TP-030-1

TP-030-1 : Inhibitor of RIPK1

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(0 ratings)

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Probe TP-030-1 is in the process of SERP review.

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Information

RIPK1

Inhibitor

100 nM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q13546

Target Class: Kinase

Target SubClass: TKL

Potency: Ki

Potency Value: 3.9 nM

Potency Assay: Human RIPK1 in cell free assay

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: Clean LeadProfilingScreen (68 targets tested; Eurofins-Panlabs). One off-target in the GPCR scan: GABA/PBR Ki = 374.92 nM.

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SERP ratings and comments

SERP Ratings

In Cell Rating

(last updated: 27 Jun 2022 )

SERP+ Ratings

In Cell Rating

SERP+ Comments:

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.

(last updated: 23 May 2024 )