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Inhibition of human recombinant Vps34 using substrate PI incubated for 1 hr by Adapta kinase assay

PubChem AID
1321995
Primary Citation
Class II Phosphoinositide 3-Kinases as Novel Drug Targets [PMID: 27644332]
Source
External ID
BioAssay Type
Confirmatory
Tested Substances
Tested Compounds
Version
Status
Live
Dates
  • Deposit:
    2018-09-07
  • Modify:
    2022-08-30
Description
This bioassay record (AID 1321995) reports results from the above primary citation. Additional data from the same publication are reported in a total of 34 BioAssay records in PubChem.

1 Description

Title: Class II Phosphoinositide 3-Kinases as Novel Drug Targets.

Abstract: The phosphoinositide 3-kinases (PI3Ks) are a family of lipid kinases central to regulating a wide range of important intracellular processes. Despite the vast knowledge around class I PI3Ks, the class II PI3Ks have been neglected, seemingly only due to the chronology of their discovery. Here we focus on the cellular functions of the three class II PI3K isoforms, PI3KC2α, PI3KC2β, and PI3KC2γ, in different cell systems and underline the emerging importance of these enzymes in different physiological and pathological contexts. We provide an overview on the current development of class II PI3 kinase inhibitors and outline the potential use for such inhibitors. The field is in its infancy as compared to their class I counterparts. Nevertheless, recent advances in understanding the roles of class II PI3 kinases in different pathological contexts is leading to an increased interest in the development of specific inhibitors that can provide potential novel pharmacological tools.

2 Comment

Compounds with activity <= 10uM or explicitly reported as active by ChEMBL are flagged as active in this PubChem assay presentation.

Journal: J Med Chem

Year: 2017

Volume: 60

Issue: 1

First Page: 47

Last Page: 65

DOI: 10.1021/acs.jmedchem.6b00963

Target ChEMBL ID: CHEMBL1075165

ChEMBL Target Name: Phosphatidylinositol 3-kinase catalytic subunit type 3

ChEMBL Target Type: SINGLE PROTEIN - Target is a single protein chain

Relationship Type: D - Direct protein target assigned

Confidence: Direct single protein target assigned

3 Result Definitions

4 Data Table

5 Target

8 Identity

8.1 BioAssay Name

Inhibition of human recombinant Vps34 using substrate PI incubated for 1 hr by Adapta kinase assay

8.2 Source

8.3 External ID

8.4 Project Category

Literature, Extracted

8.5 BioAssay Type

Confirmatory

8.6 Deposit Date

2018-09-07

8.7 Modify Date

Version 1.1
Version 1.2
Version 1.3
2022-08-30 (currently shown)

8.8 Status

Live

9 Same-Publication BioAssays

10 BioAssay Annotations

Assay Type
Binding
Assay Organism

11 Information Sources

  1. PubChem
  2. ChEMBL
    LICENSE
    Access to the web interface of ChEMBL is made under the EBI's Terms of Use (http://www.ebi.ac.uk/Information/termsofuse.html). The ChEMBL data is made available on a Creative Commons Attribution-Share Alike 3.0 Unported License (http://creativecommons.org/licenses/by-sa/3.0/).
    http://www.ebi.ac.uk/Information/termsofuse.html
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