NUAK1-In-10i |
NUAK1-In-10i : Inhibitor of NUAK1
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| NUAK1 |
|
|
Inhibitor
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
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