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FIBOFLAPON | FIBOFLAPON : Inhibitor of ALOX5AP
RATINGS:
Cellular Use: (3 reviews)

In Model Organisms: (3 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
ALOX5AP
  • IC50:2.9 ± 1.0 nM
  • IC50:0.7 ± 03 nM
  • IC50:76 ± 15 nM (5h)
Inhibitor
up to 100 nM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
AM803 had no COX-1 cross-reactivity and showed very little activity toward other enzymes in the leuk ...

Potency
Cellular
In Vitro

ALOX5AP

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? No

DOI Reference: 10.1021/jm2008369

In Vivo Validations

Rat
Dose: 2 mg/Kg IV, 10 mg/Kg PO
Route of delivery: Intravenous, Oral
Plasma half life: 2.0 h IV
Systemic clearance: 8.0 mK/min/Kg
Cmax: 12.2 uM
Area Under the Curve:: 26 h*ug/mL
Bioavailability: 100%
Volume of Distribution at Steady-State: 0.70 L/Kg

DOI Reference: 10.1021/jm2008369

Chemical Information

Molecular Formula C38H43N3O4S
SMILEs CCOc1ccc(-c2ccc(Cn3c(CC(C)(C)C(=O)O)c(SC(C)(C)C)c4cc(OCc5ccc(C)cn5)ccc43)cc2)cn1
InChI InChI=1S/C38H43N3O4S/c1-8-44-34-18-14-28(22-40-34)27-12-10-26(11-13-27)23-41-32-17-16-30(45-24-29-15-9-25(2)21-39-29)19-31(32)35(46-37(3,4)5)33(41)20-38(6,7)36(42)43/h9-19,21-22H,8,20,23-24H2,1-7H3,(H,42,43)
Molecular weight 637.30 Da
AlogP 8.97662
HBond acceptors 7
HBond donors 1
Atoms 89

References

Publications

Cross References

canSARChEMBLBindingDBBindingDB

Vendors

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Expert Reviews

by SERP
(on 4 Nov 2023 )
Cellular Use Rating
In Model Organisms
( The reviewer did not leave any comments )
by SERP
(on 23 Nov 2023 )
Cellular Use Rating
In Model Organisms
Although Fiboflapon does not inhibit any of the major human CYP isoforms or the COX enzymes, wider profiling is lacking. There may thus be off-targets that limit the selectivity of the probe. The use of...
by SERP
(on 10 Dec 2023 )
Cellular Use Rating
In Model Organisms
The compounds is an inhibitor of FLAP (5-lipoxygenase-activating protein) and thereby indirectly inhibits 5-LO. Synonyms: 936350-00-4, GSK2190915, AM-803, AM803
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