SSR180575: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 9930560 |
| CHEMBL ID | 517539 |
| SCHEMBL ID | 197375 |
| MeSH ID | M0427330 |
| Synonym |
|---|
| ssr180575 |
| ssr 180575 |
| (7-chloro-n,n,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4h-pyridazino[4,5-b]indole-1-acetamide) |
| bdbm50255226 |
| (7-chloro-n,n,5-trimethyl-4-oxo-3-phenyl-3,5-dihydro-4h-pyridozino[4,5-b]indole-1-acetamide) |
| sr-180575 |
| CHEMBL517539 , |
| 2-(7-chloro-5-methyl-4-oxo-3-phenyl-4,5-dihydro-3h-pyridazino[4,5-b]indol-1-yl)-n,n-dimethylacetamide |
| 220448-02-2 |
| ssr-180,575 |
| SCHEMBL197375 |
| MB03473 |
| ssr-180575 |
| DTXSID10433007 |
| 7-chloro-4,5-dihydro-n,n,5-trimethyl-4-oxo-3-phenyl-3h-pyridazino[4,5-b]indole-1-acetamide |
| 7-chloro-4,5-dihydro-n,n,5-trimethyl-4-oxo-3-phenyl-3h-pyridazino(4,5-b)indole-1-acetamide |
| 4K8W47WK2L , |
| 3h-pyridazino(4,5-b)indole-1-acetamide, 7-chloro-4,5-dihydro-n,n,5-trimethyl-4-oxo-3-phenyl- |
| unii-4k8w47wk2l |
| FT-0751759 |
| 7-chloro-n,n-dimethyl-5-methyl-4-oxo-3-phenyl-3,5-dihydro-4h-pyridazino[4,5-b]indole-1-acetamide |
| Q7393049 |
| 2-(7-chloro-5-methyl-4-oxo-3-phenylpyridazino[4,5-b]indol-1-yl)-n,n-dimethylacetamide |
SSR180575 (1) is a high-affinity (0.83 nM) TSPO 18 kDa ligand belonging to the pyridazino[4,5-b]indole-1-acetamides family.
| Excerpt | Reference | Relevance |
|---|---|---|
| "SSR180575 (1) is a high-affinity (0.83 nM) TSPO 18 kDa ligand belonging to the pyridazino[4,5-b]indole-1-acetamides family. " | ( Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575. Damont, A; Dollé, F; Marguet, F; Puech, F, 2015) | 2.08 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Translocator protein | Rattus norvegicus (Norway rat) | Kd | 0.0030 | 0.0006 | 0.8283 | 4.0000 | AID368147 |
| Translocator protein | Homo sapiens (human) | Kd | 0.0031 | 0.0011 | 0.0048 | 0.0111 | AID368147; AID408746 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| androgen binding | Translocator protein | Homo sapiens (human) |
| protein binding | Translocator protein | Homo sapiens (human) |
| benzodiazepine receptor activity | Translocator protein | Homo sapiens (human) |
| cholesterol binding | Translocator protein | Homo sapiens (human) |
| transmembrane transporter binding | Translocator protein | Homo sapiens (human) |
| cholesterol transfer activity | Translocator protein | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| mitochondrion | Translocator protein | Homo sapiens (human) |
| mitochondrial outer membrane | Translocator protein | Homo sapiens (human) |
| cytosol | Translocator protein | Homo sapiens (human) |
| intracellular membrane-bounded organelle | Translocator protein | Homo sapiens (human) |
| extracellular exosome | Translocator protein | Homo sapiens (human) |
| endoplasmic reticulum | Translocator protein | Homo sapiens (human) |
| membrane | Translocator protein | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1244455 | Selectivity for rat heart membrane TSPO over rat cerebral cortex CBR | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575. |
| AID1244460 | Solubility in 50 mM phosphate buffer at pH 7.4 after 20 hrs by HPLC method | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575. |
| AID408746 | Binding affinity to human PBR | 2008 | Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11 | Synthesis, fluorine-18 radiolabeling, and in vitro characterization of 1-iodophenyl-N-methyl-N-fluoroalkyl-3-isoquinoline carboxamide derivatives as potential PET radioligands for imaging peripheral benzodiazepine receptor. |
| AID1244459 | Biotransformation in human liver microsomes at 5 uM measured at 20 mins by HPLC/ESI-MS/MS analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575. |
| AID1244454 | n-octanol/buffer partition coefficient, log D of the compound at pH 7.4 by HPLC method | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575. |
| AID368147 | Displacement of [3H]SSR180575 from TSPO in rat cortex | 2009 | Journal of medicinal chemistry, Feb-12, Volume: 52, Issue:3 | The translocator protein (18 kDa): central nervous system disease and drug design. |
| AID1244456 | Displacement of [3H]-PK11195 from rat heart membrane TSPO | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575. |
| AID1244453 | Inhibition of [3H]-flunitrazepam binding to rat cerebral cortex CBR at 1 uM | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575. |
| AID1244457 | Biotransformation in CD1 mouse liver microsomes at 5 uM measured at 20 mins by HPLC/ESI-MS/MS analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575. |
| AID1244458 | Biotransformation in Sprague-Dawley rat liver microsomes at 5 uM measured at 20 mins by HPLC/ESI-MS/MS analysis | 2015 | European journal of medicinal chemistry, Aug-28, Volume: 101 | Synthesis and in vitro characterization of novel fluorinated derivatives of the TSPO 18 kDa ligand SSR180575. |
| [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 | 7 (58.33) | 29.6817 |
| 2010's | 5 (41.67) | 24.3611 |
| 2020's | 0 (0.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (8.33%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 11 (91.67%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||