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14th August 2014 @ 21:58

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)

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Attached Files
BQ_20120404_arylpyrrol_IC50s_DHODH_results_N5441-96.xlsx
BQ_20130718_Report Arylpyrrole series_DHODH.pdf