Target Binding Site Detail

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Target General Information
Ligand General Information
Drug Binding Sites of Target
References
Target General Information  Top
Target ID T08741 Target Info
Target Name Tyrosine-protein kinase CSK (CSK)
Synonyms Protein-tyrosine kinase CYL; C-Src kinase
Target Type Patented-recorded Target
Gene Name CSK
Biochemical Class Kinase
UniProt ID
CSK_HUMAN
Ligand General Information  Top
Ligand Name Staurosporine Ligand Info
Canonical SMILES CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC
InChI 1S/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/t17-,20-,26-,28+/m1/s1
InChIKey HKSZLNNOFSGOKW-FYTWVXJKSA-N
PubChem Compound ID 44259
Drug Binding Sites of Target  Top
PDB ID: 1BYG      KINASE DOMAIN OF HUMAN C-TERMINAL SRC KINASE (CSK) IN COMPLEX WITH INHIBITOR STAUROSPORINE
Method X-ray diffraction Resolution 2.40 Å Mutation No [1]
PDB Sequence
GWALNMKELK
196
LLQTIGKGEF
206
GDVMLGDYRG
216
NKVAVKCIKN
226
DAQAFLAEAS
238

VMTQLRHSNL
248
VQLLGVIVEE
258
GLYIVTEYMA
270
KGSLVDYLRS
280
RGRSVLGGDC
290

LLKFSLDVCE
300
AMEYLEGNNF
310
VHRDLAARNV
320
LVSEDNVAKV
330
SDFGLLPVKW
352

TAPEALREKK
362
FSTKSDVWSF
372
GILLWEIYSF
382
GRVPYPRIPL
392
KDVVPRVEKG
402

YKMDAPDGCP
412
PAVYEVMKNC
422
WHLDAAMRPS
432
FLQLREQLEH
442
IKTHEL
Residue
Distance (Å)
ILE201
3.632
GLY202
3.362
LYS203
3.741
GLY204
4.090
VAL209
3.819
ALA220
3.162
LYS222
4.010
VAL249
3.929
THR266
3.387
GLU267
2.933
Residue
Distance (Å)
TYR268
3.529
MET269
2.663
GLY272
3.660
SER273
3.668
ASP276
4.851
ARG318
3.011
ASN319
3.621
VAL320
4.585
LEU321
3.391
SER331
3.967
PDB ID: 3D7T      Structural basis for the recognition of c-Src by its inactivator Csk
Method X-ray diffraction Resolution 2.90 Å Mutation Yes [2]
PDB Sequence
WALNMKELKL
197
LQTIGKGEFG
207
DVMLGDYRGN
217
KVAVKCIKND
227
ATAQAFLAEA
237

SVMTQLRHSN
247
LVQLLGVIVE
257
EKGGLYIVTE
267
YMAKGSLVDY
277
LRSRGRSVLG
287

GDCLLKFSLD
297
VCEAMEYLEG
307
NNFVHRDLAA
317
RNVLVSEDNV
327
AKVSDFGPVK
351

WTAPEALREA
361
AFSTKSDVWS
371
FGILLWEIYS
381
FGRVPYPRIP
391
LKDVVPRVEK
401

GYKMDAPDGC
411
PPAVYEVMKN
421
CWHLDAAMRP
431
SFLQLREQLE
441
HIKTHELHL
Residue
Distance (Å)
ILE201
2.994
GLY202
3.271
LYS203
4.414
GLY204
4.126
VAL209
3.654
ALA220
3.410
LYS222
3.678
VAL249
4.891
THR266
3.653
GLU267
3.621
TYR268
3.527
Residue
Distance (Å)
MET269
3.042
ALA270
4.161
LYS271
4.613
GLY272
3.987
SER273
3.499
ASP276
4.852
ARG318
3.521
VAL320
4.656
LEU321
3.344
SER331
3.738
ASP332
3.834
References  Top
REF 1 Structure of the protein tyrosine kinase domain of C-terminal Src kinase (CSK) in complex with staurosporine. J Mol Biol. 1999 Jan 15;285(2):713-25.
REF 2 Structural basis for the recognition of c-Src by its inactivator Csk. Cell. 2008 Jul 11;134(1):124-34.

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