Biological Evaluation of Compounds

The following compounds have been evaluated by Kiaran Kirk and Adele Lehane in their ion regulation assay, and will now be evaluated vs ATP4-resistant mutants in Kiaran's lab. The same samples are being sent to David Fidock's lab at Columbia to testing vs his ATP4 resistant mutants, for comparison. Compounds being shipped 28th August 2014. Results will be posted to this lab notebook when obtained.

An assay was performed on several Series 1 compounds in July 2013 by GSK to determine activity vs P. falciparum Dihydroorotate dehydrogenase (DHODH). Assay carried out by María José Lafuente. Reports/Data attached.

Compounds tested:

PMY 12-5 OSM-S-8 Preparation of OSM-S-8

PMY 27-2 OSM-S-16 Preparation of OSM-S-16

PMY 31-5 OSM-S-19 Preparation of OSM-S-19

PMY 34-1 OSM-S-21 Preparation of OSM-S-21

ZYH 3-1 OSM-S-35 Preparation of OSM-S-35

ZYH 5-1 OSM-S-37 Preparation of OSM-S-37

ZYH 6-1/6-2 OSM-S-38 Preparation of OSM-S-38

ZYH 7-2 OSM-S-39 Preparation of OSM-S-39

ZYH 10-2 A OSM-S-42 Preparation of OSM-S-42

ZYH 10-2 B OSM-S-43 Preparation of OSM-S-43

ZYH 12-1/12-2 OSM-S-45 Preparation of OSM-S-45

ZYH 15-1 OSM-S-48 Preparation of OSM-S-48
ZYH 16-1 OSM-S-49 Preparation of OSM-S-49
ZYH 17-1 OSM-S-50 Preparation of OSM-S-50
ZYH 18-1 OSM-S-51 Preparation of OSM-S-51
ZYH 19-1 OSM-S-52 Preparation of OSM-S-52
ZYH 22-3 OSM-S-54 Preparation of OSM-S-54
ZYH 23-1 OSM-S-55 Preparation of OSM-S-55

PMY12-1 OSM-S-7 Preparation of OSM-S-7
PMY 2-4 OSM-S-2 Preparation of OSM-S-2
PMY 6-1 OSM-S-3 Preparation of OSM-S-3
PMY 8-2 OSM-S-4 Preparation of OSM-S-4
PMY 11-2 (TCMDC-123794) OSM-S-6 Preparation of OSM-S-6

PMY 10-2 (TCMDC-123812) OSM-S-5 Preparation of OSM-S-5

PMY 14-1 OSM-S-9 Preparation of OSM-S-9

Result: No activity

(This post authored by Mat Todd)