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FGFR4-IN-8B | FGFR4-IN-8B : Covalent Inhibitor of FGFR4
RATINGS:
Cellular Use: (2 reviews)

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

Targets Biochemical/Biophysical Potency Cellular Potency
FGFR4
  • IC50:0.5 nM
  • Ki:5.7 ± 0.17 nM
  • EC50:52 ± 7 nM
  • EC50:5 ± 4 nM
Covalent Inhibitor
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
8B was tested in the HotSpot format against all other FGFRs as well as MAPKAPK2, MAPKAPK3, S6K2, and ...

Potency
Cellular
In Vitro

FGFR4

Mode of Action: Covalent Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.3c02483

Negative Control Compounds

cpd 14A
Notes: 14A was inactive in both biochemical assay (IC50 >5000 nM) and in cellular NanoBRET (EC50 >2250 nM)
SMILES: COC1=CC(C2=CC3=CN=C(NC4=NC=CC=C4[N+]([O-])=O)N=C3C=C2)=CC(OC)=C1

Chemical Information

Molecular Formula C21H14Cl3N5O4
SMILEs COc1cc(OC)c(Cl)c(-c2ccc3nc(Nc4nc(Cl)ccc4[N+](=O)[O-])ncc3c2)c1Cl
InChI InChI=1S/C21H14Cl3N5O4/c1-32-14-8-15(33-2)19(24)17(18(14)23)10-3-4-12-11(7-10)9-25-21(26-12)28-20-13(29(30)31)5-6-16(22)27-20/h3-9H,1-2H3,(H,25,26,27,28)
Molecular weight 505.01 Da
AlogP 0.0
HBond acceptors 9
HBond donors 1
Atoms 47

References

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Expert Reviews

by SERP
(on 24 Jun 2024 )
Cellular Use Rating
( The reviewer did not leave any comments )
by SERP
(on 8 Jul 2024 )
Cellular Use Rating
FGFR4-IN-8B is a covalent inhibitor of FGFR4 kinase with minimal activity over FGFR1-3 isoforms that lack the reactive cysteine that the compound targets. Based on two separate kinome-screening methods,...
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