TP-030-2

TP-030-2 : Inhibitor of RIPK1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe TP-030-2 is in the process of SERP review.

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Information

RIPK1

Inhibitor

100 nM
Reviewer recommended concentration: >100nM to inhibit >95% of RIPK1

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q13546

Target Class: Kinase

Target SubClass: TKL

Potency: Ki

Potency Value: 0.43 nM

Potency Assay: TR-FRET (human RIPK1)

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Receptor-interacting serine/threonine-protein kina ...

DOI Reference: 10.1021/acs.jmedchem.7b01647

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Selectivity within target family - No significant binding observed at 1 µM from in-house Global Kinase Panel (303 kinases). Selectivity outside target family - LeadProfilingScreen (68 targets tested; Eurofins-Panlabs): Closest off-targets in the GPCR scan are GABA/PBR Ki = 346.58 nM, HTR2A Ki = 2071.02 nM and ADRA2A Ki = 2355.74 nM.

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

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 against a non-cancer cell line is missing.

(last updated: 22 Mar 2023 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

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 PK profile which may prevent to use it in vivo. Data can also be found in the patent: US20180319819

(last updated: 17 Jun 2024 )