DDR1-IN-1 : Inhibitor of DDR1



  • DDR1
  • Inhibitor
  • 50 nM - 200 nM

In Vitro Validations

Uniprot ID: Q08345
Target Class: Protein kinase
Target SubClass: TK
Potency: IC50
Potency Value: 105 nM
Potency Assay: Lanthascreen
PDB ID for probe-target interaction (3D structure): 4CKR
Target aliases:
Epithelial discoidin domain-containing receptor 1, ...

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency end-point : IC50 DDR2 413 nM
Potency assay (off target): KinomeScan binding assay revealed off-target activity against ABL, KIT and PDGFRbeta
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SERP ratings and comments

SERP Ratings

In Cell Rating

SERP Comments:

DDR1-IN-1 has modest biochemical selectivity (4X) for DDR1 over DDR2, but shows excellent broader selectivity across the KinomeScan panel when tested at 1 uM (S(1) at 1 uM of 0.01). DDR1-IN-1 demonstrates only weak cellular potency (no antiproliferative effects at concentrations of <10 uM), and it is not clear if this is a limitation of the compound or reflective of the target biology. Positive combination effects are seen with other kinase inhibitors, such as GSK2126458 (a PI3K/mTOR inhibitor), implying that the compound is capable of engaging its target in cells. For now, DDR1-IN-1 appears to be an acceptable probe for DDR1-dependent signal transduction.

(last updated: 19 Jun 2016 )

SERP Ratings

In Cell Rating

SERP Comments:

DDR1-IN-1 is selective across 451 kinases with selectivity score (S(1) at 1 uM) of 0.01, as assessed with the KinomeScan approach. It is more effective in combination with inhibitors against EGFR, SRC, CDK1, mTOR and PI3K, for example with GSK212458. The PK profile is modest with t1/2 = 2.76 hrs; CL = 89.88 (mL/min/kg); Vss = 18.02; and F = 26%. The compound is commercially available and accessible synthetically through a four step synthesis. X-ray crystal structure shows DDR1-IN-1 bound to DDR1 in the hinge binding area.

(last updated: 20 Jun 2016 )

SERP Ratings

In Cell Rating
In Model Organisms

(last updated: 19 Nov 2020 )