6111-6123. | ||||
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