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Englerin-A | Agonist of TRPC4, TRPC5
RATINGS:
Cellular Use: (3 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
TRPC4
    • EC 50:11.2 nM
    TRPC5
      • EC 50:7.6 nM
      Agonist
      10-1,000 nM

      Selectivity

      In Vitro Selectivity Assessment
      Selectivity Assessment Description:
      Englerin A (1 µM) was assayed for inhibition of selected protein kinases (SelectScreen Kinase Profli ...
      In Cell Selectivity Assessment
      Potency Assay Off-Target:
      No (agonistic) activity of Englerin A was detected in HEK293 cells overexpressing TRPC6, TRPM2 or TR ...

      Potency
      Cellular
      In Vitro

      TRPC4

      Mode of Action: Agonist

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1002/anie.201411511

      TRPC5

      Mode of Action: Agonist

      Structure-Activity-Relationship data available? No

      DOI Reference: 10.1002/anie.201411511

      Negative Control Compounds

      (+)-englerin A

      Chemical Information

      Molecular Formula C26H34O6
      SMILEs CC(C)[C@@]12C[C@@H](OC(=O)CO)[C@@](C)(O1)[C@@H]1CC[C@@H](C)[C@H]1[C@@H]2OC(=O)/C=C/c1ccccc1
      InChI InChI=1S/C26H34O6/c1-16(2)26-14-20(30-22(29)15-27)25(4,32-26)19-12-10-17(3)23(19)24(26)31-21(28)13-11-18-8-6-5-7-9-18/h5-9,11,13,16-17,19-20,23-24,27H,10,12,14-15H2,1-4H3/b13-11+/t17-,19-,20-,23-,24+,25+,26-/m1/s1
      Molecular weight 442.24 Da
      AlogP 0.0
      HBond acceptors 6
      HBond donors 1
      Atoms 66

      References

      Publications

      Cross References

      canSARChEMBLBindingDB

      Vendors

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      Expert Reviews

      by SERP
      (on 10 Mar 2017 )
      Cellular Use Rating
      In Model Organisms
      Cytotoxicity was observed at 17 nM and 45 nM at different timepoints. Cell EC50s for TRPC4 and TRPC5 are 11 nM and 8 nM, respectively; therefore, there is an insufficient window between on-target activity...
      by SERP
      (on 20 Mar 2017 )
      Cellular Use Rating
      There have been several papers showing that this compound activates TRPC4/5 including doi: 10.1002/anie.201411511. The data in those papers is quite convincing that the compound at low nM concentrations...
      by SERP
      (on 26 Apr 2017 )
      Cellular Use Rating
      ( The reviewer did not leave any comments )
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