Chemical Probes logo
Filgotinib | Inhibitor of JAK1
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
JAK1
  • Kd:11 nM
  • IC50:10 nM
  • IC50:629 nM
Inhibitor
200 nM - 2 uM

Selectivity

In Vitro Selectivity Assessment

Potency: IC50 - JAK2 28 nM; TYK2 116 nM; JAK3 810 nM; FLT3: 338 nM, FLT4: 274 nM; CSF1R: 489 nM

Potency Assay Off-Target:
In a panel of 170 kinases at 1 uM, filgotinib had notable activity against the kinases listed below. ...
Selectivity Assessment Description:
In a panel containing 99 proteins (GPCRs, ion channels, transporters or non-kinase enzymes), no n ...
In Cell Selectivity Assessment

Potency: IC50 - JAK2: 17.4 uM

Potency Assay Off-Target:
In hERG patch clamp assay, IC50>100 uM

Potency
Cellular
In Vitro

JAK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.4049/jimmunol.1201348

In Vivo Validations

Rat
Dose: 1 mg/kg (IV); 5 mg/kg (oral)
Route of delivery: Intravenous, Oral
Plasma half life: 1.6 h (IV), 3.9 h (oral)
Systemic clearance: 1.35 L/h/kg (IV)

DOI Reference: 10.4049/jimmunol.1201348

Orthogonal Probes def

Baricitinib
Ruxolitinib

Chemical Information

Molecular Formula C21H23N5O3S
SMILEs O=C(Nc1nc2cccc(-c3ccc(CN4CCS(=O)(=O)CC4)cc3)n2n1)C1CC1
InChI InChI=1S/C21H23N5O3S/c27-20(17-8-9-17)23-21-22-19-3-1-2-18(26(19)24-21)16-6-4-15(5-7-16)14-25-10-12-30(28,29)13-11-25/h1-7,17H,8-14H2,(H,23,24,27)
Molecular weight 425.15 Da
AlogP 1.9751999999999998
HBond acceptors 8
HBond donors 1
Atoms 53

References

Publications

Cross References

Vendors

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

Expert Reviews

by SERP
(on 30 Mar 2017 )
Cellular Use Rating
In Model Organisms
Filgotinib is one of a number of JAK inhibitors available with varying selectivity within the JAK family and across other kinases. I recommend using more than one JAK inhibitor as a tool in cellular...
by SERP
(on 11 Apr 2017 )
Cellular Use Rating
In Model Organisms
The probe appears to show a significant degree of selectivity of JAK1 in cellular assays. I would hence recommend this compound as a fairly selective probe for JAK1 but not for the other kinases listed...
by SERP
(on 16 Jun 2017 )
Cellular Use Rating
In Model Organisms
Filgotinib is an orally available, selective JAK1 inhibitor and is one of the best JAK inhibitors at this moment. However, the in vitro selectivity index to JAK2 is only 2.8, and the results should...
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