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ZIMLOVISERTIB | ZIMLOVISERTIB : Inhibitor of IRAK4
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (1 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
IRAK4
  • IC50:0.2 ± 0.1 nM
  • IC50:2.4 ± 1.9 nM
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
The kinome selectivity profile of ZIMLOVISERTIB was assessed in a panel of 278 kinases (Invitrogen) ...
In Cell Selectivity Assessment
Potency Assay Off-Target:
KiNativ kinome screen (ActivX) in THP1 cell lysates at concentrations of 10, 50, 200, 1000, and 5000 ...

Potency
Cellular
In Vitro

IRAK4

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.7b00231

In Vivo Validations

Rat
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 0.6 h
Systemic clearance: 56 mL/min/kg
Volume of Distribution at Steady-State: 1.8 L/Kg

DOI Reference: 10.1021/acs.jmedchem.7b00231

Dose: 5 mg/Kg
Route of delivery: Oral
Plasma half life: 1.4–2.1 h
Bioavailability: 34–50%

DOI Reference: 10.1021/acs.jmedchem.7b00231

Dog
Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.1 h
Systemic clearance: 10 mL/min/kg
Volume of Distribution at Steady-State: 0.77 L/Kg

DOI Reference: 10.1021/acs.jmedchem.7b00231

Dose: 5 mg/Kg
Route of delivery: Oral
Plasma half life: 4.0 h
Bioavailability: 41%

DOI Reference: 10.1021/acs.jmedchem.7b00231

Dose: 1 mg/Kg
Route of delivery: Intravenous
Plasma half life: 1.7 h
Systemic clearance: 10 mL/min/kg
Volume of Distribution at Steady-State: 0.95 L/Kg

DOI Reference: 10.1021/acs.jmedchem.7b00231

Dose: 5 mg/Kg
Route of delivery: Oral
Plasma half life: 6.2 h
Bioavailability: 6.9 %

DOI Reference: 10.1021/acs.jmedchem.7b00231

Negative Control Compounds

CANSAR1682746
Notes: Biochemical IC50 29 nM, In Cell IC50 2836 nM

Orthogonal Probes def

FJ0

Chemical Information

Molecular Formula C18H20FN3O4
SMILEs CC[C@H]1[C@@H](COc2nccc3cc(C(N)=O)c(OC)cc23)NC(=O)[C@H]1F
InChI InChI=1S/C18H20FN3O4/c1-3-10-13(22-17(24)15(10)19)8-26-18-11-7-14(25-2)12(16(20)23)6-9(11)4-5-21-18/h4-7,10,13,15H,3,8H2,1-2H3,(H2,20,23)(H,22,24)/t10-,13+,15-/m0/s1
Molecular weight 361.14 Da
AlogP 1.5837999999999994
HBond acceptors 7
HBond donors 3
Atoms 46

References

Publications

Cross References

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Expert Reviews

by SERP+
(on 22 Mar 2023 )
Cellular Use Rating
In Model Organisms
ZIMLOVISERTIB showed promising in vivo results in monkeys, dogs and rats.
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