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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

      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 public comments)
      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