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TP-030-1 | TP-030-1 : 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:3.9 nM
  • IC50:18 nM
Inhibitor
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 Kinas ...

Potency
Cellular
In Vitro

RIPK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

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

Chemical Information

Molecular Formula C23H22N4O3
SMILEs CN1C(=O)[C@@H](N2CCc3cn(Cc4ccccc4)nc3C2=O)COc2ccccc21
InChI InChI=1S/C23H22N4O3/c1-25-18-9-5-6-10-20(18)30-15-19(22(25)28)27-12-11-17-14-26(24-21(17)23(27)29)13-16-7-3-2-4-8-16/h2-10,14,19H,11-13,15H2,1H3/t19-/m0/s1
Molecular weight 402.17 Da
AlogP 2.353699999999999
HBond acceptors 7
HBond donors --
Atoms 52

Expert Reviews

by SERP
(on 27 Jun 2022)
Cellular Use Rating
(The reviewer did not leave any public comments)
by SERP+
(on 23 May 2024)
Cellular Use Rating
Please note the drop of in potency on mouse protein. Methodology on details for TR-FRET has not been provided especially lacking ATP and tracer concentration.
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