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INCB085660 | INCB085660 : inhibitor of PD-L1
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 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
CD274
  • IC50:3.1 nM
  • IC50:13 nM
  • IC50:6.3 nM
  • EC50:21.4 nM
PPI
200 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Selectivity within target family: PD-L2 IC50 > 10uM

Potency
Cellular
In Vitro

CD274

Mode of Action: PPI

Structure-Activity-Relationship data available? No

DOI Reference: 10.1158/2159-8290.CD-21-1156

In Vivo Validations

Mouse
Dose: 2, 20, 200 mg/Kg
Route of delivery: Oral
Target engagement assay: tumor growth inhibition (TGI) of 32%, 66%, and 69% for 2, 20, and 200 mg/kg, respectively.

DOI Reference: 10.1158/2159-8290.CD-21-1156

Chemical Information

Molecular Formula C41H39N7O4
SMILEs Cc1c(Nc2nccc3cc(CN4CC[C@@H](O)C4)cnc23)cccc1-c1cccc(-c2nc3cc(CN4CC[C@@H](C(=O)O)C4)cc(C#N)c3o2)c1C
InChI InChI=1S/C41H39N7O4/c1-24-32(5-3-7-34(24)40-46-36-17-26(15-30(18-42)38(36)52-40)20-47-13-10-29(22-47)41(50)51)33-6-4-8-35(25(33)2)45-39-37-28(9-12-43-39)16-27(19-44-37)21-48-14-11-31(49)23-48/h3-9,12,15-17,19,29,31,49H,10-11,13-14,20-23H2,1-2H3,(H,43,45)(H,50,51)/t29-,31-/m1/s1
Molecular weight 693.31 Da
AlogP 6.810220000000006
HBond acceptors 11
HBond donors 3
Atoms 91

Vendors

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Expert Reviews

No SERP comments found for INCB085660

Probe INCB085660 is in the process of SERP review.

Please continue to check back for new reviews and commentary.