SCH 51344: inhibits ras transformation; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
SCH51344 : A pyrazoloquinoline that is 6-methoxy-3-methyl-1H-pyrazolo[3,4-b]quinoline bearing an additional 2-[(2-hydroxyethoxy)ethyl]amino substituent at position 4 [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 9995890 |
| CHEMBL ID | 3793901 |
| CHEBI ID | 77556 |
| MeSH ID | M0253854 |
| Synonym |
|---|
| 6-methoxy-4-(2-((2-hydroxyethoxyl)-ethyl)amino)-3-methyl-1h-pyrazolo[3,4-b]quinoline |
| ras/rac transformation blocker, sch 51344 |
| chembl3793901 , |
| bdbm50162076 |
| HMS3229N03 |
| 171927-40-5 |
| AKOS024458551 |
| CHEBI:77556 |
| 2-{2-[(6-methoxy-3-methyl-1h-pyrazolo[3,4-b]quinolin-4-yl)amino]ethoxy}ethanol |
| sch51344 |
| sch-51344 |
| 2-[2-[(6-methoxy-3-methyl-1h-pyrazolo[3,4-b]quinolin-4-yl)amino]ethoxy]ethanol |
| sch 51344 |
| DTXSID10433926 |
| AKOS027324122 |
| J-010781 |
| NCGC00384193-04 |
| BCP17385 |
| Q27147171 |
| 2-(2-((6-methoxy-3-methyl-1h-pyrazolo[3,4-b]quinolin-4-yl)amino)ethoxy)ethan-1-ol |
| 2-(2-((6-methoxy-3-methyl-1h-pyrazolo[3,4-b]quinolin-4-yl)amino)ethoxy)ethanol |
| AS-16962 |
| HMS3674M09 |
| EX-A4182 |
| 2-[2-[(6-methoxy-3-methyl-2h-pyrazolo[3,4-b]quinolin-4-yl)amino]ethoxy]ethanol |
| WGA92740 |
| CS-0012160 |
| HY-12656 |
| AC-36953 |
SCH 51344 is a pyrazolo-quinoline derivative identified based on its ability to derepress transformation sensitive alpha-actin promoter in RAS-transformed cells.
| Excerpt | Reference | Relevance |
|---|---|---|
| "SCH 51344 is a pyrazolo-quinoline derivative identified based on its ability to derepress transformation sensitive alpha-actin promoter in RAS-transformed cells." | ( SCH 51344-induced reversal of RAS-transformation is accompanied by the specific inhibition of the RAS and RAC-dependent cell morphology pathway. Bar-Sagi, D; Dhanasekaran, M; Kumar, CC; Walsh, AB, 1997) | 2.46 |
| "SCH 51344 is a pyrazoloquinoline derivative identified on the basis of its ability to derepress alpha-actin promoter in RAS-transformed cells." | ( SCH 51344, an inhibitor of RAS/RAC-mediated cell morphology pathway. Bar-Sagi, D; Kumar, CC; Mizuno, K; Nagata, K; Ohashi, K; Walsh, A, 1999) | 2.47 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "SCH 51344 treatment had very little effect, if any, on the activation of MAP kinase kinase, MAP kinase, and p90RSK activity in response to growth factor stimulation." | ( SCH 51344 inhibits ras transformation by a novel mechanism. Afonso, A; Armstrong, L; Dong, Z; Kelly, J; Kumar, CC; Kung, HF; Lin, JJ; Prorock-Rogers, C; Weber, MJ, 1995) | 2.46 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "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 |
| Role | Description |
|---|---|
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| pyrazoloquinoline | Any organic heterotricyclic compound that consists of a pyrazole ring ortho-fused to a quinoline. |
| aromatic ether | Any ether in which the oxygen is attached to at least one aryl substituent. |
| aromatic amine | An amino compound in which the amino group is linked directly to an aromatic system. |
| secondary amino compound | A compound formally derived from ammonia by replacing two hydrogen atoms by organyl groups. |
| primary alcohol | A primary alcohol is a compound in which a hydroxy group, -OH, is attached to a saturated carbon atom which has either three hydrogen atoms attached to it or only one other carbon atom and two hydrogen atoms attached to it. |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| PPM1D protein | Homo sapiens (human) | Potency | 4.1544 | 0.0052 | 9.4661 | 32.9993 | AID1347411 |
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 37.9083 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 23.9185 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 9.5221 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| Interferon beta | Homo sapiens (human) | Potency | 9.0954 | 0.0033 | 9.1582 | 39.8107 | AID1347411; AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 23.9185 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 23.9185 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 23.9185 | 0.0123 | 8.9648 | 39.8107 | AID1645842 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| 7,8-dihydro-8-oxoguanine triphosphatase | Homo sapiens (human) | IC50 (µMol) | 0.4137 | 0.0520 | 1.2093 | 5.6000 | AID1293607; AID1547864; AID1547865 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1347159 | Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347160 | Primary screen NINDS Rhodamine qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
| AID1293607 | Inhibition of recombinant human MTH1 expressed in Escherichia coli BL21 DE3 cells preincubated for 15 mins followed by 8-oxo-dGTP substrate addition measured after 15 mins by luminescence based assay | 2016 | Journal of medicinal chemistry, Mar-24, Volume: 59, Issue:6 | MutT Homolog 1 (MTH1): The Silencing of a Target. |
| AID1547866 | Cytotoxicity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by celltiter glo assay | 2020 | ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3 | Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation. |
| AID1547864 | Inhibition of human recombinant human His-tagged MTH1 expressed in Escherichia coli BL21 (DE3) using 8-oxo-dGTP as substrate incubated for 15 mins followed by substrate addition and measured after 15 mins by PPiLight Inorganic Pyrophosphate assay kit meth | 2020 | ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3 | Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation. |
| AID1547865 | Inhibition of human recombinant human His-tagged MTH1 expressed in Escherichia coli BL21 (DE3) using 8-oxo-dGTP as substrate incubated for 15 mins followed by substrate addition and measured after 3 hrs by PPiLight Inorganic Pyrophosphate assay kit method | 2020 | ACS medicinal chemistry letters, Mar-12, Volume: 11, Issue:3 | Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation. |
| AID1347411 | qHTS 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) Libary | 2020 | ACS 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. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 6 (42.86) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 4 (28.57) | 24.3611 |
| 2020's | 4 (28.57) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
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.
| This Compound (11.61) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 3 (21.43%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 11 (78.57%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||