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LYS006 | Inhibitor of LTA4H
RATINGS:
Cellular Use: (0 reviews)

In Model Organisms: (0 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
LTA4H
  • IC50:0.12 nM
  • IC50:3.7 nM
  • IC50:53 nM
Inhibitor
up to 200 nM

Selectivity

In Vitro Selectivity Assessment
Selectivity Assessment Description:
LYS006 shows an exquisite selectivity profile when tested at concentrations of ≥10 μM in binding ...

Potency
Cellular
In Vitro

LTA4H

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/acs.jmedchem.0c01955

In Vivo Validations

Mouse, Rat, Dog
Dose: 0.1, 1, 3 (IV) mg/Kg, 0.3, 3, 10 (PO) mg/Kg
Route of delivery: Intravenous, Oral
Plasma half life: 16.7±5.3 (M), 169 (R), 48.8±4.3 (D) h
Systemic clearance: 4.2 (M), 0.66 (R), 0.94 (D) mL/min/Kg

DOI Reference: 10.1021/acs.jmedchem.0c01955

Negative Control Compounds

cpd 10

Chemical Information

Molecular Formula C16H14ClFN6O3
SMILEs N[C@@H](CC(=O)O)Cn1nnc(-c2ccc(Oc3ncc(Cl)cc3F)cc2)n1
InChI InChI=1S/C16H14ClFN6O3/c17-10-5-13(18)16(20-7-10)27-12-3-1-9(2-4-12)15-21-23-24(22-15)8-11(19)6-14(25)26/h1-5,7,11H,6,8,19H2,(H,25,26)/t11-/m0/s1
Molecular weight 392.08 Da
AlogP 0.0
HBond acceptors 9
HBond donors 3
Atoms 41

References

Publications

Cross References

canSARChEMBLBindingDBPDB

Vendors

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Expert Reviews

No SERP comments found for LYS006

Probe LYS006 is in the process of SERP review.

Please continue to check back for new reviews and commentary.