| serine/threonine protein kinase, putative44 (CLK3) |
PF3D7_1114700 |
can target
be structurally enabled? |
optimization of hits; more
chemical starting points |
| cGMP-dependent protein
kinase (PKG) |
PF3D7_1436600 |
rate of kill
with selective inhibitor |
Rate of kill (PRR assay); optimize
chemical starting points |
| geranylgeranyl pyrophosphate
synthase (F/GGPPS) |
Pf3D7_1128400 |
small
molecule inhibitors |
generate additional chemical matter |
| phenylalanine tRNA synthetase–alpha subunit
(PheRS) |
PF3D7_0109800 |
resistance risk |
more screening/scaffold hopping to identify more start points |
| prolyl tRNA synthetase, putative (ProRS) |
PF3D7_0925300 |
is selectivity versus human orthologues
possible? |
additional screens |
| acetyl CoA synthetase, putative (AcAS) |
PF3D7_0627800 |
resistance risk; can the target be structurally enabled? |
proof of concept from MMV693183 first-in-human study; establish
alternate lead series from existing hits/new screens and H2L; crystal
structure to guide chemistry program |
| isoleucine—tRNA
ligase, putative (cIRS) |
PF3D7_1332900 |
rate of kill, resistance risk |
generate additional chemical
matter |
