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TP-030-2 | TP-030-2 : Inhibitor of RIPK1
RATINGS:
Cellular Use: (2 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
RIPK1
  • Ki:0.43 nM
  • IC50:1.3 nM
Inhibitor
>100nM to inhibit >95% of RIPK1
100 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
Selectivity within target family - No significant binding observed at 1 µM from in-house Global Kina ...

Potency
Cellular
In Vitro

RIPK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.7b01647

Negative Control Compounds

TP-030n
Notes: TP-030n: RIPK1 (h): Ki = 6900 nM; RIPK1 (m): Ki > 10 µM.

Orthogonal Probes def

GSK481
GSK2982772

Chemical Information

Molecular Formula C23H21BrN4O3
SMILEs CN1C(=O)[C@@H](N2CCc3c(nn(Cc4ccccc4)c3Br)C2=O)COc2ccccc21
InChI InChI=1S/C23H21BrN4O3/c1-26-17-9-5-6-10-19(17)31-14-18(22(26)29)27-12-11-16-20(23(27)30)25-28(21(16)24)13-15-7-3-2-4-8-15/h2-10,18H,11-14H2,1H3/t18-/m0/s1
Molecular weight 480.08 Da
AlogP 3.116200000000001
HBond acceptors 7
HBond donors --
Atoms 52

Expert Reviews

by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
The compound is well characterised with very detailed on/off rate determination. An excellent safety panel test and selectivity panel against > 300 kinases has been performed. Cytotoxicity assessment...
by SERP+
(on 17 Jun 2024 )
Cellular Use Rating
It is well-charaterized, potent and highly selective probe compound vs off- and in-family targets. An excellent negative probe is available. The compound has a moderate solubility and moderate in vivo...
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