SGC-PIKFYVE-1

SGC-PIKFYVE-1 : Inhibitor of PIKFYVE

Structure

SERP Rating

In Cells

(1 ratings)

In Model Organisms

(0 ratings)

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Probe SGC-PIKFYVE-1 is in the process of SERP review.

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Information

PIKFYVE

Inhibitor

up to 1 uM

Additional Data

SGC Chemical Probe Collection

Probe Availability:

MedChemExpress

In Vitro Validations

Uniprot ID: Q9Y2I7

Target Class: Kinase

Target SubClass: Serine kinase

Potency: IC50

Potency Value: 6.9 nM

Potency Assay: Enzymatic assay (SignalChem)

PDB ID for probe-target interaction (3D structure): --

Target aliases:

1-phosphatidylinositol 3-phosphate 5-kinase, PIP5K ...

DOI Reference: 10.1021/acs.jmedchem.2c00697

In Cell Validations

In Vivo Data

No in Vivo Validations

Off-Target Selectivity Assesments

Potency assay (off target): SGC-PIKFYVE-1 was profiled in the KINOMEscan assay against 403 wild-type kinases at 1 μM. Only 8 kinases showed PoC <10 giving an S10(1 μM) = 0.02. When the PoC <35 fraction was examined, 20 kinases were included (S35(1 μM) = 0.05). Potential off-targets within the S35(1 μM) fraction as well as PIKfyve were tested using a NanoBRET target engagement assay and via biochemical enzymatic assays where an assay was available.

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SERP ratings and comments

SERP+ Ratings

In Cell Rating

SERP+ Comments:

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 three replicates.

(last updated: 23 Sept 2024 )