Page last updated: 2024-12-10
uccf-029
Description
Research Excerpts
Clinical Trials
Roles
Classes
Pathways
Study Profile
Bioassays
Related Drugs
Related Conditions
Protein Interactions
Research Growth
Cross-References
| ID Source | ID |
|---|---|
| PubMed CID | 3163532 |
| CHEMBL ID | 177991 |
| CHEBI ID | 116557 |
| SCHEMBL ID | 4069839 |
| MeSH ID | M0519743 |
Synonyms (19)
| Synonym |
|---|
| 2-pyridin-4-yl-benzo[h]chromen-4-one |
| 2110-25-0 |
| smr000525005 |
| MLS001209162 |
| CHEBI:116557 |
| AKOS000507523 |
| bdbm50159612 |
| 4-(4-oxo-4h-benzo[h]chromen-2-yl)-pyridinium |
| uccf-029 , |
| CHEMBL177991 , |
| 2-pyridin-4-ylbenzo[h]chromen-4-one |
| HMS2841G23 |
| gtpl4335 |
| 2-(pyridin-4-yl)-4h-benzo[h]chromen-4-one |
| SCHEMBL4069839 |
| DTXSID20390354 |
| 4-(4-oxo-4h-benzo[h]chromen-2-yl)pyridinium bisulfate |
| J-013846 |
| Q27089050 |
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]
Drug Classes (2)
| Class | Description |
|---|---|
| organic heterotricyclic compound | An organic tricyclic compound in which at least one of the rings of the tricyclic skeleton contains one or more heteroatoms. |
| organooxygen compound | An organochalcogen compound containing at least one carbon-oxygen bond. |
| [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 Targets (16)
Potency Measurements
| Protein | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Chain A, MAJOR APURINIC/APYRIMIDINIC ENDONUCLEASE | Homo sapiens (human) | Potency | 11.9173 | 0.0032 | 45.4673 | 12,589.2998 | AID2517 |
| ATAD5 protein, partial | Homo sapiens (human) | Potency | 7.3048 | 0.0041 | 10.8903 | 31.5287 | AID504467 |
| TDP1 protein | Homo sapiens (human) | Potency | 24.5192 | 0.0008 | 11.3822 | 44.6684 | AID686978; AID686979 |
| Smad3 | Homo sapiens (human) | Potency | 1.7783 | 0.0052 | 7.8098 | 29.0929 | AID588855 |
| nonstructural protein 1 | Influenza A virus (A/WSN/1933(H1N1)) | Potency | 3.1623 | 0.2818 | 9.7212 | 35.4813 | AID2326 |
| nuclear factor erythroid 2-related factor 2 isoform 2 | Homo sapiens (human) | Potency | 18.3564 | 0.0041 | 9.9848 | 25.9290 | AID504444 |
| DNA polymerase beta | Homo sapiens (human) | Potency | 79.4328 | 0.0224 | 21.0102 | 89.1251 | AID485314 |
| flap endonuclease 1 | Homo sapiens (human) | Potency | 39.8107 | 0.1337 | 25.4129 | 89.1251 | AID588795 |
| DNA polymerase iota isoform a (long) | Homo sapiens (human) | Potency | 100.0000 | 0.0501 | 27.0736 | 89.1251 | AID588590 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Inhibition Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cytochrome P450 1A1 | Homo sapiens (human) | IC50 (µMol) | 0.0187 | 0.0079 | 1.2478 | 9.9000 | AID1581701 |
| Cytochrome P450 1A2 | Homo sapiens (human) | IC50 (µMol) | 0.0364 | 0.0001 | 1.7740 | 10.0000 | AID1581702 |
| DNA-dependent protein kinase catalytic subunit | Homo sapiens (human) | IC50 (µMol) | 10.0000 | 0.0005 | 1.3500 | 10.0000 | AID241691 |
| Cytochrome P450 1B1 | Homo sapiens (human) | IC50 (µMol) | 0.0093 | 0.0013 | 0.8696 | 9.9000 | AID1581700 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Activation Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Cystic fibrosis transmembrane conductance regulator | Homo sapiens (human) | EC50 (µMol) | 3.5000 | 0.0030 | 2.0312 | 9.0000 | AID340528 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Other Measurements
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| dual specificity tyrosine-phosphorylation-regulated kinase 1A | Rattus norvegicus (Norway rat) | AC50 | 0.4960 | 0.0056 | 4.6932 | 26.6940 | AID588345 |
| glycogen synthase kinase-3 alpha | Homo sapiens (human) | AC50 | 0.3121 | 0.0135 | 29.7434 | 171.7000 | AID463203 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
Biological Processes (168)
Molecular Functions (49)
Ceullar Components (31)
Bioassays (20)
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1745847 | CMV-Luciferase Counterscreen for Inhibitors of ATXN expression | |||
| AID1745849 | Viability Counterscreen for CMV-Luciferase Assay of Inhibitors of ATXN expression | |||
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID504810 | Antagonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID504812 | Inverse Agonists of the Thyroid Stimulating Hormone Receptor: HTS campaign | 2010 | Endocrinology, Jul, Volume: 151, Issue:7 | A small molecule inverse agonist for the human thyroid-stimulating hormone receptor. |
| AID1745848 | Confirmatory qHTS for Inhibitors of ATXN expression | |||
| AID1745850 | Viability Counterscreen for Confirmatory qHTS for Inhibitors of ATXN expression | |||
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1745846 | Firefly Luciferase Counterscreen for Inhibitors of ATXN expression | |||
| AID1581704 | Selectivity index, ratio of IC50 for human recombinant CYP1A2 to IC50 for human recombinant CYP1B1 using 7-ethoxyresorufin as substrate in presence of glucose-6-phosphate, glucose-6-phosphate dehydrogenase and NADPH-generating system by fluorometry | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Synthesis and structure-activity relationship studies of α-naphthoflavone derivatives as CYP1B1 inhibitors. |
| AID1581703 | Selectivity index, ratio of IC50 for human recombinant CYP1A1 to IC50 for human recombinant CYP1B1 using 7-ethoxyresorufin as substrate in presence of glucose-6-phosphate, glucose-6-phosphate dehydrogenase and NADPH-generating system by fluorometry | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Synthesis and structure-activity relationship studies of α-naphthoflavone derivatives as CYP1B1 inhibitors. |
| AID340771 | Agonist activity at CFTR-deltaF508 mutant expressed in NIH3T3 cells assessed as increase in forskolin-stimulated current at 20 uM by whole cell assay relative to control | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Activation of CFTR by UCCF-029 and genistein. |
| AID1581702 | Inhibition of human recombinant CYP1A2 using 7-ethoxyresorufin as substrate in presence of glucose-6-phosphate, glucose-6-phosphate dehydrogenase and NADPH-generating system incubated for 50 mins by fluorometry | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Synthesis and structure-activity relationship studies of α-naphthoflavone derivatives as CYP1B1 inhibitors. |
| AID340528 | Agonist activity at CFTR-deltaF508 mutant expressed in NIH3T3 cells assessed as increase in forskolin-stimulated current | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Activation of CFTR by UCCF-029 and genistein. |
| AID1581701 | Inhibition of human recombinant CYP1A1 using 7-ethoxyresorufin as substrate in presence of glucose-6-phosphate, glucose-6-phosphate dehydrogenase and NADPH-generating system incubated for 15 mins by fluorometry | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Synthesis and structure-activity relationship studies of α-naphthoflavone derivatives as CYP1B1 inhibitors. |
| AID340532 | Agonist activity at CFTR-K1250A mutant assessed as increase in forskolin-stimulated current at 5 uM | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Activation of CFTR by UCCF-029 and genistein. |
| AID241691 | Inhibition of DNA dependent protein kinase isolated from HeLa cells | 2005 | Journal of medicinal chemistry, Jan-27, Volume: 48, Issue:2 | Selective benzopyranone and pyrimido[2,1-a]isoquinolin-4-one inhibitors of DNA-dependent protein kinase: synthesis, structure-activity studies, and radiosensitization of a human tumor cell line in vitro. |
| AID340529 | Agonist activity at CFTR-deltaF508 mutant expressed in NIH3T3 cells assessed as increase in forskolin-stimulated current at 30 uM by whole cell assay relative to control | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Activation of CFTR by UCCF-029 and genistein. |
| AID1581700 | Inhibition of human recombinant CYP1B1 using 7-ethoxyresorufin as substrate in presence of glucose-6-phosphate, glucose-6-phosphate dehydrogenase and NADPH-generating system incubated for 35 mins by fluorometry | 2020 | European journal of medicinal chemistry, Feb-01, Volume: 187 | Synthesis and structure-activity relationship studies of α-naphthoflavone derivatives as CYP1B1 inhibitors. |
| AID340530 | Agonist activity at CFTR-deltaF508 mutant expressed in NIH3T3 cells assessed as increase in forskolin-stimulated current at 30 uM by whole cell assay relative to genistein | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Activation of CFTR by UCCF-029 and genistein. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
Research
Studies (5)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 0 (0.00) | 18.2507 |
| 2000's | 2 (40.00) | 29.6817 |
| 2010's | 1 (20.00) | 24.3611 |
| 2020's | 2 (40.00) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
Study Types
| 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 | 5 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||