DDR-TRK-1

DDR-TRK-1 : Inhibitor of DDR1, DDR2, NTRK1, NTRK2, NTRK3

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(1 ratings)

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Probe DDR-TRK-1 is in the process of SERP review.

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Information

DDR1
DDR2
NTRK1
NTRK2
NTRK3

Inhibitor

5 µM; use with selective TRK inhibitor to dissect phenotype

Additional Data

SGC Chemical Probe Collection

In Vitro Validations

Uniprot ID: Q08345

Target Class: Kinase

Target SubClass: Tyrosine kinase

Potency: IC50

Potency Value: 9.4 ± 1.7 nM

Potency Assay: LANCE ULTRA kinase assay

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

Target aliases:

Epithelial discoidin domain-containing receptor 1, ...

DOI Reference: 10.1021/acs.jmedchem.6b00140

Uniprot ID: Q08345

Target Class: Kinase

Target SubClass: Tyrosine kinase

Potency: Kd

Potency Value: 4.7 ± 0.8 nM

Potency Assay: DiscoverX profiling

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

Target aliases:

Epithelial discoidin domain-containing receptor 1, ...

DOI Reference: 10.1021/acs.jmedchem.6b00140

Uniprot ID: Q08345

Target Class: Kinase

Target SubClass: Tyrosine kinase

Potency: IC50

Potency Value: 27 nM

Potency Assay: In an activity assay at RBC (10μM ATP)

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

Target aliases:

Epithelial discoidin domain-containing receptor 1, ...

DOI Reference: 10.1021/acs.jmedchem.6b00140

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): DDR-TRK-1 is selective in KINOMEscan® at 1μM. The closest off target is CDK11 (370 nM), which was however shown to be only poorly inhibited in cells (~5 µM in NanoBRET).

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 5 Jun 2023 )