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ALW-II-49-7 | ALW-II-49-7: Type II inhibitor of DDR2, DDR1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
DDR2
  • IC50:18.6 nM
  • INH:1 µM
DDR1
  • IC50:12.4 nM
    Type II
    1 - 2 µM compound is effective and avoids off-target effects
    up to 5 uM

    Selectivity

    In Vitro Selectivity Assessment
    Potency Assay Off-Target:
    Profiled at a concentration of 1 μM against a diverse panel of 353 kinases by DiscoverX. Identified ...

    Potency
    Cellular
    In Vitro

    DDR2

    Mode of Action: Type II

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acschembio.5b00655

    DDR1

    Mode of Action: Type II

    Structure-Activity-Relationship data available? Yes

    DOI Reference: 10.1021/acschembio.5b00655

    Chemical Information

    Molecular Formula C21H17F3N4O2
    SMILEs Cc1ccc(C(=O)Nc2cccc(C(F)(F)F)c2)cc1Nc1cncc(C(N)=O)c1
    InChI InChI=1S/C21H17F3N4O2/c1-12-5-6-13(8-18(12)27-17-7-14(19(25)29)10-26-11-17)20(30)28-16-4-2-3-15(9-16)21(22,23)24/h2-11,27H,1H3,(H2,25,29)(H,28,30)
    Molecular weight 414.13 Da
    AlogP 4.503620000000002
    HBond acceptors 6
    HBond donors 4
    Atoms 47

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    Expert Reviews

    by SERP
    (on 17 May 2023 )
    Cellular Use Rating
    A useful inhibitor although has RAF1 as an off-target (IC50 = 22 nM). May have more off-targets based on the published kinome profiling data.
    by SERP+
    (on 17 Jun 2024 )
    Cellular Use Rating
    Compound ALW-II-49-7 (in the original publication as "compound 1") shows potent in vitro inhibition of DDR1, DDR2, RAF1 and LYN showing IC50s of 12.4 nM, 18.6 nM, 22 nM and 257 nM respectively. The selectivity...
    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