Page last updated: 2024-11-12

ne 10790

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Cross-References

ID SourceID
PubMed CID10014835
CHEMBL ID397829
SCHEMBL ID4893738
MeSH IDM0527272

Synonyms (34)

Synonym
gtpl3165
(r)-2-hydroxy-2-phosphono-3-(pyridin-3-yl)propanoic acid
3-(3-pyridyl)-2-hydroxy-2-phosphonopropanoic acid
2-hydroxy-2-phosphono-3-(pyridin-3-yl)propanoic acid ,
bdbm50226002
CHEMBL397829 ,
ne10790 ,
3-pehpc
ne-10790
ne 10790
SCHEMBL4893738
152831-36-2
2-hydroxy-2-phosphono-3-(3-pyridyl)propionic acid
2-hydroxy-2-phosphono-3-pyridin-3-ylpropanoic acid
CS-0006102
HY-16011
Q27087880
2-hydroxy-2-phosphono-3-pyridin-3-yl-propionic acid
ne 10790 (3-pehpc)
mfcd20233001
3-pyridinepropanoic acid, .alpha.-hydroxy-.alpha.-phosphono-
.alpha.-hydroxy-.alpha.-phosphono-3-pyridinepropanoic acid
D81226
3-pehpc3-pehpc
EX-A3623
3-pyridinepropanoic acid, alpha-hydroxy-alpha-phosphono-
3pehpc
unii-nr6e47e4wn
alpha-hydroxy-alpha-phosphono-3-pyridinepropanoic acid
NR6E47E4WN ,
BN178035
DTXSID001249251
GLXC-25731
AKOS040742281
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (2)

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Farnesyl pyrophosphate synthaseHomo sapiens (human)IC50 (µMol)434.90000.00020.71099.3600AID1204206; AID303799; AID318593; AID318594; AID480313
Farnesyl pyrophosphate synthaseHomo sapiens (human)Ki79.25000.00010.21651.9000AID318593; AID318594
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (6)

Processvia Protein(s)Taxonomy
cholesterol biosynthetic processFarnesyl pyrophosphate synthaseHomo sapiens (human)
geranyl diphosphate biosynthetic processFarnesyl pyrophosphate synthaseHomo sapiens (human)
farnesyl diphosphate biosynthetic processFarnesyl pyrophosphate synthaseHomo sapiens (human)
visual perceptionGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
protein geranylgeranylationGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
protein modification processGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (8)

Processvia Protein(s)Taxonomy
RNA bindingFarnesyl pyrophosphate synthaseHomo sapiens (human)
protein bindingFarnesyl pyrophosphate synthaseHomo sapiens (human)
metal ion bindingFarnesyl pyrophosphate synthaseHomo sapiens (human)
dimethylallyltranstransferase activityFarnesyl pyrophosphate synthaseHomo sapiens (human)
geranyltranstransferase activityFarnesyl pyrophosphate synthaseHomo sapiens (human)
Rab geranylgeranyltransferase activityGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
protein bindingGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
zinc ion bindingGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
small GTPase bindingGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
Rab geranylgeranyltransferase activityGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
nucleoplasmFarnesyl pyrophosphate synthaseHomo sapiens (human)
cytosolFarnesyl pyrophosphate synthaseHomo sapiens (human)
cytoplasmFarnesyl pyrophosphate synthaseHomo sapiens (human)
cytosolGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
plasma membraneGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
Rab-protein geranylgeranyltransferase complexGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
cytoplasmGeranylgeranyl transferase type-2 subunit alphaHomo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (35)

Assay IDTitleYearJournalArticle
AID480326Inhibition of rabbit osteoclast rab11 prenylation after 24 hrs by Western blot analysis2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID480315Inhibition of recombinant RGGT assessed as incorporation of [3H]GGPP into His-tagged canine rab1a after 30 mins2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID480323Inhibition of recombinant RGGT by uncompetitive inhibition based Lineweaver-Burke plot using Rab1a as substrate2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID480322Inhibition of GGTase1 assessed as incorporation of [3H]GGPP into His-tagged canine rab1a after 30 mins2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID303803Inhibition of RGGT mediated Rab11 prenylation in J744 cells2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.
AID318595Inhibition of bone resorption in rat assessed as phosphate2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.
AID1204209Inhibition of GGTase 2 in human RPMI8226 cells assessed as reduction in membrane bound Rab6 protein at 5 mM incubated for 48 hrs by immunoblot method2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.
AID1121273Inhibition of rat RabGGTase using [3H]GGPP by scintillation counting2013MedChemComm, Mar, Volume: 4, Issue:3
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.
AID480313Inhibition of human FPPS after 10 mins using [14C]IPP as substrate by liquid scintillation counting2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID480314Cytotoxicity against mouse J774 cells assessed as cell viability after 48 hrs by alamar blue assay2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID1121272Inhibition of human RabGGTase using [3H]GGPP by scintillation counting2013MedChemComm, Mar, Volume: 4, Issue:3
Prenyltransferase Inhibitors: Treating Human Ailments from Cancer to Parasitic Infections.
AID1204205Inhibition of GGTase 2 (unknown origin)2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.
AID480320Inhibition of RGGT-mediated Rap1A prenylation in mouse J774 cells at 2 mM after 24 hrs by Western blot analysis2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID1204214Induction of endoplasmic reticulum stress in human RPMI8226 cells assessed as increase in calnexin cleavage at 5 mM incubated for 48 hrs by immunoblot method2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.
AID303799Inhibition of human cloned FPPS expressed in Escherichia col BL2 (DE3)2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.
AID480317Inhibition of RGGT-mediated Rab11 prenylation in mouse J774 cells after 24 hrs by Western blot analysis2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID480327Antiresorptive activity in rabbit osteoclasts assessed as number of actin rings after 48 hrs using TRITC-phelloidin stain relative to control2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID1204208Inhibition of GGTase 1 in human RPMI8226 cells assessed as unmodified Rap1a accumulation at 5 mM incubated for 48 hrs by immunoblot method2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.
AID318593Inhibition of human recombinant FPPS expressed in Escherichia coli BL212008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.
AID303798Bone mineral affinity on hydroxyaptite assessed as retention time by chromatography2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.
AID318594Inhibition of human recombinant FPPS expressed in Escherichia coli BL21 after 10 mins2008Journal of medicinal chemistry, Apr-10, Volume: 51, Issue:7
Structure-activity relationships among the nitrogen containing bisphosphonates in clinical use and other analogues: time-dependent inhibition of human farnesyl pyrophosphate synthase.
AID480316Inhibition of recombinant RGGT assessed as incorporation of [3H]GGPP into His-tagged canine rab1a after 20 mins2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID1204207Inhibition of recombinant GGTase 2 (unknown origin) using recombinant Rab1A and [3H]GGPP as substrate after 20 mins in presence of recombinant REP-2 by liquid scintillation counting analysis2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.
AID471506Inhibition of recombinant Rab geranylgeranyltransferase expressed in human MCF7 cells assessed as inhibition of geranylgeranylation of EYFP-Rab7 protein at 100 uM to 0.5 mM by Western blot relative to compactin2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
Design, synthesis, and characterization of peptide-based rab geranylgeranyl transferase inhibitors.
AID303802Inhibition of RGGT2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.
AID1204215Inhibition of GGTase 2 in human RPMI8226 cells assessed as disruption of monoclonal protein trafficking by measuring accumulation of intracellular lambda light chain at 5 mM incubated for 48 hrs by ELISA2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.
AID480319Inhibition of RGGT-mediated Rap1A prenylation in mouse J774 cells at 4 mM after 24 hrs by Western blot analysis2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID480329Inhibition of human FPPS at 10 uM after 10 mins using [14C]IPP as substrate2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID1204206Inhibition of recombinant FDPS (unknown origin) assessed as decrease in radiolabeld GGPP level using GPP and [14C]IPP as substrate treated with enzyme for 10 mins prior to substrate challenge for 30 mins by liquid scintillation counting analysis2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.
AID1204212Induction of apoptosis in human RPMI8226 cells assessed as increase in PARP cleavage at 5 mM incubated for 48 hrs by immunoblot method2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.
AID480321Inhibition of GGPPS after 10 mins using [14C]IPP as substrate by liquid scintillation counting2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID1204213Induction of apoptosis in human RPMI8226 cells assessed as increase in caspase-3 cleavage at 5 mM incubated for 48 hrs by immunoblot method2015Bioorganic & medicinal chemistry letters, Jun-01, Volume: 25, Issue:11
N-Oxide derivatives of 3-(3-pyridyl)-2-phosphonopropanoic acids as potential inhibitors of Rab geranylgeranylation.
AID480328Antiresorptive activity in Schenk growing rat model assessed as inhibition of bone resorption2010Journal of medicinal chemistry, May-13, Volume: 53, Issue:9
Synthesis, chiral high performance liquid chromatographic resolution and enantiospecific activity of a potent new geranylgeranyl transferase inhibitor, 2-hydroxy-3-imidazo[1,2-a]pyridin-3-yl-2-phosphonopropionic acid.
AID303800Reduction of viability of mouse J744 cells after 48 hrs2007Journal of medicinal chemistry, Nov-29, Volume: 50, Issue:24
Synthesis and biological evaluation of alpha-halogenated bisphosphonate and phosphonocarboxylate analogues of risedronate.
AID471507Inhibition of recombinant Rab geranylgeranyltransferase expressed in human MCF7 cells assessed as inhibition of geranylgeranylation of EYFP-Rab7 protein by Western blot2009Journal of medicinal chemistry, Dec-24, Volume: 52, Issue:24
Design, synthesis, and characterization of peptide-based rab geranylgeranyl transferase inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (6)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's3 (50.00)29.6817
2010's3 (50.00)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.43

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be weak demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index12.43 (24.57)
Research Supply Index1.95 (2.92)
Research Growth Index4.37 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (12.43)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other6 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]