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PFI-4 | PFI-4 : Inhibitor of BRPF1
RATINGS:
Cellular Use: (3 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
BRPF1 (Other variant:Isoform B)
  • Kd:13 nM
  • IC50:172 nM
  • ΔTm:9.4 Celciuys
  • IC50:240 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
PFI-4 induced significant temperature shifts for BRPF1B (ΔTm of 9.4 °C). Weak interactions (2.0 °C) ...

Potency
Cellular
In Vitro

BRPF1 (Other variant:Isoform B)

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/ml5002932

Chemical Information

Molecular Formula C21H24N4O3
SMILEs COc1ccccc1C(=O)Nc1cc2c(cc1N1CCCC1)n(C)c(=O)n2C
InChI InChI=1S/C21H24N4O3/c1-23-17-12-15(22-20(26)14-8-4-5-9-19(14)28-3)16(25-10-6-7-11-25)13-18(17)24(2)21(23)27/h4-5,8-9,12-13H,6-7,10-11H2,1-3H3,(H,22,26)
Molecular weight 380.18 Da
AlogP 2.738100000000001
HBond acceptors 7
HBond donors 1
Atoms 52

Vendors

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Expert Reviews

by SERP
(on 19 Jul 2022 )
Cellular Use Rating
Recommended for in vitro studies at a 1 uM concentration. No PK data available so not recommended for in vivo studies without first determining the PK profile.
by SERP
(on 2 Aug 2022 )
Cellular Use Rating
A structurally negative control compound has not been recommended in the publication. Pan-BRPF bromodomain inhibitors (OF-1, NI-57) led to similar phenotypes in specific model systems. CECR2 is an off-target...
by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
The selectivity of this compound is very good, but a negative control is missing. No in vivo efficacy has been established and no DMPK data are available.
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