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DDR1-IN-1 | DDR1-IN-1 : Inhibitor of DDR1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

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Targets Biochemical/Biophysical Potency Cellular Potency
DDR1
  • IC50:105 nM
  • EC50:86 nM
Inhibitor
50 nM - 200 nM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - DDR2 413 nM

Potency Assay Off-Target:
KinomeScan binding assay revealed off-target activity against ABL, KIT and PDGFRbeta

Potency
Cellular
In Vitro

DDR1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

Orthogonal Probes def

BAY-826

Chemical Information

Molecular Formula C30H31F3N4O3
SMILEs CCN1CCN(Cc2ccc(C(=O)Nc3ccc(C)c(Oc4ccc5c(c4)CC(=O)N5)c3)cc2C(F)(F)F)CC1
InChI InChI=1S/C30H31F3N4O3/c1-3-36-10-12-37(13-11-36)18-21-6-5-20(15-25(21)30(31,32)33)29(39)34-23-7-4-19(2)27(17-23)40-24-8-9-26-22(14-24)16-28(38)35-26/h4-9,14-15,17H,3,10-13,16,18H2,1-2H3,(H,34,39)(H,35,38)
Molecular weight 552.23 Da
AlogP 4.0672
HBond acceptors 7
HBond donors 2
Atoms 71

Vendors

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Expert Reviews

by SERP
(on 19 Jun 2016)
Cellular Use Rating
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...
by SERP
(on 20 Jun 2016)
Cellular Use Rating
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,...
by SERP
(on 19 Nov 2020)
Cellular Use Rating
In Model Organisms
(The reviewer did not leave any public comments)
Note: The Chemical Probes Portal only endorses compounds as chemical probes for use as specific and selective modulators of the proposed target if they receive three or more (3-4) stars. Read more about our evaluation criteria