Chemical Probes logo
TP-238 | TP-238 : Inhibitor of CECR2, BPTF
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
CECR2
  • IC50:30 nM
  • Kd:10 nM
  • EC50:289 nM
BPTF
  • IC50:350 nM
  • Kd:120 nM
  • EC50:228 nM
Inhibitor
up to 2 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
The closest off-target bromodomain inhibition is BRD9 with IC50 of 1.4 µM. TP-238 has been profiled ...

Potency
Cellular
In Vitro

CECR2

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1039/d0ob00506a

BPTF

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1039/d0ob00506a

Negative Control Compounds

TP-422
Notes: TP-422 exhibited no significant activity in NanoBRET
SMILES: CN(C)CCCOc1ccc(cc1)c1cc(nc(n1)OC)OCCCn1cccn1

Orthogonal Probes def

NVS-CECR2-1
NVS-BPTF-1

Chemical Information

Molecular Formula C22H30N6O3S
SMILEs CN(C)CCCOc1ccc(-c2cc(NCCCn3cccn3)nc(S(C)(=O)=O)n2)cc1
InChI InChI=1S/C22H30N6O3S/c1-27(2)13-6-16-31-19-9-7-18(8-10-19)20-17-21(26-22(25-20)32(3,29)30)23-11-4-14-28-15-5-12-24-28/h5,7-10,12,15,17H,4,6,11,13-14,16H2,1-3H3,(H,23,25,26)
Molecular weight 458.21 Da
AlogP 2.5763000000000007
HBond acceptors 9
HBond donors 1
Atoms 62

Expert Reviews

by SERP
(on 2 Jun 2023 )
Cellular Use Rating
( The reviewer did not leave any comments )
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