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BMS-986408 | BMS-986408 : Inhibitor and degrader of DGKA, DGKZ
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
DGKA
  • IC50:0.3 nM
  • Kd:158 nM
  • EC50:26 nM
  • Dmax:>90%
DGKZ
  • IC50:2 nM
  • Kd:55 nM
  • EC50:8 nM
  • Dmax:>80%
inhibitor and degrader
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Among the type I family, BMS-986408 showed > 100-fold selectivity for DGKα over DGKβ and DGKγ. Among ...

Potency
Cellular
In Vitro

DGKA

Mode of Action: inhibitor and degrader

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/2326-6066.CIR-25-0156

DGKZ

Mode of Action: inhibitor and degrader

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1158/2326-6066.CIR-25-0156

Chemical Information

Molecular Formula C27H31F3N6O
SMILEs CC[C@H]1CN([C@@H](CC)c2ccc(C(F)(F)F)cc2)[C@H](CC)CN1c1nc(=O)n(C)c2ccc(C#N)nc12
InChI InChI=1S/C27H31F3N6O/c1-5-20-16-36(25-24-23(34(4)26(37)33-25)13-12-19(14-31)32-24)21(6-2)15-35(20)22(7-3)17-8-10-18(11-9-17)27(28,29)30/h8-13,20-22H,5-7,15-16H2,1-4H3/t20-,21+,22+/m1/s1
Molecular weight 512.25 Da
AlogP 5.049480000000004
HBond acceptors 7
HBond donors --
Atoms 68

Expert Reviews

No SERP comments found for BMS-986408

Probe BMS-986408 is in the process of SERP review.

Please continue to check back for new reviews and commentary.