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PFI-3 | Antagonist of SMARCA2, SMARCA4, PBRM1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 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
SMARCA2
  • Kd:81-86 nM
SMARCA4
  • Kd:97 nM
PBRM1
  • Kd:54 nM
Antagonist
1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
PFI-3 was also profiled against 40 Bromodomains in Tm assay and in BROMOscan assay (DiscoveRx); it h ...
Selectivity Assessment Description:
In a Cerep panel containing 102 cellular receptors and 30 enzymes, PFI-3 had minimal off-target acti ...

Potency
Cellular
In Vitro

SMARCA2

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.6b00012

SMARCA4

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.6b00012

PBRM1

Mode of Action: Antagonist

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.6b00012

Negative Control Compounds

PFI-oMet

Orthogonal Probes def

SGC-SMARCA-BRDVIII
ABCI1

Chemical Information

Molecular Formula C19H19N3O2
SMILEs O=C(/C=C/N1C[C@H]2C[C@@H]1CN2c1ccccn1)c1ccccc1O
InChI InChI=1S/C19H19N3O2/c23-17-6-2-1-5-16(17)18(24)8-10-21-12-15-11-14(21)13-22(15)19-7-3-4-9-20-19/h1-10,14-15,23H,11-13H2/b10-8+/t14-,15-/m1/s1
Molecular weight 321.15 Da
AlogP 2.446700000000001
HBond acceptors 5
HBond donors 1
Atoms 43

References

Publications

Cross References

GDSC1GDSC2

Vendors

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Expert Reviews

by SERP
(on 29 Apr 2020 )
Cellular Use Rating
This is a first-in-class inhibitor of the BAF bromodomains BRG and BRM. Data is only available for cell-based interogations. In this setting, PFI-3 should enable a range of studies around the cell-based...
by SERP
(on 29 Apr 2020 )
Cellular Use Rating
In Model Organisms
PFI-3 represents a well-studied and selective probe for the targets listed, suitable for cellular work. Care is needed in choosing appropriate cellular concentrations – target engagement is reported...
by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
The compound showed potent inhibitory activity against SMARCA2/4 ATPase. The Kd is 54 - 97 nM determined by the ITC experiment, and 110 nM determined by the BLI technique. A total of 48 and 32 bromodomain...
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria