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GSK215 | GSK215 : Degrader (PROTAC) of PTK2
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PTK2
  • IC50:20 nM
  • IC50:15.8 nM
  • DC50:4 nM
  • DC50:1.3 nM
Degrader (PROTAC)
up to 100 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
Profiling of GSK215 using a cell lysate kinobead assay showed that the PROTAC maintained high select ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
GSK215 was further assessed by multiplexed proteome dynamics profiling (mPDP): In mature proteins, G ...
Selectivity Assessment Description:
After 24 h treatment, the selectivity of degradation for GSK215 was maintained up to 10 nM while at ...

Potency
Cellular
In Vitro

PTK2

Mode of Action: Degrader (PROTAC)

Structure-Activity-Relationship data available? No

DOI Reference: 10.1002/anie.202109237

In Vivo Validations

Mouse
Dose: 8 mg/Kg
Route of delivery: Subcutaneous
Cmax: 526 ng/mL
Tmax: 0.33 h

DOI Reference: 10.1002/anie.202109237

Negative Control Compounds

ent-6
Notes: ent-6 does not degrade FAK
SMILES: C[C@H](C1=CC=C(C=C1)C2=C(C)N=CS2)NC(=O)[C@H]3C[C@@H](CN3C(=O)[C@@H](C(C)(C)C)NC(=O)CN4CCN(CC4)C5=CC(=C(C=C5)NC6=NC=C(C(=C6)NC7=C(C=CC=C7)C(=O)NC)C(F)(F)F)OC)O

Chemical Information

Molecular Formula C50H59F3N10O6S
SMILEs CNC(=O)c1ccccc1Nc1cc(Nc2ccc(N3CCN(CC(=O)N[C@H](C(=O)N4C[C@H](O)C[C@H]4C(=O)N[C@@H](C)c4ccc(-c5scnc5C)cc4)C(C)(C)C)CC3)cc2OC)ncc1C(F)(F)F
InChI InChI=1S/C50H59F3N10O6S/c1-29(31-12-14-32(15-13-31)44-30(2)56-28-70-44)57-47(67)40-23-34(64)26-63(40)48(68)45(49(3,4)5)60-43(65)27-61-18-20-62(21-19-61)33-16-17-38(41(22-33)69-7)59-42-24-39(36(25-55-42)50(51,52)53)58-37-11-9-8-10-35(37)46(66)54-6/h8-17,22,24-25,28-29,34,40,45,64H,18-21,23,26-27H2,1-7H3,(H,54,66)(H,57,67)(H,60,65)(H2,55,58,59)/t29-,34+,40-,45+/m0/s1
Molecular weight 984.43 Da
AlogP 6.879820000000007
HBond acceptors 16
HBond donors 6
Atoms 129

References

Publications

Cross References

canSARChEMBLPDB

Expert Reviews

by SERP
(on 11 Jan 2026 )
Cellular Use Rating
In Model Organisms
GSK-215 is the most effective PROTAC for studying the in vivo degradation of FAK. GSK215 has been thoroughly characterised in biochemical and cellular assays. The crystal structure of the ternary complex...
by SERP+
(on 6 Feb 2026 )
Cellular Use Rating
In Model Organisms
GSK-215 represents a well validated degrader for FAK. GSK-215 exhibits high kinase selective for FAK (as determined by kinobead assay in lysate) and potent degradation in cells, DC50 = 1.3 nM, DMax ~99%....
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