Page last updated: 2024-12-10

lomeguatrib

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 CID3025944
CHEMBL ID339133
SCHEMBL ID4621691
SCHEMBL ID19549802
MeSH IDM0511536

Synonyms (60)

Synonym
6-((4-bromothiophen-2-yl)methoxy)-9h-purin-2-amine
o(6)-(4-bromothenyl)guanine
192441-08-0
6-((4-bromo-2-thienyl)methoxyl)purin-2-amine
lomeguatrib
6-(4-bromothenyloxy)-7h-purin-2-amine
patrin 2
lomeguatrib [inn]
CHEMBL339133 ,
6-(4-bromo-thiophen-2-ylmethoxy)-9h-purin-2-ylamine
bdbm50106517
6-[(4-bromothiophen-2-yl)methoxy]-7h-purin-2-amine
HY-13668
CS-1385
FT-0670846
s79265t71m ,
lomeguatrib [inn:ban]
unii-s79265t71m
S8056
lomeguatrib [who-dd]
MLS006010267
smr004701339
SCHEMBL4621691
patrin-2
6-[(4-bromo-2-thienyl)methoxy]-9h-purin-2-amine
1h-purin-2-amine, 6-[(4-bromo-2-thienyl)methoxy]-
c10h8brn5os
6-[(4-bromo-2-thienyl)methoxy]-9h-p urin-2-amine
HB1376
6-((4-bromothiophen-2-yl)methoxy)-7h-purin-2-amine
AC-30287
AKOS024458115
DTXSID60172838
GS-1303
AKOS028109340
lomeguqtrib
EX-A661
AKOS027250766
2-amino-6-[(4-bromo-2-thienyl)methoxy]-9h-purine
SR-01000945001-1
sr-01000945001
HMS3653P06
mfcd23703756
lomeguatrib, >=98% (hplc)
J-012442
NCGC00345496-08
SCHEMBL19549802
SW218182-2
lomeguatrib(patrin-2)
BCP07818
6-(4-bromothiophen-2-ylmethoxy)-9h-purin-2-ylamine
9h-purin-2-amine, 6-[(4-bromo-2-thienyl)methoxy]-
SB19180
NCGC00345496-13
HMS3740E17
CCG-265033
Q27288769
nsc-787251
nsc787251
NCGC00345496-02

Research Excerpts

Treatment

ExcerptReferenceRelevance
"treatment with Lomeguatrib (to suppress MGMT activity) and Temozolomide (to kill sensitive blasts and to presumably induce CX in resistant leukaemic cells); (b) immune response recovery phase using interleukin-2 (to possibly restore an immune response and take advantage of the hypothetical, triazene-induced CX)."( Novel role of triazenes in haematological malignancies: pilot study of Temozolomide, Lomeguatrib and IL-2 in the chemo-immunotherapy of acute leukaemia.
Alvino, E; Amadori, S; Bonmassar, E; Buccisano, F; Caporaso, P; D'Atri, S; Garbin, A; Marchesi, F; Tirindelli, MC; Toppo, L; Tortorelli, G; Turriziani, M; Venditti, A, 2007
)
0.9

Compound-Compound Interactions

Lomeguatrib was administered at dose levels of 10 to 40 mg/m2 days 1 to 5, as a single agent, and also in combination with temozolomide. The main aims of this phase I trial were to determine an ATase-depleting dose (ADD) and to define a suitable dose for use in patients with advanced cancer.

ExcerptReferenceRelevance
" Furthermore, we show that a human haemopoietic cell line (K562) transduced with a retroviral vector encoding MGMT(P140K) is highly resistant to the cytotoxic effects of PaTrin-2 in combination with the methylating agent temozolomide, and that cells expressing MGMT(P140K) can be effectively enriched in vitro following challenge with this drug combination."( The P140K mutant of human O(6)-methylguanine-DNA-methyltransferase (MGMT) confers resistance in vitro and in vivo to temozolomide in combination with the novel MGMT inactivator O(6)-(4-bromothenyl)guanine.
Fairbairn, LJ; Margison, GP; Milsom, MD; Southgate, TD; Woolford, LB, 2006
)
0.33
" The main aims of this phase I trial were to determine an ATase-depleting dose (ADD) of lomeguatrib, a potent pseudosubstrate inhibitor, and to define a suitable dose of temozolomide to be used in combination with lomeguatrib in patients with advanced cancer."( Lomeguatrib, a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase: phase I safety, pharmacodynamic, and pharmacokinetic trial and evaluation in combination with temozolomide in patients with advanced solid tumors.
Bridgewater, J; Dawson, M; Donnelly, D; Gumbrell, L; Halbert, G; Jowle, D; Lee, SM; Margison, GP; McElhinney, RS; McGrath, H; McMurry, TB; Middleton, MR; Ranson, M; Waller, S, 2006
)
2
"Lomeguatrib was administered at dose levels of 10 to 40 mg/m2 days 1 to 5, as a single agent, and also in combination with temozolomide."( Lomeguatrib, a potent inhibitor of O6-alkylguanine-DNA-alkyltransferase: phase I safety, pharmacodynamic, and pharmacokinetic trial and evaluation in combination with temozolomide in patients with advanced solid tumors.
Bridgewater, J; Dawson, M; Donnelly, D; Gumbrell, L; Halbert, G; Jowle, D; Lee, SM; Margison, GP; McElhinney, RS; McGrath, H; McMurry, TB; Middleton, MR; Ranson, M; Waller, S, 2006
)
3.22
" Herein, we report the first phase I experience of the novel O6-meG pseudosubstrate lomeguatrib, combined with dacarbazine."( Inhibition of DNA repair with MGMT pseudosubstrates: phase I study of lomeguatrib in combination with dacarbazine in patients with advanced melanoma and other solid tumours.
Kirkwood, JM; Moschos, S; Radkowski, R; Shipe-Spotloe, J; Sulecki, M; Tarhini, A; Tawbi, HA; Villaruz, L; Viverette, F, 2011
)
0.83
"This is a phase I dose-escalation study to determine the maximum tolerated dose and recommended phase II dose (RP2D) of lomeguatrib combined with a single dose of dacarbazine on a 21-day schedule."( Inhibition of DNA repair with MGMT pseudosubstrates: phase I study of lomeguatrib in combination with dacarbazine in patients with advanced melanoma and other solid tumours.
Kirkwood, JM; Moschos, S; Radkowski, R; Shipe-Spotloe, J; Sulecki, M; Tarhini, A; Tawbi, HA; Villaruz, L; Viverette, F, 2011
)
0.81

Bioavailability

ExcerptReferenceRelevance
"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

Lomeguatrib, an O(6)-methylguanine-DNA methyltransferase inactivator, was evaluated in an extended dosing regimen with temozolomide. If further studies are to be performed, emerging data suggest that higher daily doses of lomegu atrib and a dosing period beyond that of TMZ should be evaluated.

ExcerptRelevanceReference
" Extended dosing has met with early favourable results."( Exploiting the role of O6-methylguanine-DNA-methyltransferase (MGMT) in cancer therapy.
Middleton, MR; Sabharwal, A, 2006
)
0.33
"The efficacy of LM and TMZ in the current dosing schedule is similar to that of TMZ alone."( Randomized trial of the combination of lomeguatrib and temozolomide compared with temozolomide alone in chemotherapy naive patients with metastatic cutaneous melanoma.
Baka, S; Beith, J; Davis, ID; Harris, PA; Haydon, A; Hersey, P; Kefford, RF; Margison, GP; McArthur, GA; Middleton, MR; Mortimer, P; Ranson, M; Sabharwal, A; Seebaran, A; Thompson, D; Watson, AJ, 2007
)
0.61
" If further studies are to be performed, emerging data suggest that higher daily doses of lomeguatrib and a dosing period beyond that of TMZ should be evaluated."( A phase II trial of lomeguatrib and temozolomide in metastatic colorectal cancer.
Khan, OA; Levitt, NC; Margison, GP; Michael, M; Middleton, MR; Midgley, R; Mortimer, P; Olver, I; Ranson, M; Watson, AJ, 2008
)
0.89
"Lomeguatrib, an O(6)-methylguanine-DNA methyltransferase inactivator, was evaluated in an extended dosing regimen with temozolomide, designed according to pharmacodynamic data from previous studies."( A phase I study of extended dosing with lomeguatrib with temozolomide in patients with advanced melanoma.
Abdi, E; Beith, J; Corrie, PG; Kefford, RF; Kotasek, D; Margison, GP; Middleton, MR; Mortimer, P; Palmer, C; Ranson, M; Thomas, NP; Watson, AJ, 2009
)
2.06
" Early recovery of MGMT activity in tumours suggested that more protracted dosing with LM is required."( O(6)-methylguanine-DNA methyltransferase depletion and DNA damage in patients with melanoma treated with temozolomide alone or with lomeguatrib.
Beith, J; Davis, ID; Haydon, A; Hayward, O; Hersey, P; Kefford, R; Lorigan, P; Margison, GP; McArthur, G; McGown, G; Middleton, MR; Mortimer, P; Ranson, M; Sabharwal, A; Thomson, D; Thorncroft, M; Watson, AJ, 2009
)
0.56
" We sought to determine the dose of oral 6-(4-bromo-2-thienyl) methoxy purin-2-amine (lomeguatrib), a pseudosubstrate inactivator of MGMT, required to render active protein undetectable 12 hours after dosing in prostate, primary central nervous system (CNS), and colorectal cancer patients."( Tumor O(6)-methylguanine-DNA methyltransferase inactivation by oral lomeguatrib.
Bojanic, S; Kerr, R; King, A; Leung, H; Margison, GP; McGown, G; Middleton, MR; Miller, A; Sabharwal, A; Soonawalla, Z; Thorncroft, M; Waller, S; Watson, AJ, 2010
)
0.82
"Thirty-seven patients were dosed with lomeguatrib, and 32 informative tumor samples were obtained."( Tumor O(6)-methylguanine-DNA methyltransferase inactivation by oral lomeguatrib.
Bojanic, S; Kerr, R; King, A; Leung, H; Margison, GP; McGown, G; Middleton, MR; Miller, A; Sabharwal, A; Soonawalla, Z; Thorncroft, M; Waller, S; Watson, AJ, 2010
)
0.87
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (9)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
PPM1D proteinHomo sapiens (human)Potency29.41070.00529.466132.9993AID1347411
cytochrome P450 family 3 subfamily A polypeptide 4Homo sapiens (human)Potency1.06840.01237.983543.2770AID1645841
GVesicular stomatitis virusPotency26.83700.01238.964839.8107AID1645842
cytochrome P450 2D6Homo sapiens (human)Potency6.74120.00108.379861.1304AID1645840
Interferon betaHomo sapiens (human)Potency28.76730.00339.158239.8107AID1347411; AID1645842
HLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
Inositol hexakisphosphate kinase 1Homo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
cytochrome P450 2C9, partialHomo sapiens (human)Potency26.83700.01238.964839.8107AID1645842
[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)
Methylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)IC50 (µMol)0.00600.00300.37792.6000AID106501; AID579768
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (51)

Processvia Protein(s)Taxonomy
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell activation involved in immune responseInterferon betaHomo sapiens (human)
cell surface receptor signaling pathwayInterferon betaHomo sapiens (human)
cell surface receptor signaling pathway via JAK-STATInterferon betaHomo sapiens (human)
response to virusInterferon betaHomo sapiens (human)
positive regulation of autophagyInterferon betaHomo sapiens (human)
cytokine-mediated signaling pathwayInterferon betaHomo sapiens (human)
natural killer cell activationInterferon betaHomo sapiens (human)
positive regulation of peptidyl-serine phosphorylation of STAT proteinInterferon betaHomo sapiens (human)
cellular response to interferon-betaInterferon betaHomo sapiens (human)
B cell proliferationInterferon betaHomo sapiens (human)
negative regulation of viral genome replicationInterferon betaHomo sapiens (human)
innate immune responseInterferon betaHomo sapiens (human)
positive regulation of innate immune responseInterferon betaHomo sapiens (human)
regulation of MHC class I biosynthetic processInterferon betaHomo sapiens (human)
negative regulation of T cell differentiationInterferon betaHomo sapiens (human)
positive regulation of transcription by RNA polymerase IIInterferon betaHomo sapiens (human)
defense response to virusInterferon betaHomo sapiens (human)
type I interferon-mediated signaling pathwayInterferon betaHomo sapiens (human)
neuron cellular homeostasisInterferon betaHomo sapiens (human)
cellular response to exogenous dsRNAInterferon betaHomo sapiens (human)
cellular response to virusInterferon betaHomo sapiens (human)
negative regulation of Lewy body formationInterferon betaHomo sapiens (human)
negative regulation of T-helper 2 cell cytokine productionInterferon betaHomo sapiens (human)
positive regulation of apoptotic signaling pathwayInterferon betaHomo sapiens (human)
response to exogenous dsRNAInterferon betaHomo sapiens (human)
B cell differentiationInterferon betaHomo sapiens (human)
natural killer cell activation involved in immune responseInterferon betaHomo sapiens (human)
adaptive immune responseInterferon betaHomo sapiens (human)
T cell activation involved in immune responseInterferon betaHomo sapiens (human)
humoral immune responseInterferon betaHomo sapiens (human)
positive regulation of T cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
adaptive immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class I via ER pathway, TAP-independentHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of T cell anergyHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
defense responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
detection of bacteriumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-12 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of interleukin-6 productionHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protection from natural killer cell mediated cytotoxicityHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
innate immune responseHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
regulation of dendritic cell differentiationHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
antigen processing and presentation of endogenous peptide antigen via MHC class IbHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
DNA ligationMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
DNA alkylation repairMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
methylationMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
negative regulation of apoptotic processMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
positive regulation of double-strand break repairMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
DNA repairMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
inositol phosphate metabolic processInositol hexakisphosphate kinase 1Homo sapiens (human)
phosphatidylinositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
negative regulation of cold-induced thermogenesisInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol phosphate biosynthetic processInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
cytokine activityInterferon betaHomo sapiens (human)
cytokine receptor bindingInterferon betaHomo sapiens (human)
type I interferon receptor bindingInterferon betaHomo sapiens (human)
protein bindingInterferon betaHomo sapiens (human)
chloramphenicol O-acetyltransferase activityInterferon betaHomo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
signaling receptor bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
peptide antigen bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
TAP bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
protein-folding chaperone bindingHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
DNA bindingMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
methyltransferase activityMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
DNA-methyltransferase activityMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
metal ion bindingMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
methylated-DNA-[protein]-cysteine S-methyltransferase activityMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
inositol-1,3,4,5,6-pentakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol heptakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
protein bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
ATP bindingInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 1-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol hexakisphosphate 3-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol 5-diphosphate pentakisphosphate 5-kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
inositol diphosphate tetrakisphosphate kinase activityInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (22)

Processvia Protein(s)Taxonomy
extracellular spaceInterferon betaHomo sapiens (human)
extracellular regionInterferon betaHomo sapiens (human)
Golgi membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
endoplasmic reticulumHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
Golgi apparatusHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
cell surfaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
ER to Golgi transport vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
secretory granule membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
phagocytic vesicle membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
early endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
recycling endosome membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular exosomeHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
lumenal side of endoplasmic reticulum membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
MHC class I protein complexHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
extracellular spaceHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
external side of plasma membraneHLA class I histocompatibility antigen, B alpha chain Homo sapiens (human)
nucleoplasmMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
membraneMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
nucleusMethylated-DNA--protein-cysteine methyltransferaseHomo sapiens (human)
fibrillar centerInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
cytosolInositol hexakisphosphate kinase 1Homo sapiens (human)
nucleusInositol hexakisphosphate kinase 1Homo sapiens (human)
cytoplasmInositol hexakisphosphate kinase 1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (11)

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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
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.
AID1347411qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Mechanism Interrogation Plate v5.0 (MIPE) Libary2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
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.
AID1347160Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID106501In vitro inhibition of MGMT using cell free extracts from HeLa S3 cells2001Journal of medicinal chemistry, Nov-22, Volume: 44, Issue:24
Monosaccharide-linked inhibitors of O(6)-methylguanine-DNA methyltransferase (MGMT): synthesis, molecular modeling, and structure-activity relationships.
AID579768Inactivation of human O-6-methylguanine-DNA methyltransferase assessed as [3H]methylated protein formation by liquid scintillation counting in presence of [3H]methylated calf thymus DNA2011Bioorganic & medicinal chemistry, Mar-01, Volume: 19, Issue:5
Towards more specific O6-methylguanine-DNA methyltransferase (MGMT) inactivators.
AID1888337Inhibition of human recombinant MGMT expressed in Escherichia coli STAR BL21 pRare cells assessed as cleavage of fluorescent labelled substrate by Bsp 119I at 12.5 uM using O6MeG-bearing substrate (S) incubated for 5 mins by coupled enzymatic analysis rel
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (39)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's0 (0.00)18.2507
2000's16 (41.03)29.6817
2010's14 (35.90)24.3611
2020's9 (23.08)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 23.60

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 moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index23.60 (24.57)
Research Supply Index3.87 (2.92)
Research Growth Index5.83 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (23.60)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials8 (20.51%)5.53%
Reviews1 (2.56%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other30 (76.92%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]