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GSK8814 | GSK8814 : Inhibitor of ATAD2, ATAD2B
RATINGS:
Cellular Use: (2 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
ATAD2
  • Kd:7.94 nM
  • Ki:1.25 nM
  • IC 50:50.1 nM
  • IC 50:2 uM
ATAD2B
  • IC 50:20 nM ATAD2B
  • IC 50:2 uM
Inhibitor
up to 10 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
BROMOscan
Selectivity Assessment Description:
GSK8814 is more than 100 folds selective over all other bromodomains in the BROMOscan. More than ...

Potency
Cellular
In Vitro

ATAD2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.201603928

ATAD2B

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1002/anie.201603928

Orthogonal Probes def

BAY-850

Chemical Information

Molecular Formula C28H35F2N5O3
SMILEs CO[C@H]1CNC[C@@H](OCC2CCC(F)(F)CC2)[C@@H]1Nc1ncc(-c2cncc(C)c2)c2cc(C)c(=O)[nH]c12
InChI InChI=1S/C28H35F2N5O3/c1-16-8-19(11-31-10-16)21-12-33-26(24-20(21)9-17(2)27(36)35-24)34-25-22(37-3)13-32-14-23(25)38-15-18-4-6-28(29,30)7-5-18/h8-12,18,22-23,25,32H,4-7,13-15H2,1-3H3,(H,33,34)(H,35,36)/t22-,23+,25+/m0/s1
Molecular weight 527.27 Da
AlogP 4.21134
HBond acceptors 8
HBond donors 3
Atoms 73

Vendors

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Expert Reviews

by SERP
(on 4 Jan 2022)
Cellular Use Rating
No in Vitro data is available at this time. More data needed and need more update
by SERP+
(on 23 Sept 2024)
Cellular Use Rating
(The reviewer did not leave any public comments)
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