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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
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
BRPF1
  • IC50:80 nM
  • IC50:980 nM
Antagonist
500 nM up to 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? Yes

DOI Reference: 10.1021/ml5002932

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

Publications

Cross References

ChEMBL BindingDB PDB PubChem canSAR

Vendors

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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This is a good compound but it has been superseded by GSK6853 chemical probe, which has greatly improved solubility and cell activity.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 However, the compound has been superseded by GSK-6853...
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