Het-PDB Navi2 (PDB: 5X02)

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Ligands
Code	Name		Style	Show	Link
F6M	N-[(2s)-1-[5-[2-[(4-cyanophenyl)amino]-4-(propylamino)pyrimidin-5-yl]pent-4-ynylamino]-1-oxidanylidene-propan-2-yl]-4-(dimethylamino)-N-methyl-but-2-enamide				PoSSuM
SO4	Sulfate ion				PoSSuM

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Download interaction data: 5X02

Code :

5X02 PDBj RCSB PDB PDBe

Header :

TRANSFERASE/TRANSFERASE INIHIBITOR

Title :

Crystal structure of the FLT3 kinase domain bound to the inhibitor FF-10101

Release Data :

2018-01-24

Compound :

mol_id	molecule	chains	synonym
1	Receptor-type tyrosine-protein kinase FLT3	A	FL cytokine receptor,Fetal liver kinase-2,FLK-2,Fms-like tyrosine kinase 3,FLT-3,Stem cell tyrosine kinase 1,STK-1,FL cytokine receptor,Fetal liver kinase-2,FLK-2,Fms-like tyrosine kinase 3,FLT-3,Stem cell tyrosine kinase 1,STK-1
	ec: 2.7.10.1 fragment: UNP residues 564-710,762-958

Source :

mol_id	organism_scientific	organism_common	expression_system
1	Homo sapiens (taxid:9606)	Human	Spodoptera frugiperda (taxid:7108)
	gene: FLT3, CD135, FLK2, STK1 expression_system_vector_type: baculovirus

Authors :

Fujikawa, N., Hirano, D., Takasaki, M., Terada, D., Hagiwara, S., Park, S.-Y., Sugiyama, K.

Keywords :

tyrosine kinase, transferase, irreversible inhibitor complex, kinase catalytic domain, TRANSFERASE-TRANSFERASE INIHIBITOR complex

Exp. method :

X-RAY DIFFRACTION ( 2.4010 Å )

Citation :

A novel irreversible FLT3 inhibitor, FF-10101, shows excellent efficacy against AML cells withFLT3mutations.

Yamaura, T.,Nakatani, T.,Uda, K. et al.
(2018) Blood 131 : 426 - 438

Chain :

UniProt :

P36888 (FLT3_HUMAN)

Reaction:	EC:	Evidence:
Reaction:	Physiological Direction:	Evidence:
ATP + L-tyrosyl-[protein] = ADP + H(+) + O-phospho-L-tyrosyl- [protein]	2.7.10.1	PROSITE-ProRule:PRU10028, PubMed:15831474
	-	PROSITE-ProRule:PRU10028, PubMed:15831474

PDB ID: 5X02