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PFI-6 | Inhibitor of MLLT1, MLLT3
RATINGS:
Cellular Use: (1 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
MLLT1
  • IC 50:140 nM
  • Kd:82 nM
  • IC 50:760 nM
MLLT3
  • IC 50:160 nM
  • Kd:76 nM
  • IC 50:760 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
IC50 >40 uM against YEATS2/4. PFI-6 is universally inactive in the SGC Bromodomain panel. Outside ta ...

Potency
Cellular
In Vitro

MLLT1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1101/2021.02.08.430291

MLLT3

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1101/2021.02.08.430291

Negative Control Compounds

PFI-6N

Orthogonal Probes def

SGC-iMLLT
NVS-MLLT-1
SR-0813

Chemical Information

Molecular Formula C22H21N3O4
SMILEs CN(C)C(=O)c1ccc(-c2cc(C(=O)N[C@@H]3CCc4ccccc43)no2)cc1O
InChI InChI=1S/C22H21N3O4/c1-25(2)22(28)16-9-7-14(11-19(16)26)20-12-18(24-29-20)21(27)23-17-10-8-13-5-3-4-6-15(13)17/h3-7,9,11-12,17,26H,8,10H2,1-2H3,(H,23,27)/t17-/m1/s1
Molecular weight 391.15 Da
AlogP 0.0
HBond acceptors 7
HBond donors 2
Atoms 50

References

Publications

Cross References

canSARChEMBLPDBSGC Chemical Probes

Expert Reviews

by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
Presented potency data at the level <0.2 uM seem to be sufficient to support the application of compound PFI-6 as chemical probe for MLLT1/3. However, the side-by-side comparison with the negative control...
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