PD 0183812: inhibits CDK4 and CDK6; structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 5330258 |
| CHEMBL ID | 139653 |
| SCHEMBL ID | 5268115 |
| MeSH ID | M0391923 |
| Synonym |
|---|
| 8-{bicyclo[2.2.1]heptan-2-yl}-2-({4-[4-(3-hydroxypropyl)piperidin-1-yl]phenyl}amino)-7h,8h-pyrido[2,3-d]pyrimidin-7-one |
| bdbm6280 |
| 8-bicyclo[2.2.1]hept-2-yl-2-{4-[4-(3-hydroxypropyl)piperidin-1-yl]phenylamino}-8h-pyrido[2,3-d]pyrimidin-7-one |
| n8 pyrido[2,3-d]pyrimidin-7-one deriv. 72 |
| pd 0183812 |
| pd183812 , |
| pd-0183812 |
| CHEMBL139653 |
| SCHEMBL5268115 |
| 8-(2-bicyclo[2.2.1]heptanyl)-2-[4-[4-(3-hydroxypropyl)piperidin-1-yl]anilino]pyrido[2,3-d]pyrimidin-7-one |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| G2/mitotic-specific cyclin-B2 | Homo sapiens (human) | IC50 (µMol) | 40.0000 | 0.0025 | 1.8172 | 10.0000 | AID53204 |
| G1/S-specific cyclin-E2 | Homo sapiens (human) | IC50 (µMol) | 0.1650 | 0.0010 | 1.7394 | 10.0000 | AID53707 |
| Cyclin-dependent kinase 1 | Homo sapiens (human) | IC50 (µMol) | 16.0764 | 0.0004 | 1.3452 | 10.0000 | AID1795862; AID53204 |
| Fibroblast growth factor receptor 1 | Homo sapiens (human) | IC50 (µMol) | 8.6200 | 0.0002 | 0.9420 | 10.0000 | AID1795863; AID73305 |
| Cyclin-dependent kinase 4 | Homo sapiens (human) | IC50 (µMol) | 6.7350 | 0.0006 | 0.5706 | 10.0000 | AID1795862; AID442994; AID54016 |
| G2/mitotic-specific cyclin-B1 | Homo sapiens (human) | IC50 (µMol) | 16.0764 | 0.0013 | 1.4518 | 10.0000 | AID1795862; AID53204 |
| Cyclin-A2 | Homo sapiens (human) | IC50 (µMol) | 8.1182 | 0.0004 | 1.0339 | 10.0000 | AID1795862; AID53681 |
| Fibroblast growth factor receptor 2 | Homo sapiens (human) | IC50 (µMol) | 8.6200 | 0.0004 | 0.3276 | 8.6200 | AID73305 |
| Fibroblast growth factor receptor 4 | Homo sapiens (human) | IC50 (µMol) | 8.6200 | 0.0008 | 0.6217 | 8.6200 | AID73305 |
| Fibroblast growth factor receptor 3 | Homo sapiens (human) | IC50 (µMol) | 8.6200 | 0.0004 | 0.2863 | 8.6200 | AID73305 |
| G1/S-specific cyclin-D1 | Homo sapiens (human) | IC50 (µMol) | 8.0780 | 0.0006 | 0.5479 | 9.5000 | AID1795862; AID54016 |
| G1/S-specific cyclin-E1 | Homo sapiens (human) | IC50 (µMol) | 8.1094 | 0.0010 | 1.0404 | 10.0000 | AID1795862; AID53707 |
| Cyclin-dependent kinase 2 | Homo sapiens (human) | IC50 (µMol) | 6.7927 | 0.0004 | 1.0444 | 10.0000 | AID1795862; AID53681; AID53707 |
| G1/S-specific cyclin-D2 | Homo sapiens (human) | IC50 (µMol) | 0.0080 | 0.0080 | 0.1480 | 0.9250 | AID54016 |
| G1/S-specific cyclin-D3 | Homo sapiens (human) | IC50 (µMol) | 0.0080 | 0.0015 | 0.0862 | 0.9250 | AID54016 |
| Cyclin-A1 | Homo sapiens (human) | IC50 (µMol) | 0.2090 | 0.0005 | 1.4715 | 10.0000 | AID53681 |
| G2/mitotic-specific cyclin-B3 | Homo sapiens (human) | IC50 (µMol) | 40.0000 | 0.0025 | 1.8172 | 10.0000 | AID53204 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1795862 | CDKs Assay from Article 10.1021/jm000271k: \\Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.\\ | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
| AID1795863 | Tyrosine Kinase Assay from Article 10.1021/jm000271k: \\Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases.\\ | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
| AID81702 | Inhibition of HCT116 human colon carcinoma cell proliferation | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
| AID1868088 | Inhibition of CDK6/Cyclin D (unknown origin) expressed in baculovirus infected insect cells using GST-tagged Rb protein as substrate incubated for 15 mins in presence of [gamma-32P]ATP by beta-plate reader method | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9 | From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy. |
| AID53681 | Inhibition of Cyclin-dependent kinase 2-cyclin A | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
| AID53707 | Inhibition of Cyclin-dependent kinase 2-cyclin E | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
| AID1868087 | Inhibition of CDK4/Cyclin D (unknown origin) expressed in baculovirus infected insect cells using GST-tagged Rb protein as substrate incubated for 15 mins in presence of [gamma-32P]ATP by beta-plate reader method | 2022 | Journal of medicinal chemistry, 05-12, Volume: 65, Issue:9 | From Structure Modification to Drug Launch: A Systematic Review of the Ongoing Development of Cyclin-Dependent Kinase Inhibitors for Multiple Cancer Therapy. |
| AID54016 | Inhibition of Cyclin-dependent kinase 4-cyclin D | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
| AID73305 | Inhibition of Fibroblast growth factor receptor (FGFr) | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
| AID442994 | Inhibition of CDK4 | 2010 | European journal of medicinal chemistry, Feb, Volume: 45, Issue:2 | Radiosynthesis and radiopharmacological evaluation of cyclin-dependent kinase 4 (Cdk4) inhibitors. |
| AID53204 | Inhibition of Cyclin-dependent kinase 1-cyclin B | 2000 | Journal of medicinal chemistry, Nov-30, Volume: 43, Issue:24 | Pyrido[2,3-d]pyrimidin-7-one inhibitors of cyclin-dependent kinases. |
| [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 | 3 (60.00) | 29.6817 |
| 2010's | 1 (20.00) | 24.3611 |
| 2020's | 1 (20.00) | 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 (20.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 4 (80.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||