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Roblitinib

Roblitinib : Reversible-Covalent Inhibitor of FGFR4

Structure

Information

  • FGFR4
  • Reversible-Covalent Inhibitor
  • up to 100 nM

In Vitro Validations

Uniprot ID: P22455
Target Class: Kinase
Target SubClass: TK
Potency: IC50
Potency Value: 0.9 ± 0.4 nM
Potency Assay: Biochemical Assay
PDB ID for probe-target interaction (3D structure): 6YI8
Structure-activity relationship: yes
Target aliases:
Fibroblast growth factor receptor 4, TKF, JTK2, FG ...

DOI Reference: 10.1021/acs.jmedchem.0c01019

Uniprot ID: P22455
Target Class: Kinase
Target SubClass: TK
Potency: Kd
Potency Value: 2.9 nM
Potency Assay: Biochemical Assay
PDB ID for probe-target interaction (3D structure): --
Target aliases:
Fibroblast growth factor receptor 4, TKF, JTK2, FG ...

DOI Reference: 10.1021/acs.jmedchem.0c01019

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): KINOMEscan
Probe Selectivity in Vitro:

1000-fold selectivity for FGFR4 compared to the next most potent kinase inhibited (Aurora A: IC50 5.6 μM), including no appreciable activity in both biochemical and cellular assays versus the other FGFR family members (@ 10 μM). A KINOMEscan with Roblitinib showed <35% displacement of the reporter binding against the whole panel of 456 off-target kinases @ 3 μM. Of the other GK+2 cysteine containing kinases, only MAPKAPK2 (MK2) showed any appreciable inhibition (biochemical IC50 = 9.4 μM) Outside target family: In enzyme and receptor screens, Roblitinib exhibited no appreciable activity at a concentration of 10 μM against 138 representative off-targets.

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SERP ratings and comments

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