Literature summary for 2.5.1.60 extracted from

Kazmierczak, A.; Kusy, D.; Niinivehmas, S.P.; Gmach, J.; Joachimiak, L.; Pentikaeinen, O.T.; Gendaszewska-Darmach, E.; Blazewska, K.M.
Identification of the privileged position in the imidazo[1,2-a]pyridine ring of phosphonocarboxylates for development of Rab geranylgeranyl transferase (RGGT) inhibitors (2017), J. Med. Chem., 60, 8781-8800 .

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Inhibitors

Inhibitors	Comment	Organism	Structure
2-fluoro-3-(6-methylimidazo[1,2-a]pyridin-3-yl)-2-phosphonopropanoic acid	compound is an micromolar inhibitor of Rab11A prenylation, is inactive against Rap1A/Rap1B modification, and able to inhibit proliferation of HeLa cell line with IC50 value of 0.36 mM	Homo sapiens
2-fluoro-3-(6-phenylimidazo[1,2-a]pyridin-3-yl)-2-phosphonopropanoic acid	compound is an micromolar inhibitor of Rab11A prenylation, is inactive against Rap1A/Rap1B modification, and able to inhibit proliferation of HeLa cell line with IC50 value of 0.51 mM	Homo sapiens
3-(6-bromoimidazo[1,2-a]pyridin-3-yl)-2-fluoro-2-phosphonopropanoic acid	compound is an micromolar inhibitor of Rab11A prenylation, is inactive against Rap1A/Rap1B modification, and able to inhibit proliferation of HeLa cell line with IC50 value of 0.50 mM	Homo sapiens
3-(6-chloroimidazo[1,2-a]pyridin-3-yl)-2-fluoro-2-phosphonopropanoic acid	compound is an micromolar inhibitor of Rab11A prenylation, is inactive against Rap1A/Rap1B modification, and able to inhibit proliferation of HeLa cell line with IC50 value of 0.52 mM	Homo sapiens

Organism

Organism	UniProt	Comment	Textmining
Homo sapiens	P24386	-	-

Source Tissue

Source Tissue	Comment	Organism	Textmining
HeLa cell	-	Homo sapiens	-

Synonyms

Synonyms	Comment	Organism
Chm	-	Homo sapiens
Rab proteins geranylgeranyltransferase component A 1	-	Homo sapiens
Rab11a	-	Homo sapiens

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Release 2023.1 (January 2023)