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SGC-SMARCA-BRDVIII | Inhibitor of SMARCA2, SMARCA4, PBRM1
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

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Targets Biochemical/Biophysical Potency Cellular Potency
SMARCA2
  • Kd:35 nM
  • EC50:< 1000 nM
SMARCA4
  • Kd:36 nM
  • EC50:< 1000 nM
PBRM1
  • Kd:13 nM
  • EC50:< 1000 nM
500-1000 nM
up to 10 uM

Selectivity

In Vitro Selectivity Assessment

Potency: KD - PB1(2) 3655 nM, PB1(3) 1963 nM

Selectivity Assessment Description:
Selectivity of the SGC-SMARCA-BRDVIII probe within the bromodomain families was confirmed by an in-h ...
In Cell Selectivity Assessment
Selectivity Assessment Description:
SGC-SMARCA-BRDVIII is non-toxic and does not influence cell growth at a dose of 10 µM as indicated i ...

Potency
Cellular
In Vitro

SMARCA2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.0c01242

SMARCA4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.0c01242

PBRM1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.0c01242

Negative Control Compounds

SGC-BRDVIII-NC
Notes: SGC-BRDVIII-NC showed no cellular activity.

Orthogonal Probes def

PFI-3
ACBI1
GNE-064

Chemical Information

Molecular Formula C19H25N5O3
SMILEs CC(C)(C)OC(=O)N1CCN(c2cc(-c3ccccc3O)nnc2N)CC1
InChI InChI=1S/C19H25N5O3/c1-19(2,3)27-18(26)24-10-8-23(9-11-24)15-12-14(21-22-17(15)20)13-6-4-5-7-16(13)25/h4-7,12,25H,8-11H2,1-3H3,(H2,20,22)
Molecular weight 371.20 Da
AlogP 2.4885
HBond acceptors 8
HBond donors 3
Atoms 52

Vendors

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Expert Reviews

by SERP
(on 29 Mar 2021)
Cellular Use Rating
(The reviewer did not leave any public comments)
by SERP
(on 30 Mar 2021)
Cellular Use Rating
SGC-SMARCA-BRDVIII and control compound SGC-BRDVIII-NC comprise high quality small molecules for the evaluation of the inhibition of SMARCA2/4 and PBRM1.
by SERP+
(on 22 Mar 2023)
Cellular Use Rating
No direct target engagement data is available even though the functions has been tested in different cell lines.
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