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GSK-5959 | Antagonist of BRPF1
RATINGS:
Cellular Use: (3 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
BRPF1
  • IC50:0.08 uM
  • IC50:0.98 uM
Antagonist
between 500 nM and 5 uM

Selectivity

In Vitro Selectivity Assessment

Potency: pIC50 - BRPF2: 5.1, BRPF3 <4, BRD4 (1) <4.3, BRD4 (2) <4.3

Potency Assay Off-Target:
TR-FRET binding assay
Selectivity Assessment Description:
In BROMOscan with 35 bromodomains (DiscoveRx), GSK-5959 was selective for BRPF1.
In Cell Selectivity Assessment
Potency Assay Off-Target:
In nanoBRET assay, GSK-5959 is not active against BRPF1 isoform 2.

Potency
Cellular
In Vitro

BRPF1

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

Orthogonal Probes def

NI-57

Chemical Information

Molecular Formula C22H26N4O3
SMILEs COc1ccccc1C(=O)Nc1cc2c(cc1N1CCCCC1)n(C)c(=O)n2C
InChI InChI=1S/C22H26N4O3/c1-24-18-13-16(23-21(27)15-9-5-6-10-20(15)29-3)17(26-11-7-4-8-12-26)14-19(18)25(2)22(24)28/h5-6,9-10,13-14H,4,7-8,11-12H2,1-3H3,(H,23,27)
Molecular weight 394.20 Da
AlogP 3.1282000000000014
HBond acceptors 7
HBond donors 1
Atoms 55

References

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    Expert Reviews

    by SERP
    (on 13 Apr 2017 )
    Cellular Use Rating
    This is a good compound but it has been superseded by GSK6853 chemical probe, which has greatly improved solubility and cell activity.
    by SERP
    (on 18 Apr 2017 )
    Cellular Use Rating
    This benzimidazolone probe inhibits BRPF1 (bromodomain and PHD finger-containing domain 1). Biochemical data using a TR-FRET format shows an IC50 of 80 nM against BRPF1 with 100X less potency against...
    by SERP
    (on 28 Feb 2018 )
    Cellular Use Rating
    GSK-5959 is a reasonably potent (TR-FRET pIC50 7.1), selective (>100 fold over other BRDs) and cell permeable/cell active (NanoBRET pIC50 6.0). However, the compound has been superseded by GSK-6853...
    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