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GSK6853 | GSK6853 : Inhibitor of BRPF1
RATINGS:
Cellular Use: (1 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
BRPF1
  • IC50:7.9 nM
  • Kd:0.31 nM
  • IC50:20 nM
  • IC50:2.5 nM
Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Within target family: BromoSCAN against 34 DNA-tagged bromodomains, greater than 1600-fold selectivi ...

Potency
Cellular
In Vitro

BRPF1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acsmedchemlett.6b00092

In Vivo Validations

Mouse
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.7 h
Systemic clearance: 107 mL/min/kg
Volume of Distribution at Steady-State: 5.5 L/kg

DOI Reference: 10.1021/acsmedchemlett.6b00092

Dose: 3 mg/Kg
Route of delivery: Oral
Cmax: 42 ng/mL
Tmax: 1.5 h
Bioavailability: 22%

DOI Reference: 10.1021/acsmedchemlett.6b00092

Dose: 3 mg/Kg
Route of delivery: Intraperitoneal
Cmax: 469 ng/mL
Tmax: 0.25 h
Fb : 82.1%
Bioavailability: 85%

DOI Reference: 10.1021/acsmedchemlett.6b00092

Negative Control Compounds

8VI
Notes: GSK9311 (cpd 38) 100-fold drop in BRPF1 inhibition

Chemical Information

Molecular Formula C22H27N5O3
SMILEs COc1ccccc1C(=O)Nc1cc2c(cc1N1CCNC[C@H]1C)n(C)c(=O)n2C
InChI InChI=1S/C22H27N5O3/c1-14-13-23-9-10-27(14)17-12-19-18(25(2)22(29)26(19)3)11-16(17)24-21(28)15-7-5-6-8-20(15)30-4/h5-8,11-12,14,23H,9-10,13H2,1-4H3,(H,24,28)/t14-/m1/s1
Molecular weight 409.21 Da
AlogP 1.9359999999999997
HBond acceptors 8
HBond donors 2
Atoms 57

Expert Reviews

by SERP
(on 6 Mar 2026 )
Cellular Use Rating
In Model Organisms
Prior to performing in vivo experiments, I suggest reviewing the in vivo exposure data in mouse that is provided in the supplementary material to ensure that the exposure is high enough, as a higher dose...

Portal Comments

In a 2023 study, Hu et al. evaluated GSK6853 in live-cell assays for Phospholipidosis induction, cautioning about adverse effects at concentrations near 1 uM. (DOI:10.1016/j.chembiol.2023.09.003)

(last updated: 7 Nov 2023)

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