Z-360: an orally-active CCK-2R antagonist for treatment of gastrointestinal cancer models; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9872609 |
| CHEMBL ID | 4303633 |
| SCHEMBL ID | 1556430 |
| MeSH ID | M0521364 |
| Synonym |
|---|
| gtpl907 |
| 3-[[(3r)-1-cyclohexyl-5-(3,3-dimethyl-2-oxobutyl)-4-oxo-2,3-dihydro-1,5-benzodiazepin-3-yl]carbamoylamino]benzoic acid |
| z-360 |
| nastorazepide [inn] |
| nastorazepide [who-dd] |
| r22tmy97sg , |
| z-360 free acid |
| r-(-)-z-360 free acid |
| benzoic acid, 3-(((((3r)-5-cyclohexyl-1-(3,3-dimethyl-2-oxobutyl)-2,3,4,5-tetrahydro-2-oxo-1h-1,5-benzodiazepin-3-yl)amino)carbonyl)amino)- |
| 209219-38-5 |
| unii-r22tmy97sg |
| nastorazepide |
| CS-5383 |
| HY-17617 |
| VIJCCFFEBCOOIE-JOCHJYFZSA-N |
| (r)-(-)-3-[3-(1-tert-butylcarbonylmethyl-2-oxo-5-cyclohexyl-1,3,4,5-tetrahydro-2h-1,5-benzodiazepin-3-yl)ureido]benzoic acid |
| SCHEMBL1556430 |
| (r)-3-(3-(5-cyclohexyl-1-(3,3-dimethyl-2-oxobutyl)-2-oxo-2,3,4,5-tetrahydro-1h-benzo[b][1,4]diazepin-3-yl)ureido)benzoic acid |
| NCGC00485486-01 |
| A924416 |
| nastorazepide (z-360) |
| Q27089277 |
| CHEMBL4303633 |
| z360; nastorazepide |
| EX-A1929 |
| D87151 |
| MS-29658 |
| GLXC-11296 |
| AC-36256 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Z-360 is safe and well tolerated when combined with gemcitabine." | ( A phase Ib/IIa trial to evaluate the CCK2 receptor antagonist Z-360 in combination with gemcitabine in patients with advanced pancreatic cancer. Borbath, I; Caplin, ME; Coxon, F; Kato, H; Larvin, M; Meyer, T; Nagano, E; Palmer, DH; Peeters, M; Valle, JW; Waters, JS, 2010) | 2.04 |
| 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 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| 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. |
| 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. |
| 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. |
| 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. |
| AID1346883 | Human CCK2 receptor (Cholecystokinin receptors) | 2008 | Cancer chemotherapy and pharmacology, Apr, Volume: 61, Issue:5 | Effect of Z-360, a novel orally active CCK-2/gastrin receptor antagonist on tumor growth in human pancreatic adenocarcinoma cell lines in vivo and mode of action determinations in vitro. |
| 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 | 0 (0.00) | 18.2507 |
| 2000's | 2 (13.33) | 29.6817 |
| 2010's | 10 (66.67) | 24.3611 |
| 2020's | 3 (20.00) | 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 strong demand-to-supply ratio for research on this compound.
| This Compound (47.79) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 2 (13.33%) | 5.53% |
| Reviews | 1 (6.67%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 12 (80.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||