Chemical Probes logo
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
Download

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

Publications

Cross References

canSAR

Vendors

Note: This is not an exhaustive list and does not indicate endorsement by the portal.

Expert Reviews

by SERP
(on 24 Jun 2024)
Cellular Use Rating
(The reviewer did not leave any public 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