Binding Site Information of Target

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Target General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T11764 Target Info
Target Name Discoidin domain-containing receptor 2 (DDR2)
Synonyms Tyrosine-protein kinase TYRO10; Receptor protein-tyrosine kinase TKT; Neurotrophic tyrosine kinase, receptor-related 3; Discoidin domain-containing receptor tyrosine kinase 2; Discoidin domain receptor 2; DDR2; CD167 antigen-like family member B
Target Type Patented-recorded Target
Gene Name DDR2
Biochemical Class Kinase
UniProt ID
DDR2_HUMAN
Drug Binding Sites of Target  Top
Ligand Name: 2-[4,5-bis(fluoranyl)-2-oxidanylidene-1'-(1~{H}-pyrazolo[3,4-b]pyridin-5-ylcarbonyl)spiro[indole-3,4'-piperidine]-1-yl]-~{N}-[2,2,2-tris(fluoranyl)ethyl]ethanamide Ligand Info
Structure Description Crystal Structure of human DDR2 kinase in complex with 2-[4,5-difluoro-2-oxo-1'-(1H-pyrazolo[3,4-b]pyridine-5-carbonyl)spiro[indole-3,4'-piperidine]-1-yl]-N-(2,2,2-trifluoroethyl)acetamide PDB:6FER
Method X-ray diffraction Resolution 2.87 Å Mutation No [1]
PDB Sequence
VAVEEFPRKL
609
LTFKEKLGEG
619
QFGEVHLCEV
629
EGPVLVAVKM
656
LRADANKNAR
666

NDFLKEIKIM
676
SRLKDPNIIH
686
LLAVCITDDP
696
LCMITEYMEN
706
GDLNQFLSRH
716

TVSYTNLKFM
737
ATQIASGMKY
747
LSSLNFVHRD
757
LATRNCLVGK
767
NYTIKIADFG
777

MSRNLYSGDY
787
YRIQGRAVLP
797
IRWMSWESIL
807
LGKFTTASDV
817
WAFGVTLWET
827

FTFCQEQPYS
837
QLSDEQVIEN
847
TGEFFRDQGR
857
QTYLPQPAIC
867
PDSVYKLMLS
877

CWRRDTKNRP
887
SFQEIHLLLL
897
Q
Residue
Distance (Å)
LEU616
3.753
VAL624
3.075
ALA653
3.515
LYS655
3.797
GLU672
3.643
MET676
3.373
LEU679
3.796
ILE684
3.668
ILE685
3.296
LEU687
4.473
MET699
3.327
ILE700
3.798
THR701
3.017
Residue
Distance (Å)
GLU702
4.127
TYR703
3.092
MET704
3.019
GLY707
4.876
LEU748
4.188
PHE753
3.408
HIS755
3.541
LEU764
3.497
ILE773
3.829
ALA774
2.795
ASP775
2.650
PHE776
3.130
References  Top
REF 1 DNA-Encoded Library-Derived DDR1 Inhibitor Prevents Fibrosis and Renal Function Loss in a Genetic Mouse Model of Alport Syndrome. ACS Chem Biol. 2019 Jan 18;14(1):37-49.

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