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SGC-PIKFYVE-1 | SGC-PIKFYVE-1 : Inhibitor of PIKFYVE
RATINGS:
Cellular Use: (1 reviews)

In Model Organisms: (0 reviews)
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
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Probe Summary

Targets Biochemical/Biophysical Potency Cellular Potency
PIKFYVE
  • IC50:6.9 nM
  • IC50:4.0 nM
up to 1 uM

Selectivity

In Vitro Selectivity Assessment
Potency Assay Off-Target:
SGC-PIKFYVE-1 was profiled in the KINOMEscan assay against 403 wild-type kinases at 1 μM. Only 8 kin ...

Potency
Cellular
In Vitro

PIKFYVE

Mode of Action: Inhibitor

Structure-Activity-Relationship data available? Yes

DOI Reference: 10.1021/acs.jmedchem.2c00697

Negative Control Compounds

SGC-PIKFYVE-1N
Notes: SGC-PIKFYVE-1N was profiled in the KINOMEscan assay against 403 wild-type kinases at 1 μM and a follow-up PIKfyve enzymatic assay was done to confirm no activity.
SMILES: NC1=NC2=C(CCCCC3=C2C4=C(C=CC(C5CC5)=C4)N3)C=N1

Chemical Information

Molecular Formula C20H21N5
SMILEs CN(C)CC#Cc1ccc2[nH]c3c(c2c1)-c1nc(N)ncc1CCC3
InChI InChI=1S/C20H21N5/c1-25(2)10-4-5-13-8-9-16-15(11-13)18-17(23-16)7-3-6-14-12-22-20(21)24-19(14)18/h8-9,11-12,23H,3,6-7,10H2,1-2H3,(H2,21,22,24)
Molecular weight 331.18 Da
AlogP 2.608900000000001
HBond acceptors 5
HBond donors 3
Atoms 46

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Expert Reviews

by SERP+
(on 23 Sept 2024)
Cellular Use Rating
As a kinase inhibitor, the compound fulfils the requirements. There is a dip in the data for cell toxicity for the active compound 30 (supplement S3) which might be the result of one outlier within the...
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