SR-302

SR-302 : Inhibitor of DDR1, DDR2, MAPK11, MAPK14

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe SR-302 is in the process of SERP review.

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Information

DDR1
DDR2
MAPK11
MAPK14

Inhibitor

100 nM

Additional Data

SGC image SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q08345

Target Class: Kinase

Target SubClass: CMGC

Potency: IC50

Potency Value: 53.3 nM

Potency Assay: Enzyme kinetic assay from"Reaction Biology" (ATP conc.: 100 µM)

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

Target aliases:

Epithelial discoidin domain-containing receptor 1, ...

DOI Reference: 10.1021/acs.jmedchem.1c00868

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Probe Selectivity in Vitro:

Closest off-targets found in KinomeScan: ABL1, RIPK2, RPS6KA5, CHEK2, STK38L; for all IC50 > 25 µM (> 125 fold selective) in NanoBRET assay

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

SR-302 shows good potency for DDR1 and DDR2 in vitro determined by enyzme kinetic assay (IC50 = 53.3 nM and IC50 = 0.75 nM). Activity in cells was investigated via NanoBRET which delivered IC50 = 23 nM and IC50 = 18 nM. Kinome wide selectivity screening (0.1 uM inhibitor concentration) showed off-targets p38alfa (IC50 = 125 nM) and p38beta (IC50 = 196 nM) with 10fold decreased potency. Due to high IC50 values on the off-targets and very high in cellulo potency, SR-302 is a valuable tool compound for studying biology of DDR1/2 in combination with other orthogonal probes.

(last updated: 17 Jun 2024 )