Binding Site Information of Target

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Target General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T68163 Target Info
Target Name Tyrosine-protein kinase Lyn (JTK8)
Synonyms p56Lyn; p53Lyn; V-yes-1 Yamaguchi sarcoma viral related oncogene homolog; Lck/Yes-related novel protein tyrosine kinase
Target Type Clinical trial Target
Gene Name LYN
Biochemical Class Kinase
UniProt ID
LYN_HUMAN
Drug Binding Sites of Target  Top
Ligand Name: Staurosporine Ligand Info
Structure Description Lyn kinase domain PDB:3A4O
Method X-ray diffraction Resolution 3.00 Å Mutation No [1]
PDB Sequence
DAWEIPRESI
16
KLVKRLGAGQ
26
FGEVWMGYYN
36
NSTKVAVKTL
46
KPGTMSVQAF
56

LEEANLMKTL
66
QHDKLVRLYA
76
VVTREEPIYI
86
ITEYMAKGSL
96
LDFLKSDEGG
106

KVLLPKLIDF
116
SAQIAEGMAY
126
IERKNYIHRD
136
LRAANVLVSE
146
SLMCKIADFG
156

LARVEGAKFP
175
IKWTAPEAIN
185
FGCFTIKSDV
195
WSFGILLYEI
205
VTYGKIPYPG
215

RTNADVMTAL
225
SQGYRMPRVE
235
NCPDELYDIM
245
KMCWKEKAEE
255
RPTFDYLQSV
265

LDDFYTATE
Residue
Distance (Å)
LEU22
3.674
GLY23
4.099
ALA24
4.976
VAL30
3.397
ALA42
3.882
LYS44
3.732
VAL72
4.063
THR88
3.536
GLU89
2.672
TYR90
2.997
MET91
2.866
Residue
Distance (Å)
ALA92
3.785
LYS93
4.590
GLY94
3.525
SER95
3.576
ASP98
4.936
ALA140
3.265
ASN141
4.337
VAL142
4.964
LEU143
2.998
ALA153
4.339
ASP154
4.189
Ligand Name: N-(1h-Indazol-6-Yl)-8-Piperidin-4-Yloxy-6-Propyl-Quinazolin-2-Amine Ligand Info
Structure Description Crystal structure of Lyn kinase domain in complex with N-(1H-indazol-6-yl)-8-(piperidin-4-yloxy)-6-propylquinazolin-2-amine PDB:5XY1
Method X-ray diffraction Resolution 2.70 Å Mutation No [2]
PDB Sequence
SAWEIPRESI
247
KLVKRLGAGQ
257
FGEVWMGYYN
267
NSTKVAVKTL
277
KPGTMSVQAF
287

LEEANLMKTL
297
QHDKLVRLYA
307
VVTREEPIYI
317
ITEYMAKGSL
327
LDFLKSDEGG
337

KVLLPKLIDF
347
SAQIAEGMAY
357
IERKNYIHRD
367
LRAANVLVSE
377
SLMCKIADFG
387

LARVKFPIKW
409
TAPEAINFGC
419
FTIKSDVWSF
429
GILLYEIVTY
439
GKIPYPGRTN
449

ADVMTALSQG
459
YRMPRVENCP
469
DELYDIMKMC
479
WKEKAEERPT
489
FDYLQSVLDD
499

FYT
Residue
Distance (Å)
LEU253
3.753
GLY254
4.502
VAL261
3.519
ALA273
3.386
LYS275
4.587
GLU290
3.228
MET294
3.749
VAL303
4.294
THR319
3.357
GLU320
3.441
TYR321
3.536
Residue
Distance (Å)
MET322
2.984
ALA323
3.655
LYS324
4.027
GLY325
3.305
SER326
4.435
ASP329
4.334
ALA371
3.536
LEU374
3.344
ALA384
3.060
ASP385
4.275
PHE386
4.639
References  Top
REF 1 Structural basis for the inhibitor recognition of human Lyn kinase domain. Bioorg Med Chem Lett. 2009 Dec 1;19(23):6557-60.
REF 2 Crystal structure of Lyn kinase domain in complex with N-(1H-indazol-6-yl)-8-(piperidin-4-yloxy)-6-propylquinazolin-2-amine

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