Page last updated: 2024-12-08

nsc-134754

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

Description

NSC-134754: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	3246465
CHEMBL ID	1488690
MeSH ID	M0487378
PubMed CID	421494
CHEMBL ID	1718952
SCHEMBL ID	13912583
MeSH ID	M0487378

Synonyms (17)

Synonym
nsc-134754
(11br)-3-ethyl-9,10-dimethoxy-2-[[(1r)-1,2,3,4-tetrahydroisoquinolin-1-yl]methyl]-4,6,7,11b-tetrahydro-1h-benzo[a]quinolizine
NCGC00014341 ,
NCGC00097450-01
NCGC00014341-02
CHEMBL1488690
mls002701998 ,
smr001565575
NSC134754 ,
10,11-dimethoxy-2,3-didehydroemetan
10,11-dimethoxy-2,3-didehydroe.meta.n
3-ethyl-9,10-dimethoxy-2-(1,2,3,4-tetrahydroisoquinolin-1-ylmethyl)-4,6,7,11b-tetrahydro-1h-benzo[a]quinolizine
NCI60_000775
SCHEMBL13912583
CHEMBL1718952
3-ethyl-9,10-dimethoxy-2-(1,2,3,4-tetrahydro-isoquinolin-1-ylmethyl)-1,6,7,11b-tetrahydro-4h-pyrido[2,1-a]isoquinoline
aromatic and heteroaryl compound 1

[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (16)

Potency Measurements

Protein	Taxonomy	Measurement	Average (µ)	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
hypoxia-inducible factor 1, alpha subunit (basic helix-loop-helix transcription factor)	Homo sapiens (human)	Potency	3.1623	0.0013	7.7625	44.6684	AID914; AID915
thyroid stimulating hormone receptor	Homo sapiens (human)	Potency	1.5849	0.0013	18.0743	39.8107	AID926; AID938
cytochrome P450 2D6 isoform 1	Homo sapiens (human)	Potency	2.5119	0.0020	7.5337	39.8107	AID891
lethal factor (plasmid)	Bacillus anthracis str. A2012	Potency	5.0119	0.0200	10.7869	31.6228	AID912
glp-1 receptor, partial	Homo sapiens (human)	Potency	11.2202	0.0184	6.8060	14.1254	AID624417
TDP1 protein	Homo sapiens (human)	Potency	1.3971	0.0008	11.3822	44.6684	AID686978; AID686979
Smad3	Homo sapiens (human)	Potency	3.5152	0.0052	7.8098	29.0929	AID588855; AID720534; AID720536; AID720537
67.9K protein	Vaccinia virus	Potency	3.5481	0.0001	8.4406	100.0000	AID720579; AID720580
IDH1	Homo sapiens (human)	Potency	23.1093	0.0052	10.8652	35.4813	AID686970
nuclear factor erythroid 2-related factor 2 isoform 2	Homo sapiens (human)	Potency	3.6626	0.0041	9.9848	25.9290	AID504444
parathyroid hormone/parathyroid hormone-related peptide receptor precursor	Homo sapiens (human)	Potency	3.9811	3.5481	19.5427	44.6684	AID743266
peptidyl-prolyl cis-trans isomerase NIMA-interacting 1	Homo sapiens (human)	Potency	53.5818	0.4256	12.0591	28.1838	AID504891
DNA polymerase iota isoform a (long)	Homo sapiens (human)	Potency	79.4328	0.0501	27.0736	89.1251	AID588590
geminin	Homo sapiens (human)	Potency	3.2643	0.0046	11.3741	33.4983	AID624297
Glycoprotein hormones alpha chain	Homo sapiens (human)	Potency	3.5481	4.4668	8.3448	10.0000	AID624291
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Other Measurements

Protein	Taxonomy	Measurement	Average	Min (ref.)	Avg (ref.)	Max (ref.)	Bioassay(s)
MSH	Drosophila melanogaster (fruit fly)	AC50	7.6300	0.2090	9.5788	48.6900	AID743444
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (14)

Process	via Protein(s)	Taxonomy
G protein-coupled receptor signaling pathway	Glycoprotein hormones alpha chain	Homo sapiens (human)
positive regulation of cell population proliferation	Glycoprotein hormones alpha chain	Homo sapiens (human)
hormone-mediated signaling pathway	Glycoprotein hormones alpha chain	Homo sapiens (human)
regulation of signaling receptor activity	Glycoprotein hormones alpha chain	Homo sapiens (human)
positive regulation of steroid biosynthetic process	Glycoprotein hormones alpha chain	Homo sapiens (human)
positive regulation of cell migration	Glycoprotein hormones alpha chain	Homo sapiens (human)
thyroid gland development	Glycoprotein hormones alpha chain	Homo sapiens (human)
luteinizing hormone secretion	Glycoprotein hormones alpha chain	Homo sapiens (human)
organ growth	Glycoprotein hormones alpha chain	Homo sapiens (human)
follicle-stimulating hormone signaling pathway	Glycoprotein hormones alpha chain	Homo sapiens (human)
positive regulation of transcription by RNA polymerase II	Glycoprotein hormones alpha chain	Homo sapiens (human)
negative regulation of organ growth	Glycoprotein hormones alpha chain	Homo sapiens (human)
follicle-stimulating hormone secretion	Glycoprotein hormones alpha chain	Homo sapiens (human)
thyroid hormone generation	Glycoprotein hormones alpha chain	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (3)

Process	via Protein(s)	Taxonomy
hormone activity	Glycoprotein hormones alpha chain	Homo sapiens (human)
protein binding	Glycoprotein hormones alpha chain	Homo sapiens (human)
follicle-stimulating hormone activity	Glycoprotein hormones alpha chain	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (5)

Process	via Protein(s)	Taxonomy
extracellular region	Glycoprotein hormones alpha chain	Homo sapiens (human)
extracellular space	Glycoprotein hormones alpha chain	Homo sapiens (human)
Golgi lumen	Glycoprotein hormones alpha chain	Homo sapiens (human)
follicle-stimulating hormone complex	Glycoprotein hormones alpha chain	Homo sapiens (human)
pituitary gonadotropin complex	Glycoprotein hormones alpha chain	Homo sapiens (human)
extracellular space	Glycoprotein hormones alpha chain	Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (20)

Assay ID	Title	Year	Journal	Article
AID651635	Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588497	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain F protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588499	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Botulinum neurotoxin light chain A protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745849	Viability Counterscreen for CMV-Luciferase Assay of Inhibitors of ATXN expression
AID1745847	CMV-Luciferase Counterscreen for Inhibitors of ATXN expression
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Current protocols in cytometry, Oct, Volume: Chapter 13	Microsphere-based flow cytometry protease assays for use in protease activity detection and high-throughput screening.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2006	Cytometry. Part A : the journal of the International Society for Analytical Cytology, May, Volume: 69, Issue:5	Microsphere-based protease assays and screening application for lethal factor and factor Xa.
AID588501	High-throughput multiplex microsphere screening for inhibitors of toxin protease, specifically Lethal Factor Protease, MLPCN compound set	2010	Assay and drug development technologies, Feb, Volume: 8, Issue:1	High-throughput multiplex flow cytometry screening for botulinum neurotoxin type a light chain protease inhibitors.
AID1745846	Firefly Luciferase Counterscreen for Inhibitors of ATXN expression
AID1745845	Primary qHTS for Inhibitors of ATXN expression
AID1745848	Confirmatory qHTS for Inhibitors of ATXN expression
AID1745850	Viability Counterscreen for Confirmatory qHTS for Inhibitors of ATXN expression
AID1281332	Cytotoxicity against human fibroblast cells assessed as viable cells at 10 uM by trypan blue staining based assay	2016	European journal of medicinal chemistry, Mar-03, Volume: 110	Ligand-based modeling of diverse aryalkylamines yields new potent P-glycoprotein inhibitors.
AID1281329	Cytotoxicity against human fibroblast cells assessed as viable cells at 50 uM by trypan blue staining based assay	2016	European journal of medicinal chemistry, Mar-03, Volume: 110	Ligand-based modeling of diverse aryalkylamines yields new potent P-glycoprotein inhibitors.
AID1281330	Cytotoxicity against human MCF7 cells assessed as viable cells at 50 uM by trypan blue staining based assay	2016	European journal of medicinal chemistry, Mar-03, Volume: 110	Ligand-based modeling of diverse aryalkylamines yields new potent P-glycoprotein inhibitors.
AID1281333	Cytotoxicity against human MCF7 cells assessed as viable cells at 10 uM by trypan blue staining based assay	2016	European journal of medicinal chemistry, Mar-03, Volume: 110	Ligand-based modeling of diverse aryalkylamines yields new potent P-glycoprotein inhibitors.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (10)

Timeframe	Studies, This Drug (%)	All Drugs %
pre-1990	0 (0.00)	18.7374
1990's	0 (0.00)	18.2507
2000's	4 (40.00)	29.6817
2010's	5 (50.00)	24.3611
2020's	1 (10.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 17.71

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.

Metric	This Compound (vs All)
Research Demand Index	17.71 (24.57)
Research Supply Index	1.79 (2.92)
Research Growth Index	4.32 (4.65)
Search Engine Demand Index	10.37 (26.88)
Search Engine Supply Index	2.00 (0.95)

This Compound (17.71)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Observational	0 (0.00%)	0.25%
Other	5 (100.00%)	84.16%
Other	5 (100.00%)	84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Substance	Relationship Strength	Studies	Classes	Roles
sb 202190 4-(4-fluorophenyl)-2-(4-hydroxyphenyl)-5-(4-pyridyl)imidazole: structure given in first source; inhibits p38 MAP kinase	2.03	1	imidazoles; organofluorine compound; phenols; pyridines	apoptosis inducer; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor
sb 203580 [no description available]	2.03	1	imidazoles; monofluorobenzenes; pyridines; sulfoxide	EC 2.7.11.1 (non-specific serine/threonine protein kinase) inhibitor; EC 2.7.11.24 (mitogen-activated protein kinase) inhibitor; geroprotector; Hsp90 inhibitor; neuroprotective agent
dx 52-1 DX 52-1: a quinocarmycin analog; structure given in first source	2.02	1
verapamil Verapamil: A calcium channel blocker that is a class IV anti-arrhythmia agent.. verapamil : A racemate comprising equimolar amounts of dexverapamil and (S)-verapamil. An L-type calcium channel blocker of the phenylalkylamine class, it is used (particularly as the hydrochloride salt) in the treatment of hypertension, angina pectoris and cardiac arrhythmia, and as a preventive medication for migraine.. 2-(3,4-dimethoxyphenyl)-5-{[2-(3,4-dimethoxyphenyl)ethyl](methyl)amino}-2-(propan-2-yl)pentanenitrile : A tertiary amino compound that is 3,4-dimethoxyphenylethylamine in which the hydrogens attached to the nitrogen are replaced by a methyl group and a 4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl group.	2.13	1	aromatic ether; nitrile; polyether; tertiary amino compound

Condition	Relationship Strength	Studies
Experimental Neoplasms [description not available]	2.07	1
Necrosis The death of cells in an organ or tissue due to disease, injury or failure of the blood supply.	2.07	1
Breast Cancer [description not available]	2.03	1
Adenocarcinoma Of Kidney [description not available]	2.03	1
Cancer of Kidney [description not available]	2.03	1
Breast Neoplasms Tumors or cancer of the human BREAST.	2.03	1
Carcinoma, Renal Cell A heterogeneous group of sporadic or hereditary carcinoma derived from cells of the KIDNEYS. There are several subtypes including the clear cells, the papillary, the chromophobe, the collecting duct, the spindle cells (sarcomatoid), or mixed cell-type carcinoma.	2.03	1
Kidney Neoplasms Tumors or cancers of the KIDNEY.	2.03	1
Innate Inflammatory Response [description not available]	2.05	1
Inflammation A pathological process characterized by injury or destruction of tissues caused by a variety of cytologic and chemical reactions. It is usually manifested by typical signs of pain, heat, redness, swelling, and loss of function.	2.05	1

chemdatabank.com