NK 252: potentiates the action of antitumor drugs against drug-sensitive tumors; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 71618700 |
| CHEMBL ID | 4164286 |
| MeSH ID | M0182372 |
| Synonym |
|---|
| nk-252 |
| nk 252 |
| AKOS025147343 |
| 1414963-82-8 |
| n-[5-(2-furanyl)-1,3,4-oxadiazol-2-yl]-n'-(2-pyridinylmethyl)urea |
| CS-5458 |
| HY-19734 |
| EX-A5283 |
| NCGC00387474-01 |
| 1-(5-(furan-2-yl)-1,3,4-oxadiazol-2-yl)-3-(pyridin-2-ylmethyl)urea , |
| 1-[5-(furan-2-yl)-1,3,4-oxadiazol-2-yl]-3-(pyridin-2-ylmethyl)urea |
| n-[5-(2-furanyl)-1,3,4-oxadiazol-2-yl]-n inverted exclamation marka-(2-pyridinylmethyl)-urea |
| n-[5-(2-furanyl)-1,3,4-oxadiazol-2-yl]-n'-(2-pyridinylmethyl)-urea |
| BS-52158 |
| CHEMBL4164286 |
| DTXSID301020703 |
| E85084 |
| 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 | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Kelch-like ECH-associated protein 1 | Homo sapiens (human) | Ki | 800.0000 | 0.5600 | 0.5600 | 0.5600 | AID1577815 |
| [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) |
|---|---|---|---|---|---|---|---|
| Kelch-like ECH-associated protein 1 | Homo sapiens (human) | EC50 (µMol) | 800.0000 | 0.8700 | 2.7600 | 5.1100 | AID1577808 |
| Kelch-like ECH-associated protein 1 | Homo sapiens (human) | Kd | 452.0000 | 1.0000 | 1.7667 | 2.4000 | AID1577810 |
| [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) |
|---|---|---|---|---|---|---|---|
| Kelch-like ECH-associated protein 1 | Homo sapiens (human) | EC2 (µMol) | 1.3600 | 1.3600 | 1.3600 | 1.3600 | AID1354588 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| protein binding | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| identical protein binding | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| RNA polymerase II-specific DNA-binding transcription factor binding | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| disordered domain specific binding | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| ubiquitin-like ligase-substrate adaptor activity | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| transcription factor binding | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Process | via Protein(s) | Taxonomy |
|---|---|---|
| nucleoplasm | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| cytoplasm | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| endoplasmic reticulum | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| cytosol | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| actin filament | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| inclusion body | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| midbody | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| centriolar satellite | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| Cul3-RING ubiquitin ligase complex | Kelch-like ECH-associated protein 1 | Homo sapiens (human) |
| [Information is prepared from geneontology information from the June-17-2024 release] | ||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1577808 | Binding affinity to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) assessed as thermal stabilization by sypro orange dye based thermal shift assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
| AID1354588 | Activation of human GST-tagged Keap1-DC (321 to 609 residues) expressed in human Huh transformed cells after 16 hrs by ARE-based steady-glo luciferase reporter gene assay | 2018 | Journal of medicinal chemistry, 09-27, Volume: 61, Issue:18 | Non-covalent Small-Molecule Kelch-like ECH-Associated Protein 1-Nuclear Factor Erythroid 2-Related Factor 2 (Keap1-Nrf2) Inhibitors and Their Potential for Targeting Central Nervous System Diseases. |
| AID1577815 | Inhibition of Cys5-LDEETGEFL-NH2 binding to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) measured after 10 to 15 mins by fluorescence polarization assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
| AID1577839 | Redox cycling activity of the compound assessed as H2O2 production measured after 15 mins in presence of TCEP by phenol red reagent based horseradish peroxidase coupled assay | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
| AID1577813 | Binding affinity to Keap1 in mouse Hepa1c1c7 cells assessed as reduction in Keap1 interaction by measuring induction of NQO1 activity at 1 to 10 uM measured after 24 hrs | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
| AID1577810 | Binding affinity to recombinant human KEAP1 Kelch domain (321 to 609 residues) expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance analysis | 2019 | Journal of medicinal chemistry, 09-12, Volume: 62, Issue:17 | A Comparative Assessment Study of Known Small-Molecule Keap1-Nrf2 Protein-Protein Interaction Inhibitors: Chemical Synthesis, Binding Properties, and Cellular Activity. |
| 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. |
| 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. |
| 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. |
| 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. |
| 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. |
| [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 | 3 (27.27) | 18.2507 |
| 2000's | 0 (0.00) | 29.6817 |
| 2010's | 4 (36.36) | 24.3611 |
| 2020's | 4 (36.36) | 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 | 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] | ||