| ID Source | ID |
|---|---|
| PubMed CID | 90642938 |
| CHEMBL ID | 4072005 |
| SCHEMBL ID | 23607667 |
| MeSH ID | M000613463 |
| Synonym |
|---|
| S7832 |
| CS-5370 |
| HY-19715 |
| SGC707 , |
| 1687736-54-4 |
| AKOS025142099 |
| sgc 707 |
| 1-(isoquinolin-6-yl)-3-[2-oxo-2-(pyrrolidin-1-yl)ethyl] urea |
| AC-35319 |
| gtpl8552 |
| 1-isoquinolin-6-yl-3-(2-oxo-2-pyrrolidin-1-ylethyl)urea |
| 1-isoquinolin-6-yl-3-[2-oxo-2-(pyrrolidin-1-yl)ethyl]urea |
| 3zg , |
| J-690235 |
| n-{2-[(2-oxo-3-azepanyl)carbamoyl]phenyl}-1-benzothiophene-2-carboxamide |
| EX-A1304 |
| 1-(isoquinolin-6-yl)-3-[2-oxo-2-(pyrrolidin-1-yl)ethyl]urea |
| sgc707, >=98% (hplc) |
| n-6-isoquinolinyl-n'-[2-oxo-2-(1-pyrrolidinyl)ethyl]-urea |
| mfcd28411624 |
| NCGC00384204-04 |
| sgc-707 |
| bdbm50247349 |
| FT-0700238 |
| BCP16746 |
| Q27088792 |
| AS-16917 |
| urea, n-6-isoquinolinyl-n'-[2-oxo-2-(1-pyrrolidinyl)ethyl]- |
| CHEMBL4072005 , |
| CCG-267447 |
| 1-(isoquinolin-6-yl)-3-(2-oxo-2-(pyrrolidin-1-yl)ethyl)urea |
| NCGC00384204-01 |
| EN300-215410 |
| SCHEMBL23607667 |
SGC707 is a potent PRMT3 inhibitor. It has outstanding selectivity (selective against 31 other methyltransferases and more than 250 non-epigenetic targets)
| Excerpt | Reference | Relevance |
|---|---|---|
| "SGC707 is a potent PRMT3 inhibitor (IC50 =31±2 nM, KD =53±2 nM) with outstanding selectivity (selective against 31 other methyltransferases and more than 250 non-epigenetic targets)." | ( A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). Arrowsmith, CH; Atadja, P; Barsyte-Lovejoy, D; Brown, PJ; Dai, M; Dobrovetsky, E; Dong, A; Eram, MS; He, F; Huang, XP; Jin, J; Kaniskan, HÜ; Kennedy, S; Landon, M; Li, F; Lin, Y; Lin-Jones, J; Luo, X; Min, SJ; Roth, BL; Schapira, M; Schmidt, K; Smil, D; Szewczyk, MM; Vedadi, M; Yang, X; Yu, Z; Zang, I; Zhao, K, 2015) | 1.14 |
SGC707-treated mice exhibited 50% lower liver triglyceride stores as well as 32% lower plasma triglyceride levels. Treatment with SGC707 did not negatively influence the T0901317/palm oil-induced up-regulation of the cholesterol efflux ATP-binding cassette transporter genes.
| Excerpt | Reference | Relevance |
|---|---|---|
| "SGC707-treated mice exhibited 50% lower liver triglyceride stores as well as 32% lower plasma triglyceride levels." | ( PRMT3 inhibitor SGC707 reduces triglyceride levels and induces pruritus in Western-type diet-fed LDL receptor knockout mice. de Jong, LM; den Hartog, Y; Hankemeier, T; Hoekstra, M; Lindenburg, PW; Manson, ML; Martins Cardoso, R; Salvatori, DCF; Sijsenaar, TJP; Van Eck, M; Zhang, Z, 2022) | 1.79 |
| "Treatment with SGC707 did not negatively influence the T0901317/palm oil-induced up-regulation of the cholesterol efflux ATP-binding cassette transporter genes, ABCA1 and ABCG1, in peritoneal cells. " | ( Inhibition of protein arginine methyltransferase 3 activity selectively impairs liver X receptor-driven transcription of hepatic lipogenic genes in vivo. Geerling, JJ; Groeneveldt, C; Hoekstra, M; Nahon, JE; van Eck, M, 2018) | 0.83 |
| 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 |
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 1.6933 | 0.0123 | 7.9835 | 43.2770 | AID1645841 |
| cytochrome P450 2D6 | Homo sapiens (human) | Potency | 11.9877 | 0.0010 | 8.3798 | 61.1304 | AID1645840 |
| [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) |
|---|---|---|---|---|---|---|---|
| Protein arginine N-methyltransferase 3 | Homo sapiens (human) | IC50 (µMol) | 0.1065 | 0.0190 | 1.2995 | 7.1000 | AID1472768; AID1472771; AID1472772; AID1913048 |
| [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) |
|---|---|---|---|---|---|---|---|
| Protein arginine N-methyltransferase 3 | Homo sapiens (human) | EC50 (µMol) | 1.9000 | 1.8000 | 1.9000 | 2.0000 | AID1472769; AID1472770 |
| Protein arginine N-methyltransferase 3 | Homo sapiens (human) | Kd | 0.0690 | 0.0530 | 0.0690 | 0.0850 | AID1913355; AID1915360 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| negative regulation of protein ubiquitination | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| methylation | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| negative regulation of retinoic acid biosynthetic process | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| peptidyl-arginine methylation, to asymmetrical-dimethyl arginine | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| chromatin remodeling | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| protein methylation | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| protein binding | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| methyltransferase activity | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| protein-arginine N-methyltransferase activity | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| protein-arginine omega-N monomethyltransferase activity | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| protein-arginine omega-N asymmetric methyltransferase activity | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| ribosome binding | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| metal ion binding | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| histone methyltransferase activity | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| cytoplasm | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| cytosol | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| nucleus | Protein arginine N-methyltransferase 3 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1654634 | Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs by LC-MS analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model. |
| AID1654632 | Substrate activity at aldehyde oxidase in human liver cytosol at 10 uM measured after 3 hrs by UPLC/Q-TOF MS analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model. |
| AID1472769 | Binding affinity to beta galactosidase fused human PRMT3 (211 to 531 residues) expressed in human A549 cells after 6 hrs by InCELL hunter assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3). |
| AID1472771 | Inhibition of FLAG-tagged wild type human PRMT3 expressed in HEK293 cells assessed as reduction in endogenous H4R3me2a level using GFP-tagged histone H4 as substrate after 24 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3). |
| AID1654637 | Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs in presence of AOX inhibitor hydralazine by UPLC/Q-TOF MS analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model. |
| AID1549214 | Inhibition of PRMT3 (unknown origin) expressed in HEK293T cells were co-transfected with GFP-tagged histone H4 peptide assessed as reduction in H4R3 arginine asymmetric dimethylation at 1 uM incubated for 20 hrs | 2020 | Journal of medicinal chemistry, 05-28, Volume: 63, Issue:10 | Discovery of a First-in-Class Protein Arginine Methyltransferase 6 (PRMT6) Covalent Inhibitor. |
| AID1472772 | Inhibition of FLAG-tagged wild type human PRMT3 expressed in HEK293 cells assessed as decrease in exogenous H4R3 dimethylation level using GFP-tagged histone H4 as substrate after 24 hrs by Western blot analysis | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3). |
| AID1654635 | Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs by UPLC/Q-TOF MS analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model. |
| AID1654638 | Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs in presence of XO inhibitor allopurinol by UPLC/Q-TOF MS analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model. |
| AID1472768 | Inhibition of PRMT3 (unknown origin) using C-terminally biotinylated histone H4 as substrate in presence of [3H]S-adenosylmethionine by scintillation proximity assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3). |
| AID1654636 | Substrate activity at aldehyde oxidase in human liver cytosol assessed as mono-oxide metabolite formation at 10 uM measured after 3 hrs in presence of AOX inhibitor raloxifene by UPLC/Q-TOF MS analysis | 2020 | Journal of medicinal chemistry, 06-25, Volume: 63, Issue:12 | Revisiting Aldehyde Oxidase Mediated Metabolism in Drug-like Molecules: An Improved Computational Model. |
| AID1472770 | Binding affinity to beta galactosidase fused human PRMT3 (211 to 531 residues) expressed in human HEK293 cells after 6 hrs by InCELL hunter assay | 2018 | Journal of medicinal chemistry, 02-08, Volume: 61, Issue:3 | Discovery of Potent and Selective Allosteric Inhibitors of Protein Arginine Methyltransferase 3 (PRMT3). |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| AID1345237 | Human protein arginine methyltransferase 3 (2.1.1.- Protein arginine N-methyltransferases) | 2015 | Angewandte Chemie (International ed. in English), Apr-20, Volume: 54, Issue:17 | A potent, selective and cell-active allosteric inhibitor of protein arginine methyltransferase 3 (PRMT3). |
| [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 | 0 (0.00) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 6 (46.15) | 24.3611 |
| 2020's | 7 (53.85) | 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 moderate demand-to-supply ratio for research on this compound.
| This Compound (19.53) All Compounds (24.57) |
| 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 | 13 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||