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Biological Data currently not incorporated into the main Wiki sections

Mat Todd edited this page Jan 25, 2022 · 56 revisions

Once new biological data has been received on new compounds, the data will be put here in the interim before it is incorporated into the relevant main Wiki section.

2019 July Dundee Potency and the File Mirror on Github

July 2019 Metabolic/Physchem Data from Monash

June 2018 Monash Data (don't think it's on wiki)

April 2018 hERG Data from VCI

May 2018 Metabolic/Physchem Data from Monash

Feb 2017 Metabolic/Physchem Data from Monash

Done

Below this line are biological evaluations that have been installed on the wiki, and are listed as such in the section on Sources of Data

2014 June GSK Single Shot Potencies plus July analysis of the actives and the File Mirror on Github

2014 hERG data (figure in terms of IC50 or pIC50) file mirror

2014 Syngene Potency Received (Nov) and Sent (Sept) file mirror

2015 Nov Syngene Potency and the File Mirror on Github

2016 Jun Syngene Potency (sent May 2016) File Mirror on Github

2016 Nov Dundee Potency and the File Mirror on Github

2017 Jul Dundee Potency and the File Mirror on Github

2017 Oct Dundee Potency and the File Mirror on Github

2017 Dec Dundee Potency and the File Mirror on Github

2018 Feb Dundee Potency and the File Mirror on Github

2018 Apr Dundee Potency and the File Mirror on Github

2018 Jun Dundee Potency and the File Mirror on Github

Background

What is OSM Series 4?

Aims, Concerns and Current Interest in Series 4

Sources of Data

Structure-Activity Relationships

Modification of Core Triazolopyrazine

Modification of Pyrazine Substitution Pattern

Modification of the Triazole Substitution

Pyrazine Side Chain Modifications - Ethers

Pyrazine Side Chain Modifications - Amides

Pyrazine Side Chain Modifications - Reversed Amides

Pyrazine Side Chain Modifications - Others

Metabolites

Biological Data Currently not Incorporated into the Main Wiki Sections

Physicochemical/Metabolic Parameters

Physicochem/metabolism/PK

Metabolism ID

Aldehyde Oxidase Assay

Stages and Efficacy

Liver Stage

Gametocyte Stage

In Vivo Efficacy

Potency vs. Resistant Strains

Other Observations

Mechanism of Action, Activity and Toxicity

Mechanism of Action: Possible PfATP4 Activity Deduced from Parasite Ion Regulation Assays

hERG Activity

Toxicity

Synthetic Chemistry

Synthetic Design

Synthesis of the Ether-Linked Series

Synthesis of the Amide-Linked Series

Synthesis of the Reverse Amide- Linked Series

Synthesis of Benzylic Functionalised Ether-Linked Series

Alternative Routes to the Triazolopyrazine Core

Triazolopyrazine telesubstitution

Biofunctionalisation

Late Stage Functionalisation

Fluoroalkene Isostere

Spectroscopy

Chirality, Relevant and Desirable Compounds

Chirality/Stereogenic Centres in This Series

Other Sources of Compounds Relevant to this Series

Desirable Compounds Not Yet Synthesised

Other Evaluations

Evaluations vs Other Organisms

Strings

Strings for Google

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