Chemical Probes logo
NUAK1-In-10i | NUAK1-In-10i : Inhibitor of NUAK1
RATINGS:
Cellular Use: (2 reviews)

In Model Organisms: (2 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
Download

Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
NUAK1
  • IC50:0.49 nM
  • Inhibition:75%
  • INH:5 µM
up to 10 µM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
Cpd 10i activity was profiled against a panel of 416 human kinases via the ADP-Glo or HTRF assay @ 1 ...
Selectivity Assessment Description:
Only nine wild-type kinases were inhibited >90% by cpd 10i, namely PDGFRβ, TNK1, RET, NUAK1, KDR, QI ...

Potency
Cellular
In Vitro

NUAK1

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.5c03079

In Vivo Validations

Mouse
Dose: 2 mg/Kg
Route of delivery: Intravenous
Plasma half life: 0.85 h
Systemic clearance: 161 mL/min/kg
Cmax: 581 ng/mL
Tmax: 0.03 h
Area Under the Curve:: 204 h*ng/mL
Volume of Distribution at Steady-State: 6.20 L/kg

DOI Reference: 10.1021/acs.jmedchem.5c03079

Dose: 6 mg/Kg
Route of delivery: Oral
Plasma half life: 1.69 h
Cmax: 45.6 ng/mL
Tmax: 0.08 h
Area Under the Curve:: 96.6 h*ng/mL
Bioavailability: 16.6%

DOI Reference: 10.1021/acs.jmedchem.5c03079

Dose: 60 mg/Kg
Route of delivery: Oral
Plasma half life: 1.21 h
Cmax: 809 ng/mL
Tmax: 0.194 h
Area Under the Curve:: 768 h*ng/mL
Bioavailability: 12.6%

DOI Reference: 10.1021/acs.jmedchem.5c03079

Dose: 60 mg/Kg
Route of delivery: Intraperitoneal
Plasma half life: 0.773 h
Cmax: 7177 ng/mL
Tmax: 0.194 h
Area Under the Curve:: 5947 h*ng/mL
Bioavailability: 95.9%

DOI Reference: 10.1021/acs.jmedchem.5c03079

Chemical Information

Molecular Formula C30H35ClFN7O6
SMILEs CO[C@@H]1CO[C@H]2[C@@H]1OC[C@H]2Oc1nc(Nc2ccc(OC[C@@]34CCCN3C[C@H](F)C4)c(NC(=O)c3cnn(C)c3)c2)ncc1Cl
InChI InChI=1S/C30H35ClFN7O6/c1-38-12-17(10-34-38)27(40)36-21-8-19(4-5-22(21)44-16-30-6-3-7-39(30)13-18(32)9-30)35-29-33-11-20(31)28(37-29)45-24-15-43-25-23(41-2)14-42-26(24)25/h4-5,8,10-12,18,23-26H,3,6-7,9,13-16H2,1-2H3,(H,36,40)(H,33,35,37)/t18-,23-,24-,25-,26-,30+/m1/s1
Molecular weight 643.23 Da
AlogP 3.374600000000001
HBond acceptors 13
HBond donors 2
Atoms 80

References

Publications

Cross References

canSAR: 7719222 PubChem: 179077308

Expert Reviews

by SERP
(on 8 Apr 2026)
Cellular Use Rating
In Model Organisms
There are not a lot of selective NUAK1 inhibitors out there, many based on pan kinase scaffolds. This compound is one of the best options available, still a long way to go. together with: https://pubs.acs.org/doi/pdf/10.1021/acs.jmedchem.4c01237?ref=article_openPDF,...
by SERP
(on 20 Apr 2026)
Cellular Use Rating
In Model Organisms
In summary, 5–10 µM of this proposed NUAK1 chemical probe is likely too high to be reliable for clean biology. My concerns are (1) The selectivity panel (see supplemental) at 1 µM already shows substantial...
If you would like to explore AI-generated evaluations, you may wish to visit the page for this compound on our collaborator website
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