Page last updated: 2024-11-13

lys01

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Description

Lys01: an autophagy inhibitor with antineoplastic activity; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID Source	ID
PubMed CID	70673567
CHEMBL ID	4282488
SCHEMBL ID	15483264
MeSH ID	M0575768

Synonyms (18)

Synonym
SCHEMBL15483264
1391426-22-4
EX-A1202
n-(7-chloroquinolin-4-yl)-n'-[2-[(7-chloroquinolin-4-yl)amino]ethyl]-n'-methylethane-1,2-diamine
AKOS027447180
n2-(7-chloro-4-quinolinyl)-n1-[2-[(7-chloro-4-quinolinyl)amino]ethyl]-n1-methyl-1,2-ethanediamine
mfcd28127224
n1-(7-chloroquinolin-4-yl)-n2-(2-((7-chloroquinolin-4-yl)amino)ethyl)-n2-methylethane-1,2-diamine
BCP18908
lys-01; lys 01
lys05 (free base)
lys01
compound 3a [pmid: 30344903]
gtpl10320
1391426-22-4 (free base)
lys01 free base
1,2-ethanediamine, n2-(7-chloro-4-quinolinyl)-n1-[2-[(7-chloro-4-quinolinyl)amino]ethyl]-n1-methyl-
CHEMBL4282488

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

Bioassays (20)

Assay ID	Title	Year	Journal	Article
AID1765951	Inhibition of autophagy in human A375P cells assessed as fold change in BNIP3 at 3 uM incubated for 24 hrs by immunoblot analysis relative to control	2021	Bioorganic & medicinal chemistry letters, 10-01, Volume: 49	Anticancer properties of bisaminoquinolines with modified linkers.
AID1422825	Potency index, ratio of chloroquine IC50 to compound IC50 for antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.
AID1422834	Inhibition of Plasmodium falciparum FCR-3 HDP expressed in Escherichia coli assessed as reduction in hemazoin formation	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.
AID1765953	Inhibition of autophagy in human A375P cells assessed as fold change in LC3BII/ LC3BI ratio at 3 uM incubated for 24 hrs by immunoblot analysis relative to control	2021	Bioorganic & medicinal chemistry letters, 10-01, Volume: 49	Anticancer properties of bisaminoquinolines with modified linkers.
AID1765958	Inhibition of autophagy in human A375P cells assessed as fold change in LC3BII/ LC3BI ratio at 10 uM incubated for 24 hrs by immunoblot analysis relative to control	2021	Bioorganic & medicinal chemistry letters, 10-01, Volume: 49	Anticancer properties of bisaminoquinolines with modified linkers.
AID1422827	Antimalarial activity against Plasmodium berghei N infected in mouse assessed as inhibition of parasitemia at 30 mg/kg, po once daily for 4 consecutive days starting from 2 hrs post infection measured on day 4 post last dose relative to control	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.
AID1765960	Inhibition of autophagy in human A375P cells harbouring mCherry-egfp-LC3B assessed as autophagic flux by measuring yellow puncta at 10 uM incubated for 24 hrs by fluorescence microscopy relative to control	2021	Bioorganic & medicinal chemistry letters, 10-01, Volume: 49	Anticancer properties of bisaminoquinolines with modified linkers.
AID1765952	Inhibition of autophagy in human A375P cells assessed as fold change in p62 at 3 uM incubated for 24 hrs by immunoblot analysis relative to control	2021	Bioorganic & medicinal chemistry letters, 10-01, Volume: 49	Anticancer properties of bisaminoquinolines with modified linkers.
AID1422821	Antiplasmodial activity against chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes measured after 72 hrs by malstat reagent based LDH release assay	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.
AID1765959	Inhibition of autophagy in human A375P cells assessed as fold change in H2AX at 10 uM incubated for 24 hrs by immunoblot analysis relative to control	2021	Bioorganic & medicinal chemistry letters, 10-01, Volume: 49	Anticancer properties of bisaminoquinolines with modified linkers.
AID1422830	Antimalarial activity against Plasmodium berghei N infected in mouse assessed as mouse survival at 30 mg/kg, po once daily for 4 consecutive days starting from 2 hrs post infection relative to control	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.
AID1765957	Inhibition of autophagy in human A375P cells assessed as fold change in p62 at 10 uM incubated for 24 hrs by immunoblot analysis relative to control	2021	Bioorganic & medicinal chemistry letters, 10-01, Volume: 49	Anticancer properties of bisaminoquinolines with modified linkers.
AID1422829	Antimalarial activity against Plasmodium berghei N infected in mouse assessed as mouse survival at 30 mg/kg, sc once daily for 4 consecutive days starting from 2 hrs post infection relative to control	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.
AID1422833	Binding affinity to hemin assessed as protection against H2O2-induced hemin degradation up to 100 uM at pH 5.2 preincubated followed by H2O2 addition measured after 120 mins	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.
AID1765954	Cytotoxicity against human A375P cells incubated for 72 hrs by MTT assay	2021	Bioorganic & medicinal chemistry letters, 10-01, Volume: 49	Anticancer properties of bisaminoquinolines with modified linkers.
AID1765956	Inhibition of autophagy in human A375P cells assessed as fold change in BNIP3 at 10 uM incubated for 24 hrs by immunoblot analysis relative to control	2021	Bioorganic & medicinal chemistry letters, 10-01, Volume: 49	Anticancer properties of bisaminoquinolines with modified linkers.
AID1422826	Antimalarial activity against Plasmodium berghei N infected in mouse assessed as inhibition of parasitemia at 30 mg/kg, sc once daily for 4 consecutive days starting from 2 hrs post infection measured on day 4 post last dose relative to control	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.
AID1422822	Antiplasmodial activity against chloroquine-sensitive Plasmodium falciparum FCR-3 infected in human erythrocytes measured after 72 hrs by malstat reagent based LDH release assay	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.
AID1422823	Cytotoxicity against human MRC5 cells after 7 days by MTT assay	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.
AID1422824	Selectivity index, ratio of cytotoxic concentration for human MRC5 cells to IC50 for chloroquine-resistant Plasmodium falciparum K1 infected in human erythrocytes	2018	ACS medicinal chemistry letters, Oct-11, Volume: 9, Issue:10	Potent Antimalarial Activity of Two Arenes Linked with Triamine Designed To Have Multiple Interactions with Heme.
[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	0 (0.00)	29.6817
2010's	6 (60.00)	24.3611
2020's	4 (40.00)	2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 12.16

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.

Metric	This Compound (vs All)
Research Demand Index	12.16 (24.57)
Research Supply Index	2.48 (2.92)
Research Growth Index	4.64 (4.65)
Search Engine Demand Index	0.00 (26.88)
Search Engine Supply Index	0.00 (0.95)

This Compound (12.16)

All Compounds (24.57)

Study Types

Publication Type	This drug (%)	All Drugs (%)
Trials	0 (0.00%)	5.53%
Reviews	0 (0.00%)	6.00%
Case Studies	0 (0.00%)	4.05%
Observational	0 (0.00%)	0.25%
Other	11 (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
chloroquine Chloroquine: The prototypical antimalarial agent with a mechanism that is not well understood. It has also been used to treat rheumatoid arthritis, systemic lupus erythematosus, and in the systemic therapy of amebic liver abscesses.. chloroquine : An aminoquinoline that is quinoline which is substituted at position 4 by a [5-(diethylamino)pentan-2-yl]amino group at at position 7 by chlorine. It is used for the treatment of malaria, hepatic amoebiasis, lupus erythematosus, light-sensitive skin eruptions, and rheumatoid arthritis.	2.17	1	aminoquinoline; organochlorine compound; secondary amino compound; tertiary amino compound	anticoronaviral agent; antimalarial; antirheumatic drug; autophagy inhibitor; dermatologic drug
hydroxychloroquine Hydroxychloroquine: A chemotherapeutic agent that acts against erythrocytic forms of malarial parasites. Hydroxychloroquine appears to concentrate in food vacuoles of affected protozoa. It inhibits plasmodial heme polymerase. (From Gilman et al., Goodman and Gilman's The Pharmacological Basis of Therapeutics, 9th ed, p970). hydroxychloroquine : An aminoquinoline that is chloroquine in which one of the N-ethyl groups is hydroxylated at position 2. An antimalarial with properties similar to chloroquine that acts against erythrocytic forms of malarial parasites, it is mainly used as the sulfate salt for the treatment of lupus erythematosus, rheumatoid arthritis, and light-sensitive skin eruptions.	2.81	3	aminoquinoline; organochlorine compound; primary alcohol; secondary amino compound; tertiary amino compound	anticoronaviral agent; antimalarial; antirheumatic drug; dermatologic drug
pyrroles 1H-pyrrole : A tautomer of pyrrole that has the double bonds at positions 2 and 4.. pyrrole : A five-membered monocyclic heteroarene comprising one NH and four CH units which forms the parent compound of the pyrrole group of compounds. Its five-membered ring structure has three tautomers. A 'closed class'.. azole : Any monocyclic heteroarene consisting of a five-membered ring containing nitrogen. Azoles can also contain one or more other non-carbon atoms, such as nitrogen, sulfur or oxygen.	2.15	1	pyrrole; secondary amine
quinine [no description available]	2.17	1	cinchona alkaloid	antimalarial; muscle relaxant; non-narcotic analgesic
su 11248 [no description available]	2.15	1	monocarboxylic acid amide; pyrroles	angiogenesis inhibitor; antineoplastic agent; EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor; immunomodulator; neuroprotective agent; vascular endothelial growth factor receptor antagonist
artesunate artesunic acid: RN given for (3R-(3alpha,5abeta,6beta,8abeta,9alpha,10alpha,12beta,(2aR*))-isomer; succinic ester of artemether	2.17	1	artemisinin derivative; cyclic acetal; dicarboxylic acid monoester; hemisuccinate; semisynthetic derivative; sesquiterpenoid	antimalarial; antineoplastic agent; ferroptosis inducer
dactolisib dactolisib: antineoplastic agent that inhibits both phosphatidylinositol 3-kinase and mTOR. dactolisib : An imidazoquinoline that is 3-methyl-2-oxo-2,3-dihydro-1H-imidazo[4,5-c]quinoline substituted at position 1 by a 4-(1-cyanoisopropyl)phenyl group and at position 8 by a quinolin-3-yl group. A dual PI3K/mTOR inhibitor used in cancer treatment.	2.6	1	imidazoquinoline; nitrile; quinolines; ring assembly; ureas	antineoplastic agent; EC 2.7.1.137 (phosphatidylinositol 3-kinase) inhibitor; mTOR inhibitor

Condition	Relationship Strength	Studies
Canine Diseases [description not available]	2.6	1
Osteogenic Sarcoma [description not available]	2.6	1
Osteosarcoma A sarcoma originating in bone-forming cells, affecting the ends of long bones. It is the most common and most malignant of sarcomas of the bones, and occurs chiefly among 10- to 25-year-old youths. (From Stedman, 25th ed)	2.6	1
Astrocytoma, Grade IV [description not available]	2.53	2
Glioblastoma A malignant form of astrocytoma histologically characterized by pleomorphism of cells, nuclear atypia, microhemorrhage, and necrosis. They may arise in any region of the central nervous system, with a predilection for the cerebral hemispheres, basal ganglia, and commissural pathways. Clinical presentation most frequently occurs in the fifth or sixth decade of life with focal neurologic signs or seizures.	2.53	2
Malignant Melanoma [description not available]	2.15	1
Melanoma A malignant neoplasm derived from cells that are capable of forming melanin, which may occur in the skin of any part of the body, in the eye, or, rarely, in the mucous membranes of the genitalia, anus, oral cavity, or other sites. It occurs mostly in adults and may originate de novo or from a pigmented nevus or malignant lentigo. Melanomas frequently metastasize widely, and the regional lymph nodes, liver, lungs, and brain are likely to be involved. The incidence of malignant skin melanomas is rising rapidly in all parts of the world. (Stedman, 25th ed; from Rook et al., Textbook of Dermatology, 4th ed, p2445)	2.15	1
Granulocytic Leukemia, Chronic [description not available]	2.21	1
Leukemia, Myelogenous, Chronic, BCR-ABL Positive Clonal hematopoetic disorder caused by an acquired genetic defect in PLURIPOTENT STEM CELLS. It starts in MYELOID CELLS of the bone marrow, invades the blood and then other organs. The condition progresses from a stable, more indolent, chronic phase (LEUKEMIA, MYELOID, CHRONIC PHASE) lasting up to 7 years, to an advanced phase composed of an accelerated phase (LEUKEMIA, MYELOID, ACCELERATED PHASE) and BLAST CRISIS.	2.21	1
Epithelial Ovarian Cancer [description not available]	2.15	1
Epithelial Neoplasms [description not available]	2.15	1
Cancer of Ovary [description not available]	2.15	1
Carcinoma, Ovarian Epithelial A malignant neoplasm that originates in cells on the surface EPITHELIUM of the ovary and is the most common form of ovarian cancer. There are five histologic subtypes: papillary serous, endometrioid, mucinous, clear cell, and transitional cell. Mutations in BRCA1, OPCML, PRKN, PIK3CA, AKT1, CTNNB1, RRAS2, and CDH1 genes are associated with this cancer.	2.15	1
Ovarian Neoplasms Tumors or cancer of the OVARY. These neoplasms can be benign or malignant. They are classified according to the tissue of origin, such as the surface EPITHELIUM, the stromal endocrine cells, and the totipotent GERM CELLS.	2.15	1
Adenocarcinoma, Clear Cell An adenocarcinoma characterized by the presence of varying combinations of clear and hobnail-shaped tumor cells. There are three predominant patterns described as tubulocystic, solid, and papillary. These tumors, usually located in the female reproductive organs, have been seen more frequently in young women since 1970 as a result of the association with intrauterine exposure to diethylstilbestrol. (From Holland et al., Cancer Medicine, 3d ed)	2.15	1
Adenocarcinoma, Basal Cell [description not available]	2.07	1
Benign Neoplasms, Brain [description not available]	2.07	1
Cancer of Colon [description not available]	2.07	1
Adenocarcinoma A malignant epithelial tumor with a glandular organization.	2.07	1
Brain Neoplasms Neoplasms of the intracranial components of the central nervous system, including the cerebral hemispheres, basal ganglia, hypothalamus, thalamus, brain stem, and cerebellum. Brain neoplasms are subdivided into primary (originating from brain tissue) and secondary (i.e., metastatic) forms. Primary neoplasms are subdivided into benign and malignant forms. In general, brain tumors may also be classified by age of onset, histologic type, or presenting location in the brain.	2.07	1
Colonic Neoplasms Tumors or cancer of the COLON.	2.07	1
Intestinal Obstruction Any impairment, arrest, or reversal of the normal flow of INTESTINAL CONTENTS toward the ANAL CANAL.	2.07	1

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