Page last updated: 2024-12-07

ym 529

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Description

YM 529: inhibits osteoclastic bone resorption; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID130956
CHEMBL ID319144
SCHEMBL ID145238
MeSH IDM0232842

Synonyms (70)

Synonym
CHEMBL319144
bph 261
ono 5920
gtpl3164
recalbon
bonoteo
ono-5920
minodronic acid
onobis
ym-529
yh-529
minodronate ,
phosphonic acid, (1-hydroxy-2-imidazo[1,2-a]pyridin-3-ylethylidene)bis-
bisphosphonate, 57
(1-hydroxy-2-{imidazo[1,2-a]pyridin-3-yl}-1-phosphonoethyl)phosphonic acid
bdbm25308
m0n ,
(1-hydroxy-2-imidazo[1,2-a]pyridin-3-ylethane-1,1-diyl)bis(phosphonic acid)
nsc-725590
(1-hydroxy-2-imidazo[1,1-bisphos phonate
180064-38-4
nsc725590
ym529
phosphonic acid, (1-hydroxy-2-imidazo(1,2-a)pyridin-3-ylethylidene)bis-
127657-42-5
yh 529
ym 529
(1-hydroxy-2-imidazo[1,2-a]pyridin-3-yl-1-phosphonoethyl)phosphonic acid
NCGC00183829-01
cas-180064-38-4
tox21_113255
dtxsid4048779 ,
dtxcid4028705
(2-imidazo[1,2-a]pyridin-3-yl-1-oxidanyl-1-phosphono-ethyl)phosphonic acid
[1-hydroxy-2-(3-imidazo[1,2-a]pyridinyl)-1-phosphonoethyl]phosphonic acid
A812516
nsc 725590
phosphonic acid, p,p'-(1-hydroxy-2-imidazo(1,2-a)pyridin-3-ylethylidene)bis-
unii-40sgr63tgl
40sgr63tgl ,
minodronic acid [inn]
FT-0687492
FT-0689646
(1-hydroxy-2-(imidazo[1,2-a]pyridin-3-yl)ethane-1,1-diyl)diphosphonic acid
AM84629
AKOS015856182
S5057
c9h12n2o7p2
minodronic acid [mi]
minodronic acid [who-dd]
minodronic acid [mart.]
(1-hydroxy-2-imidazo(1,2-a)pyridin-3-ylethylidene)diphosphonic acid
SCHEMBL145238
VMMKGHQPQIEGSQ-UHFFFAOYSA-N
AC-24008
1-hydroxy-2-[imidazo[1,2-a]pyridin-3-yl]ethylidene-1,1-diphosphonic acid
M2360
AS-73348
(1-hydroxy-2-(imidazo[1,2-a]pyridin-3-yl)ethane-1,1-diyl)bis(phosphonic acid)
Q2823280
phosphonic acid, p,p'-(1-hydroxy-2-imidazo[1,2-a]pyridin-3-ylethylidene)bis-
mfcd00890772
DB06548
(1-hydroxy-2-(imidazo[1,2-a]pyridin-3-yl)ethane-1,1-diyl)diphosphonicacid
minodronic-acid
ym-529; ono-5920; yh-529
HY-16322
CS-0006290
minodronic acidminodronic acid
C73434

Research Excerpts

Toxicity

ExcerptReferenceRelevance
" The changes in bone mineral density (BMD) and bone turnover markers were investigated at 3 and 6 months, and adverse events, including the presence or absence of an incident osteoporotic fracture, were examined over a period of 6 months."( Efficacy and safety of minodronic acid hydrate in patients with steroid-induced osteoporosis.
Ikumi, N; Inomata, H; Iwata, M; Karasawa, H; Kitamura, N; Matsukawa, Y; Nagasawa, Y; Nozaki, T; Shiraiwa, H; Sugiyama, K; Takei, M, 2018
)
0.48
" Adverse events included toothache for which the patient discontinued the treatment and three cases of gastrointestinal disorder that did not lead to discontinuation, and thus minodronic acid hydrate was well tolerated."( Efficacy and safety of minodronic acid hydrate in patients with steroid-induced osteoporosis.
Ikumi, N; Inomata, H; Iwata, M; Karasawa, H; Kitamura, N; Matsukawa, Y; Nagasawa, Y; Nozaki, T; Shiraiwa, H; Sugiyama, K; Takei, M, 2018
)
0.48
" BMD, bone metabolism markers, incidence of bone fractures, medication compliance, and other adverse events (AE) were examined every 24 weeks following administration."( Efficacy and Safety of Monthly Minodronate Therapy in Postmenopausal Breast Cancer Patients Receiving Aromatase Inhibitors.
Akagi, Y; Matushima, S; Ogata, N; Ogata, S; Sudou, T; Sugihara, R; Takao, Y; Toh, U; Watanabe, H, 2022
)
0.72
" No adverse grade 2 or higher event was observed throughout this study."( Efficacy and Safety of Monthly Minodronate Therapy in Postmenopausal Breast Cancer Patients Receiving Aromatase Inhibitors.
Akagi, Y; Matushima, S; Ogata, N; Ogata, S; Sudou, T; Sugihara, R; Takao, Y; Toh, U; Watanabe, H, 2022
)
0.72
"The combined administration of minodronate and AIs was safe and effective in preventing bone loss complications in postmenopausal BC patients."( Efficacy and Safety of Monthly Minodronate Therapy in Postmenopausal Breast Cancer Patients Receiving Aromatase Inhibitors.
Akagi, Y; Matushima, S; Ogata, N; Ogata, S; Sudou, T; Sugihara, R; Takao, Y; Toh, U; Watanabe, H, 2022
)
0.72

Pharmacokinetics

ExcerptReferenceRelevance
" The aim of this study was to evaluate the pharmacokinetic profiles and tolerability of minodronic acid in healthy subjects, as well as to assess the effects of food and age on the pharmacokinetics."( Pharmacokinetics and tolerability of minodronic acid tablets in healthy Chinese subjects and food and age effects on the pharmacokinetics.
Chen, H; He, X; Li, H; Li, W; Ni, Y; Sattar, H; Xu, M; Zhou, Y, 2015
)
0.42

Compound-Compound Interactions

ExcerptReferenceRelevance
" We report the induction of apoptosis by MDA in combination with γδ T-cells."( Minodronic Acid in Combination with γδT Cells Induces Apoptosis of Non-small Cell Lung Carcinoma Cell Lines.
Kawaguchi, T; Kawai, N; Nakazawa, T; Taniguchi, S; Tojo, T; Tsujimura, T; Yasukawa, M, 2016
)
0.43

Bioavailability

ExcerptReferenceRelevance
" Food, especially high-fat food, reduced the bioavailability of minodronic acid."( Pharmacokinetics and tolerability of minodronic acid tablets in healthy Chinese subjects and food and age effects on the pharmacokinetics.
Chen, H; He, X; Li, H; Li, W; Ni, Y; Sattar, H; Xu, M; Zhou, Y, 2015
)
0.42
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)
0.51

Dosage Studied

ExcerptRelevanceReference
" Although a transient decrease in serum Ca and increase in PTH levels were observed in all three groups at slightly different magnitudes and time courses, changes in bone turnover markers were comparable among the different dosage groups with a similar time course."( Efficacy and safety of monthly oral minodronate in patients with involutional osteoporosis.
Fukunaga, M; Hagino, H; Ito, M; Matsumoto, T; Mizunuma, H; Nakamura, T; Nishizawa, Y; Ohashi, Y; Okazaki, R; Shiraki, M; Sone, T, 2012
)
0.38
" The total dosing amount was comparable between the two dosing regimens."( Intermittent minodronic acid treatment with sufficient bone resorption inhibition prevents reduction in bone mass and strength in ovariectomized rats with established osteopenia comparable with daily treatment.
Fukushima, S; Kimoto, A; Mori, H; Mori, M; Nakamura, T; Nozaki, K; Shiroya, T; Tanaka, M, 2013
)
0.39
" Approximately, 65 % of patients were willing to switch to MIN 50 mg, with the predominant reason being "less frequent dosing more convenient."( Clinical efficacy and treatment persistence of monthly minodronate for osteoporotic patients unsatisfied with, and shifted from, daily or weekly bisphosphonates: the BP-MUSASHI study.
Arita, S; Fukuda, F; Ikeda, S; Matsumoto, H; Nagashima, M; Okazaki, Y; Okimoto, N; Sakai, A; Teshima, K; Tsurukami, H; Yoshioka, T, 2014
)
0.4
"Single dosing of minodronic acid exhibited linear pharmacokinetics over the range of 1 to 4 mg; there was no accumulation after repeated administration."( Pharmacokinetics and tolerability of minodronic acid tablets in healthy Chinese subjects and food and age effects on the pharmacokinetics.
Chen, H; He, X; Li, H; Li, W; Ni, Y; Sattar, H; Xu, M; Zhou, Y, 2015
)
0.42
"Minodronate is a potent nitrogen-containing bisphosphonate that can be administered according to a monthly (every 4 weeks) dosing regimen."( Patient preference for monthly bisphosphonate versus weekly bisphosphonate in a cluster-randomized, open-label, crossover trial: Minodroate Alendronate/Risedronate Trial in Osteoporosis (MARTO).
Furuya, T; Hasegawa, M; Hirabayashi, H; Iwamoto, J; Kumakubo, T; Makita, K; Okano, H; Urano, T, 2016
)
0.43
" OVX rats were orally treated with MIN (6, 30, and 150 µg/kg/day) for 12 months and necropsied on the day after the last dosing or following 3 months of withdrawal."( Attenuation of Antiresorptive Action in Withdrawal of Minodronic Acid for Three Months After Treatment for Twelve Months in Ovariectomized Rats.
Kawabata, K; Mori, H; Tanaka, M, 2015
)
0.42
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (5)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
TDP1 proteinHomo sapiens (human)Potency11.88560.000811.382244.6684AID686979
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Geranylgeranyl pyrophosphate synthaseHomo sapiens (human)IC50 (µMol)75.99400.00401.02764.5000AID1798541; AID326141; AID391371; AID480321
Geranylgeranyl pyrophosphate synthaseHomo sapiens (human)Ki1.80001.80002.25002.7000AID326142
Farnesyl pyrophosphate synthaseHomo sapiens (human)IC50 (µMol)0.00260.00020.71099.3600AID1197852; AID1519530; AID480313
Farnesyl diphosphate synthaseEscherichia coli K-12IC50 (µMol)1.10001.10001.10001.1000AID275060
Geranylgeranyl pyrophosphate synthaseSaccharomyces cerevisiae S288CIC50 (µMol)0.34000.00400.41200.7100AID326139
Geranylgeranyl pyrophosphate synthaseSaccharomyces cerevisiae S288CKi0.13000.13000.19500.2600AID326140
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (6)

Processvia Protein(s)Taxonomy
isoprenoid metabolic processGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
geranyl diphosphate biosynthetic processGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
geranylgeranyl diphosphate biosynthetic processGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
farnesyl diphosphate biosynthetic processGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
isoprenoid biosynthetic processGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
cholesterol biosynthetic processFarnesyl pyrophosphate synthaseHomo sapiens (human)
geranyl diphosphate biosynthetic processFarnesyl pyrophosphate synthaseHomo sapiens (human)
farnesyl diphosphate biosynthetic processFarnesyl pyrophosphate synthaseHomo sapiens (human)
geranyl diphosphate biosynthetic processFarnesyl diphosphate synthaseEscherichia coli K-12
farnesyl diphosphate biosynthetic processFarnesyl diphosphate synthaseEscherichia coli K-12
isoprenoid biosynthetic processFarnesyl diphosphate synthaseEscherichia coli K-12
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (9)

Processvia Protein(s)Taxonomy
dimethylallyltranstransferase activityGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
farnesyltranstransferase activityGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
geranyltranstransferase activityGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
protein bindingGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
identical protein bindingGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
metal ion bindingGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
prenyltransferase activityGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
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)
dimethylallyltranstransferase activityFarnesyl diphosphate synthaseEscherichia coli K-12
geranyltranstransferase activityFarnesyl diphosphate synthaseEscherichia coli K-12
prenyltransferase activityFarnesyl diphosphate synthaseEscherichia coli K-12
protein bindingFarnesyl diphosphate synthaseEscherichia coli K-12
transferase activityFarnesyl diphosphate synthaseEscherichia coli K-12
metal ion bindingFarnesyl diphosphate synthaseEscherichia coli K-12
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Processvia Protein(s)Taxonomy
nucleoplasmGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
cytoplasmGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
cytosolGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
Z discGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
perinuclear region of cytoplasmGeranylgeranyl pyrophosphate synthaseHomo sapiens (human)
nucleoplasmFarnesyl pyrophosphate synthaseHomo sapiens (human)
cytosolFarnesyl pyrophosphate synthaseHomo sapiens (human)
cytoplasmFarnesyl pyrophosphate synthaseHomo sapiens (human)
cytoplasmFarnesyl diphosphate synthaseEscherichia coli K-12
cytosolFarnesyl diphosphate synthaseEscherichia coli K-12
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (34)

Assay IDTitleYearJournalArticle
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1346874Human geranylgeranyl diphosphate synthase (Lanosterol biosynthesis pathway)2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation.
AID1346874Human geranylgeranyl diphosphate synthase (Lanosterol biosynthesis pathway)2010Journal 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.
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.
AID184809Bone resorption activity in rats.2002Journal of medicinal chemistry, Jul-04, Volume: 45, Issue:14
An investigation of bone resorption and Dictyostelium discoideum growth inhibition by bisphosphonate drugs.
AID71579Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using individual observed maximum TNF-alpha release2004Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
Quantitative structure-activity relationships for gammadelta T cell activation by bisphosphonates.
AID326140Binding affinity to Saccharomyces cerevisiae GGPPS2007Proceedings of the National Academy of Sciences of the United States of America, Jun-12, Volume: 104, Issue:24
Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases.
AID275056Antibacterial activity against Escherichia coli pTMV19 in presence of mevalonate2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Isoprenoid biosynthesis as a drug target: bisphosphonate inhibition of Escherichia coli K12 growth and synergistic effects of fosmidomycin.
AID71581pIC50 value for stimulation of TNF-alpha release in gamma-delta T cells, using individual observed maximum TNF-alpha release2004Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
Quantitative structure-activity relationships for gammadelta T cell activation by bisphosphonates.
AID391371Inhibition of human recombinant geranylgeranyl diphosphate synthase2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation.
AID71578Inhibitory activity, for stimulation of TNF-alpha release in gamma-delta T cells, using a constrained maximum TNF-alpha release of 2700 pg/mL2004Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
Quantitative structure-activity relationships for gammadelta T cell activation by bisphosphonates.
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.
AID248772In vitro inhibitory concentration against the growth of Toxoplasma gondii in human foreskin fibroblast monolayer cells (HFF cells)2005Journal of medicinal chemistry, May-05, Volume: 48, Issue:9
Bisphosphonate inhibitors of Toxoplasma gondi growth: in vitro, QSAR, and in vivo investigations.
AID326147Inhibition of Escherichia coli OPPS2007Proceedings of the National Academy of Sciences of the United States of America, Jun-12, Volume: 104, Issue:24
Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases.
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.
AID326141Inhibition of human GGPPS2007Proceedings of the National Academy of Sciences of the United States of America, Jun-12, Volume: 104, Issue:24
Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases.
AID326142Binding affinity to human GGPPS2007Proceedings of the National Academy of Sciences of the United States of America, Jun-12, Volume: 104, Issue:24
Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases.
AID71580pIC50 value for stimulation of TNF-alpha release in gamma-delta T cells, using a constrained maximum TNF-alpha release of 2700 pg/mL2004Journal of medicinal chemistry, Jan-15, Volume: 47, Issue:2
Quantitative structure-activity relationships for gammadelta T cell activation by bisphosphonates.
AID1519530Inhibition of FDPS (unknown origin)2019Bioorganic & medicinal chemistry letters, 12-15, Volume: 29, Issue:24
Novel benzimidazole phosphonates as potential inhibitors of protein prenylation.
AID275055Antibacterial activity against Escherichia coli pTMV192006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Isoprenoid biosynthesis as a drug target: bisphosphonate inhibition of Escherichia coli K12 growth and synergistic effects of fosmidomycin.
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.
AID1197854Reduction in hypercalcemia in sc dosed rat2015Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase.
AID326146Inhibition of Sulfolobus solfataricus HPPS2007Proceedings of the National Academy of Sciences of the United States of America, Jun-12, Volume: 104, Issue:24
Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases.
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.
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.
AID480318Inhibition of RGGT-mediated Rap1A 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.
AID275054Antibacterial activity against Escherichia coli W31102006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Isoprenoid biosynthesis as a drug target: bisphosphonate inhibition of Escherichia coli K12 growth and synergistic effects of fosmidomycin.
AID275060Inhibition of Escherichia coli FPPS2006Journal of medicinal chemistry, Dec-14, Volume: 49, Issue:25
Isoprenoid biosynthesis as a drug target: bisphosphonate inhibition of Escherichia coli K12 growth and synergistic effects of fosmidomycin.
AID1197852Inhibition of human FPPS2015Bioorganic & medicinal chemistry letters, Mar-01, Volume: 25, Issue:5
Probing the molecular and structural elements of ligands binding to the active site versus an allosteric pocket of the human farnesyl pyrophosphate synthase.
AID326139Inhibition of Saccharomyces cerevisiae GGPPS2007Proceedings of the National Academy of Sciences of the United States of America, Jun-12, Volume: 104, Issue:24
Bisphosphonates target multiple sites in both cis- and trans-prenyltransferases.
AID1798541GGPP Synthase Inhibition Assay from Article 10.1021/jm800325y: \\Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation.\\2008Journal of medicinal chemistry, Sep-25, Volume: 51, Issue:18
Inhibition of geranylgeranyl diphosphate synthase by bisphosphonates: a crystallographic and computational investigation.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (136)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's7 (5.15)18.2507
2000's53 (38.97)29.6817
2010's62 (45.59)24.3611
2020's14 (10.29)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 10.23

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 Index10.23 (24.57)
Research Supply Index5.10 (2.92)
Research Growth Index5.33 (4.65)
Search Engine Demand Index0.00 (26.88)
Search Engine Supply Index0.00 (0.95)

This Compound (10.23)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials23 (16.43%)5.53%
Reviews11 (7.86%)6.00%
Case Studies6 (4.29%)4.05%
Observational6 (4.29%)0.25%
Other94 (67.14%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]