RO 3306: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 135400873 |
| CHEMBL ID | 393929 |
| SCHEMBL ID | 4874056 |
| MeSH ID | M0501284 |
| Synonym |
|---|
| ro-3306 |
| CHEMBL393929 , |
| (5z)-5-(quinolin-6-ylmethylidene)-2-[(thiophen-2-ylmethyl)amino]-1,3-thiazol-4(5h)-one |
| HMS3229B19 |
| bdbm50205472 |
| (z)-5-(quinolin-6-ylmethylene)-2-(thiophen-2-ylmethylamino)thiazol-4(5h)-one |
| 872573-93-8 |
| S7747 |
| BRD-K78373679-001-01-1 |
| SCHEMBL4874056 |
| CS-3790 |
| ro 3306 |
| 5-(6-quinolinylmethylene)-2-[(2-thienylmethyl)amino]-4(5h)-thiazolone |
| 5-(quinolin-6-ylmethylene)-2-(thiophen-2-ylmethylamino)thiazol-4(5h)-one |
| AC-33718 |
| HY-12529 |
| AKOS024458017 |
| bdbm181049 |
| EX-A575 |
| (5z)-5-[(quinolin-6-yl)methylidene]-2-{[(thiophen-2-yl)methyl]amino}-4,5-dihydro-1,3-thiazol-4-one |
| ro-3306, >=98% (hplc) |
| mfcd17392573 |
| (5z)-5-(quinolin-6-ylmethylidene)-2-(thiophen-2-ylmethylimino)-1,3-thiazolidin-4-one |
| XOLMRFUGOINFDQ-YBEGLDIGSA-N |
| 2-[(thiophen-2-ylmethyl)-amino]-5-[1-quinolin-6-yl-meth-(z)-ylidene]-thiazol-4-one |
| R0201 |
| (z)-5-(quinolin-6-ylmethylene)-2-[(thiophen-2-ylmethyl)amino]thiazol-4(5h)-one |
| CCG-268045 |
| Q27463911 |
| XJB57393 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Aurora kinase A | Homo sapiens (human) | IC50 (µMol) | 5.6500 | 0.0000 | 0.4620 | 8.6000 | AID1513690; AID655144 |
| Cyclin-T1 | Homo sapiens (human) | IC50 (µMol) | 14.5000 | 0.0010 | 0.5585 | 8.0000 | AID1513684 |
| Tyrosine-protein kinase Fyn | Homo sapiens (human) | Ki | 2.0000 | 0.0100 | 3.7550 | 7.5000 | AID294350 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 (µMol) | 1.0837 | 0.0004 | 1.3452 | 10.0000 | AID1513678; AID294352; AID294353; AID294354; AID294355; AID294357; AID655146 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | Ki | 0.0350 | 0.0010 | 1.2551 | 5.0000 | AID294341 |
| Cyclin-dependent kinase 4 | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.0006 | 0.5706 | 10.0000 | AID1513680 |
| Cyclin-dependent kinase 4 | Homo sapiens (human) | Ki | 2.0000 | 0.0006 | 0.7369 | 3.6000 | AID294343 |
| G2/mitotic-specific cyclin-B1 | Homo sapiens (human) | IC50 (µMol) | 0.0470 | 0.0013 | 1.4518 | 10.0000 | AID1513678 |
| Protein kinase C alpha type | Homo sapiens (human) | Ki | 2.0000 | 0.0002 | 1.0945 | 6.9600 | AID294346 |
| Cyclin-A2 | Homo sapiens (human) | IC50 (µMol) | 0.2530 | 0.0004 | 1.0339 | 10.0000 | AID1513681 |
| G1/S-specific cyclin-D1 | Homo sapiens (human) | IC50 (µMol) | 20.0000 | 0.0006 | 0.5479 | 9.5000 | AID1513680 |
| G1/S-specific cyclin-E1 | Homo sapiens (human) | IC50 (µMol) | 0.1860 | 0.0010 | 1.0404 | 10.0000 | AID1513679 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 0.2195 | 0.0004 | 1.0444 | 10.0000 | AID1513679; AID1513681 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | Ki | 0.3400 | 0.0005 | 0.6427 | 5.0000 | AID294342 |
| Mitogen-activated protein kinase 1 | Homo sapiens (human) | Ki | 2.0000 | 0.0020 | 0.5490 | 2.0000 | AID294348 |
| RAC-alpha serine/threonine-protein kinase | Homo sapiens (human) | Ki | 2.0000 | 0.0001 | 0.7670 | 4.5000 | AID294345 |
| RAC-beta serine/threonine-protein kinase | Homo sapiens (human) | Ki | 2.0000 | 0.0040 | 0.0040 | 0.0040 | AID294345 |
| Dual specificity protein kinase CLK1 | Homo sapiens (human) | IC50 (µMol) | 1.1347 | 0.0074 | 0.4344 | 2.1000 | AID1801641 |
| Dual specificity protein kinase CLK2 | Homo sapiens (human) | IC50 (µMol) | 1.1347 | 0.0005 | 0.7554 | 8.0380 | AID1801641 |
| Dual specificity protein kinase CLK3 | Homo sapiens (human) | IC50 (µMol) | 1.1347 | 0.0410 | 2.0143 | 8.7440 | AID1801641 |
| Glycogen synthase kinase-3 alpha | Homo sapiens (human) | Ki | 0.5000 | 0.0091 | 0.3468 | 1.6000 | AID294349 |
| Glycogen synthase kinase-3 beta | Homo sapiens (human) | Ki | 0.5000 | 0.0020 | 0.3668 | 1.6000 | AID294349 |
| Cyclin-dependent kinase 7 | Homo sapiens (human) | IC50 (µMol) | 17.4000 | 0.0001 | 0.9106 | 9.2000 | AID1513683 |
| Cyclin-dependent kinase 9 | Homo sapiens (human) | IC50 (µMol) | 14.5000 | 0.0010 | 0.6236 | 8.0000 | AID1513684 |
| Cyclin-H | Homo sapiens (human) | IC50 (µMol) | 17.4000 | 0.0005 | 1.0823 | 9.2000 | AID1513683 |
| CDK-activating kinase assembly factor MAT1 | Homo sapiens (human) | IC50 (µMol) | 17.4000 | 0.0030 | 1.6892 | 9.2000 | AID1513683 |
| Cyclin-dependent-like kinase 5 | Homo sapiens (human) | IC50 (µMol) | 2.4800 | 0.0002 | 1.1832 | 10.0000 | AID1513682 |
| Protein kinase C delta type | Homo sapiens (human) | Ki | 0.3200 | 0.0003 | 0.9489 | 6.9600 | AID294347 |
| Dual specificity tyrosine-phosphorylation-regulated kinase 1A | Homo sapiens (human) | IC50 (µMol) | 1.1347 | 0.0031 | 0.7140 | 9.0120 | AID1801641 |
| Cyclin-dependent kinase 5 activator 1 | Homo sapiens (human) | IC50 (µMol) | 2.4800 | 0.0010 | 1.2898 | 10.0000 | AID1513682 |
| Aurora kinase B | Homo sapiens (human) | IC50 (µMol) | 0.8150 | 0.0003 | 0.9634 | 9.8000 | AID1513691 |
| RAC-gamma serine/threonine-protein kinase | Homo sapiens (human) | Ki | 2.0000 | 0.0130 | 0.0130 | 0.0130 | AID294345 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1513683 | Inhibition of GST-tagged CDK7/cyclinH/MAT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID294356 | Antiproliferative activity against human SJSA1 cells | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID294347 | Inhibition of PKCd | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID294344 | Inhibition of PKAP1 | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID655148 | Toxicity in human BMNC assessed as granulocyte/monocyte colony forming units ratio after 14 days by microscopic analysis | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5 | Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1. |
| AID294349 | Inhibition of GSKp1 | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID294342 | Inhibition of CDK2 | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID294354 | Antiproliferative activity against human SW480 cells | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID294351 | Inhibition of EPHB3 | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID294340 | Inhibition of CDK1/cyclinB | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID1513691 | Inhibition of GST-tagged AURORA B (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID294343 | Inhibition of CDK4 | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID1513682 | Inhibition of GST-tagged CDK5/p25 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID294348 | Inhibition of ERK | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID1513721 | Binding affinity to CDK1 in human HCT116 cells assessed as induction of thermal stabilization at 4 to 20 uM incubated for 4 hrs by immunoblot analysis | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID1513690 | Inhibition of GST-tagged AURORA A (unknown origin) expressed in baculovirus infected Sf9 cells using MBP as substrate | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID294345 | Inhibition of AKT | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID1513679 | Inhibition of His-tagged CDK2/cyclin E (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID294346 | Inhibition of PKCa | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID294355 | Antiproliferative activity against human MDA435 cells | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID294341 | Inhibition of CDK1 | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID294352 | Antiproliferative activity against human HCT116 cells | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID1513684 | Inhibition of GST-tagged CDK9/CyclinT1 (unknown origin) expressed in Baculovirus infected Sf9 cells using YSPTSPS-2 KK peptide as substrate as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID1513678 | Inhibition of His-tagged CDK1/cyclin B1 (unknown origin) expressed in Baculovirus infected Sf9 cells using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID1513680 | Inhibition of GST-tagged CDK4/cyclin D1 (unknown origin) expressed in Baculovirus infected Sf9 cells using RPPTLSPIPHIPR peptide as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID655147 | Cytotoxicity against human HCT116 cells after 5 days by MTS assay | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5 | Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1. |
| AID655146 | Inhibition of CDK1 | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5 | Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1. |
| AID294353 | Antiproliferative activity against human H460a cells | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID1513681 | Inhibition of GST-tagged CDK2/cyclin A2 (unknown origin) expressed in Escherichia coli using histone H1 as substrate in presence of [gamma-33P]-ATP by radiometric filter binding assay | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID294350 | Inhibition of FYN | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID655144 | Inhibition of aurora A kinase | 2012 | Bioorganic & medicinal chemistry letters, Mar-01, Volume: 22, Issue:5 | Synthesis, SAR and biological evaluation of 1,6-disubstituted-1H-pyrazolo[3,4-d]pyrimidines as dual inhibitors of Aurora kinases and CDK1. |
| AID1513685 | Induction of cell cycle arrest in human HCT116 cells assessed as accumulation at G2/M phase at 3.9 to 19.8 uM after 24 hrs by propidium iodide-staining based flow cytometry relative to control | 2018 | Journal of medicinal chemistry, 10-25, Volume: 61, Issue:20 | How Selective Are Pharmacological Inhibitors of Cell-Cycle-Regulating Cyclin-Dependent Kinases? |
| AID294357 | Antiproliferative activity against human RKO cells | 2007 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 17, Issue:8 | Synthesis and activity of quinolinyl-methylene-thiazolinones as potent and selective cyclin-dependent kinase 1 inhibitors. |
| AID1801641 | Kinase Inhibition Assay from Article 10.1021/acs.biochem.5b01128: \\Benzobisthiazoles Represent a Novel Scaffold for Kinase Inhibitors of CLK Family Members.\\ | 2016 | Biochemistry, Jan-26, Volume: 55, Issue:3 | Benzobisthiazoles Represent a Novel Scaffold for Kinase Inhibitors of CLK Family Members. |
| [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 | 8 (14.04) | 29.6817 |
| 2010's | 40 (70.18) | 24.3611 |
| 2020's | 9 (15.79) | 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 | 58 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||