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NVS-BPTF-1 | NVS-BPTF-1 : Inhibitor of BPTF
RATINGS:
Cellular Use: (2 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
BPTF
  • Kd:3 nM
  • Kd:71 nM
  • IC50:56 nM
  • IC50:16 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
A DSF screen against Human bromodomains reveals no significant off-targets. A BROMOscan with NVS-BPT ...

Potency
Cellular
In Vitro

BPTF

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1016/j.bmcl.2021.128208

Negative Control Compounds

CANSAR3550558
Notes: NVS-BPTF-C showed no binding to 14 GPCRs, 3 nuclear receptors, 3 transporters and 5 enzymes with an IC50<10µM in the NIBR principal panel.

Chemical Information

Molecular Formula C26H28FN7O3S
SMILEs Cc1c(Nc2ccc(S(=O)(=O)N3CCN(C)CC3)cc2F)nc2ccc(-c3cnn(C4CC4)c3)cn2c1=O
InChI InChI=1S/C26H28FN7O3S/c1-17-25(29-23-7-6-21(13-22(23)27)38(36,37)32-11-9-31(2)10-12-32)30-24-8-3-18(15-33(24)26(17)35)19-14-28-34(16-19)20-4-5-20/h3,6-8,13-16,20,29H,4-5,9-12H2,1-2H3
Molecular weight 537.20 Da
AlogP 0.0
HBond acceptors 10
HBond donors 1
Atoms 66

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Expert Reviews

by SERP
(on 9 May 2022 )
Cellular Use Rating
The reported IC50 values for NVS-BPTF-1 are single and double digit nM against the primary target (depending upon the assay). The reported off-target potencies for NVS-BPTF-1 against 3 GPCRS are: Ad3 (4.9...
by SERP
(on 14 Jul 2022 )
Cellular Use Rating
NVS-BPTF-1 shows IC50 values for target engagement in the 30-70 nM range and good selectivity in bromodomain and kinase panels. Currently, only limited data is for intracellular target engagement, but...
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