| ID Source | ID |
|---|---|
| PubMed CID | 53326156 |
| CHEMBL ID | 1682283 |
| SCHEMBL ID | 1928082 |
| MeSH ID | M0568768 |
| Synonym |
|---|
| 5-[(3-ethynylphenyl)amino]pyrimido[4,5-c]quinoline-8-carboxylic acid |
| CHEMBL1682283 |
| 5-((3-ethynylphenyl)amino)pyrimido[4,5-c]quinoline-8-carboxylic acid |
| 1009821-06-0 |
| AKOS016005325 |
| E1B , |
| FT-0689683 |
| gy6276icqj , |
| unii-gy6276icqj |
| pyrimido(4,5-c)quinoline-8-carboxylic acid, 5-((3-ethynylphenyl)amino)- |
| cx-5011 free acid |
| SCHEMBL1928082 |
| DTXSID00143603 |
| us9062043, table 13, compound 22 |
| us9062043, table 20b, compound 15 |
| bdbm165355 |
| 5-(3-ethynylphenylamino)pyrimido[4,5-c]quinoline-8-carboxylic acid |
| NCGC00408819-01 |
| pyrimido[4,5-c]quinoline-8-carboxylic acid,5-[(3-ethynylphenyl)amino]- |
| pyrimido[4,5-c]quinoline-8-carboxylic acid, 5-[(3-ethynylphenyl)amino]- |
| Q27279351 |
| 1009821-06-0 (cx-5011) ; 1333382-30-1 (cx-5011 sodium salt). |
| 5-((3-ethynylphenyl)amino)pyrimido-[4,5-c]quinoline-8-carboxylic acid |
| 5-(3-ethynylanilino)pyrimido[4,5-c]quinoline-8-carboxylic acid |
| CS-0004263 |
| 5-[(3-ooe(2)>>u+/-(1/2)>>u) degrees +/->>u]-axa currency>>u[4,5-c]a-sso-8-oeea |
| cx5011 |
| 5-((3-ethynylphenyl)amino)pyrimido[4,5-c]quinoline-8-carboxylicacid |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| cytochrome P450 family 3 subfamily A polypeptide 4 | Homo sapiens (human) | Potency | 37.9083 | AID1645841 |
| G | Vesicular stomatitis virus | Potency | 26.8370 | AID1645842 |
| Interferon beta | Homo sapiens (human) | Potency | 26.8370 | AID1645842 |
| HLA class I histocompatibility antigen, B alpha chain | Homo sapiens (human) | Potency | 26.8370 | AID1645842 |
| Inositol hexakisphosphate kinase 1 | Homo sapiens (human) | Potency | 26.8370 | AID1645842 |
| cytochrome P450 2C9, partial | Homo sapiens (human) | Potency | 26.8370 | AID1645842 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Casein kinase II subunit alpha' | Homo sapiens (human) | IC50 | 0.0030 | AID579515 |
| Casein kinase II subunit beta | Homo sapiens (human) | IC50 | 0.0030 | AID579515 |
| Casein kinase II subunit alpha | Homo sapiens (human) | IC50 | 0.0030 | AID579515 |
| Casein kinase II subunit alpha | Homo sapiens (human) | Ki | 0.4200 | AID1539762 |
| Protein | Taxonomy | Measurement | Average (mM) | Bioassay(s) |
|---|---|---|---|---|
| Casein kinase II subunit alpha' | Homo sapiens (human) | EC50 | 0.2700 | AID579517 |
| Casein kinase II subunit beta | Homo sapiens (human) | EC50 | 0.2700 | AID579517 |
| Casein kinase II subunit alpha | Homo sapiens (human) | EC50 | 0.2700 | AID579517 |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 ISSN: 2472-5560 | 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 ISSN: 1521-0111 | 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 ISSN: 1091-6490 | Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors. |
| 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 ISSN: 1091-6490 | 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 ISSN: 1521-0111 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID579519 | Volume of distribution at steady state in mouse at 5.4 mg/kg, iv and 10.8 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID1539762 | Inhibition of CK2alpha (unknown origin) using RRRADDSDDDDD as substrate in presence of [gamma33P]-ATP by autoradiography | 2019 | European journal of medicinal chemistry, Nov-01, Volume: 181ISSN: 1768-3254 | Small molecule modulators targeting protein kinase CK1 and CK2. |
| AID579521 | Cmax in mouse at 10.8 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579526 | Elimination half life in rat at 1.6 mg/kg, iv and 8.1 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579536 | Analgesic activity in mouse assessed as reduction of formalin-induced inflammatory pain at 25 to 150 mg/kg, po administered 1 hr before formalin challenge measured after 10 mins | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579523 | Oral bioavailability in mouse at 10.8 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579520 | Elimination half life in mouse at 5.4 mg/kg, iv and 10.8 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579516 | Competitive inhibition of human recombinant CK2 | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579537 | Analgesic activity in po dosed mouse assessed as reduction of formalin-induced inflammatory pain administered 1 hr before formalin challenge measured after 11 to 40 mins | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579529 | Oral bioavailability in rat at 8.1 mg/kg | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579528 | AUC in rat at 8.1 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579518 | Clearance in mouse at 5.4 mg/kg, iv and 10.8 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579515 | Inhibition of human recombinant CK2 by radiometric assay | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579525 | Volume of distribution at steady state in rat at 1.6 mg/kg, iv and 8.1 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579517 | Inhibition of CK2 in human BxPC3 cells assessed as reduction of Akt phosphorylation at Ser129 | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579527 | Cmax in rat at 8.1 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579522 | AUC in mouse at 10.8 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| AID579524 | Clearance in rat at 1.6 mg/kg, iv and 8.1 mg/kg, po | 2011 | Bioorganic & medicinal chemistry letters, Mar-15, Volume: 21, Issue:6 ISSN: 1464-3405 | Novel potent pyrimido[4,5-c]quinoline inhibitors of protein kinase CK2: SAR and preliminary assessment of their analgesic and anti-viral properties. |
| 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 | 3 (60.00) | 24.3611 |
| 2020's | 2 (40.00) | 2.80 |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (20.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 4 (80.00%) | 84.16% |
| Condition | Indicated | Studies | First Year | Last Year | Average Age | Relationship Strength | Trials | pre-1990 | 1990's | 2000's | 2010's | post-2020 |
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Congenital Zika Syndrome | 0 | 2020 | 2020 | 4.0 | high | 0 | 0 | 0 | 0 | 1 | 0 | |
| Disease Models, Animal | 0 | 2020 | 2020 | 4.0 | high | 0 | 0 | 0 | 0 | 1 | 0 | |
| Zika Virus Infection | 0 | 2020 | 2020 | 4.0 | high | 0 | 0 | 0 | 0 | 1 | 0 |
| Article | Year |
|---|---|
| A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular pharmacology, , Volume: 96, Issue:5 | 2019 |