Structure of PDB 5fbn Chain D

Receptor sequence
>5fbnD (length=255) Species: 9606 (Homo sapiens) [Search protein sequence]
SWEIDPKDLTFLKELGTGQFGVVKYGKWRGQYDVAIKMIKEGSMSEDEFI
EEAKVMMNLSHEKLVQLYGVCTKQRPIFIITEYMANGCLLNYLREMRHRF
QTQQLLEMCKDVCEAMEYLESKQFLHRDLAARNCLVNDQGVVKVSDFGLS
RYVLDFPVRWSPPEVLMYSKFSSKSDIWAFGVLMWEIYSLGKMPYERFTN
SETAEHIAQGLRLYRPHLASEKVYTIMYSCWHEKADERPTFKILLSNILD
VMDEE
3D structure
PDB5fbn Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis.
ChainD
Resolution1.8 Å
3D
structure
Catalytic site residues are labeled in the structure
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Enzymatic activity
Catalytic site (original residue number in PDB) N526 D539
Catalytic site (residue number reindexed from 1) N133 D146
Enzyme Commision number 2.7.10.2: non-specific protein-tyrosine kinase.
Interaction with ligand
Site
#		 Ligand Ligand
chain		 Binding residues on receptor
(original residue number in PDB)		 Binding residues on receptor
(residue number reindexed from 1)		 Binding affinity
BS01 5WF D L408 T410 V416 A428 K430 F442 M449 L460 I472 T474 M477 G480 C481 N484 L528 S538 D539 F540 L542 L15 T17 V23 A35 K37 F49 M56 L67 I79 T81 M84 G87 C88 N91 L135 S145 D146 F147 L149 MOAD: ic50=0.27nM
BindingDB: IC50=8.0nM,EC50=<10.00nM
BS02 5WE D W421 Y425 S453 Q459 Y461 W28 Y32 S60 Q66 Y68
BS03 5WE D R618 E624 Y627 T628 Y631 R215 E221 Y224 T225 Y228
Gene Ontology
Molecular Function
GO:0004672 protein kinase activity
GO:0004713 protein tyrosine kinase activity
GO:0005524 ATP binding
Biological Process
GO:0006468 protein phosphorylation

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Molecular Function
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Biological Process
External links
PDB RCSB:5fbn, PDBe:5fbn, PDBj:5fbn
PDBsum5fbn
PubMed26985298
UniProtQ06187|BTK_HUMAN Tyrosine-protein kinase BTK (Gene Name=BTK)

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