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HAMI3379 | HAMI3379 : Antagonist of CYSLTR2
RATINGS:
Cellular Use: (2 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
CYSLTR2
  • IC50:37.9 ± 14.7 nM
  • IC50:3.8-4.4 nM
  • INH:10 nM to 1 µM
Antagonist
CRITICAL TO STAY AT OR BELOW 100 nM
up to 100 nM

Selectivity

In Cell Selectivity Assessment
Potency Assay Off-Target:
HAMI3379 was added to both the CysLT1 and the CysLT2 receptor cell lines and did not induce any intr ...
In Vitro Selectivity Assessment
Potency Assay Off-Target:
HAMI3379 showed very low affinity to the CysLT1 receptor (IC50 > 30000 nM).

Potency
Cellular
In Vitro

CYSLTR2

Mode of Action: Antagonist

Structure-Activity-Relationship data available? No

DOI Reference: 10.1111/j.1476-5381.2010.00730.x

Orthogonal Probes def

ZAFIRLUKAST

Chemical Information

Molecular Formula C34H45NO8
SMILEs O=C(O)c1ccc(OCCCc2ccc(OCCCCOC3CCCCC3)cc2)c(C(=O)NC2CCCC(C(=O)O)C2)c1
InChI InChI=1S/C34H45NO8/c36-32(35-27-10-6-9-25(22-27)33(37)38)30-23-26(34(39)40)15-18-31(30)43-21-7-8-24-13-16-29(17-14-24)42-20-5-4-19-41-28-11-2-1-3-12-28/h13-18,23,25,27-28H,1-12,19-22H2,(H,35,36)(H,37,38)(H,39,40)
Molecular weight 595.31 Da
AlogP 6.2779
HBond acceptors 9
HBond donors 3
Atoms 88

References

Publications

Cross References

canSARChEMBLBindingDB

Vendors

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Expert Reviews

by SERP
(on 6 Dec 2022 )
Cellular Use Rating
HAMI3379 is a compound that antagonizes cysteinyl leukotriene 2 (CysLT2) receptor without affecting a closely related cysteinyl leukotriene 1 (CysLT1) receptor when used at concentrations < 100 nM. The...
by SERP
(on 7 Dec 2022 )
Cellular Use Rating
This interesting compound could be used with greater confidence as an antagonist of CysLT2 if more selectivity data were provided
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