PD 089828: structure in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
| ID Source | ID |
|---|---|
| PubMed CID | 5328112 |
| CHEMBL ID | 57366 |
| SCHEMBL ID | 8124128 |
| MeSH ID | M0277956 |
| Synonym |
|---|
| 6-arylpyrido[2,3-d]pyrimidine deriv. 1 |
| chembl57366 , |
| pd089828 , |
| bdbm3428 |
| 1-[2-amino-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl]-3-tert-butylurea |
| SCHEMBL8124128 |
| pd-089828 |
| 179343-17-0 |
| AKOS025286335 |
| J-002982 |
| egf/fgf/pdgf receptor tyrosine kinase inhibitor |
| 1-(2-amino-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl)-3-(tert-butyl)urea , |
| 1-[2-amino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]pyrimidin-7-yl]-3-tert-butylurea |
| RRWSNCZYJCOEFX-UHFFFAOYSA-N , |
| 1-[2-amino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]-pyrimidin-7-yl]-3-tert-butylurea |
| HY-112345 |
| AS-16916 |
| CS-0045270 |
| pd 089828 |
| 1-(2-amino-6-(2,6-dichlorophenyl)pyrido[2,3-d]pyrimidin-7-yl)-3-tert-butyl urea |
| pdgfr tyrosine kinase inhibitor xiii |
| EX-A4724 |
| AC-36624 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "PD 089828 was found to inhibit human full-length fibroblast growth factor (FGF) receptor-1 (FGFR-1), platelet-derived growth factor (PDGF) receptor beta subunit (PDGFR-beta), Src nonreceptor tyrosine kinase (c-Src) and epidermal growth factor (EGF) receptor (EGFR) tyrosine kinases with half-maximal inhibitory potencies (IC50 values) of 0.15 +/- 0.02 (n = 4), 0.18 +/- 0.04 (n = 3), 1.76 +/- 0.28 (n = 4) and 5.47 +/- 0.78 (n = 6) microM, respectively." | ( Inhibition of growth factor-mediated tyrosine phosphorylation in vascular smooth muscle by PD 089828, a new synthetic protein tyrosine kinase inhibitor. Batley, BL; Dahring, TK; Hamby, JM; Kraker, AJ; Lu, GH; Panek, RL, 1997) | 1.24 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Subsequent SAR studies led to the synthesis of new analogs with improved potency, solubility, and bioavailability relative to the initial lead." | ( Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. Amar, A; Bradford, L; Connolly, CJ; Dahring, T; Doherty, AM; Fry, DW; Hallak, H; Hamby, JM; Keiser, J; Kraker, AJ; Lu, GH; Major, TC; Nelson, JM; Olsewski, B; Panek, RL; Ryan, MJ; Schroeder, MC; Shen, C; Showalter, HD; Slintak, V; Winters, RT, 1997) | 0.3 |
| Protein | Taxonomy | Measurement | Average | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| Proto-oncogene tyrosine-protein kinase Src | Gallus gallus (chicken) | IC50 (µMol) | 0.2200 | 0.0004 | 0.9151 | 5.1000 | AID219507 |
| Epidermal growth factor receptor | Homo sapiens (human) | IC50 (µMol) | 0.4500 | 0.0000 | 0.5369 | 10.0000 | AID69732 |
| Platelet-derived growth factor receptor beta | Mus musculus (house mouse) | IC50 (µMol) | 1.1500 | 0.0018 | 0.7552 | 9.5000 | AID155203; AID161090 |
| Insulin receptor | Homo sapiens (human) | IC50 (µMol) | 50.0000 | 0.0017 | 0.8479 | 10.0000 | AID93076 |
| Platelet-derived growth factor receptor beta | Homo sapiens (human) | IC50 (µMol) | 0.5200 | 0.0006 | 0.8007 | 8.5000 | AID1795526 |
| Fibroblast growth factor receptor 1 | Homo sapiens (human) | IC50 (µMol) | 0.2750 | 0.0002 | 0.9420 | 10.0000 | AID1193339; AID1795526; AID242108; AID73312; AID73438; AID73441 |
| Proto-oncogene tyrosine-protein kinase Src | Homo sapiens (human) | IC50 (µMol) | 0.4000 | 0.0002 | 0.5335 | 10.0000 | AID1795526; AID219521; AID219647 |
| Platelet-derived growth factor receptor alpha | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.8700 | 0.0050 | 0.7741 | 4.0000 | AID161109; AID166382 |
| Fibroblast growth factor receptor 2 | Homo sapiens (human) | IC50 (µMol) | 0.1300 | 0.0004 | 0.3276 | 8.6200 | AID1193340; AID242108; AID73312 |
| Fibroblast growth factor receptor 4 | Homo sapiens (human) | IC50 (µMol) | 0.2733 | 0.0008 | 0.6217 | 8.6200 | AID1193342; AID242108; AID73312 |
| Fibroblast growth factor receptor 3 | Homo sapiens (human) | IC50 (µMol) | 0.1833 | 0.0004 | 0.2863 | 8.6200 | AID1193341; AID242108; AID73312 |
| Gastrin/cholecystokinin type B receptor | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.2200 | 0.0001 | 0.2480 | 1.4000 | AID219521 |
| Platelet-derived growth factor receptor beta | Rattus norvegicus (Norway rat) | IC50 (µMol) | 0.8700 | 0.0050 | 0.7128 | 4.0000 | AID161109; AID166382 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID73312 | Inhibition of Fibroblast growth factor receptor (FGFr) tyrosine kinase | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. |
| AID166382 | Inhibition of platelet derived growth factor (PDGF) stimulated PDGF-receptor autophosphorylation in rat aortic vascular smooth muscle cells (RAVSMCs) | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. |
| AID242232 | Inhibition of Platelet-derived growth factor receptor | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1. |
| AID1193341 | Inhibition of FGFR3 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID93076 | Inhibition of insulin receptor (InsR) tyrosine kinase | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. |
| AID161109 | Inhibition of Platelet-derived growth factor receptor (PDGFr) tyrosine kinase in rat aortic vascular smooth muscle cells (RAVSMCs). | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. |
| AID219521 | Inhibition of the phosphorylation of a random glutamate-tyrosine (4:1) copolymer by isolated avian c-Src protein. | 2000 | Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22 | 3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase. |
| AID155203 | Ability to prevent phosphorylation of isolated mouse PDGF receptor beta | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity. |
| AID1193346 | Cytotoxicity against human HL7702 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1193344 | Cytotoxicity against human HeLa 229 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1193340 | Inhibition of FGFR2 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID1193345 | Cytotoxicity against mouse B16F10 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID219507 | Ability to prevent phosphorylation of avian c-Src TK | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity. |
| AID1193343 | Cytotoxicity against human A549 cells after 72 hrs by MTT assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID219647 | Inhibition of C-src tyrosine kinase | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. |
| AID73438 | Ability to prevent phosphorylation of human fibroblast growth factor receptor 1 | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity. |
| AID1193339 | Inhibition of FGFR1 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID242108 | Inhibition of Fibroblast growth factor receptor | 2005 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 15, Issue:7 | Structure-activity relationships for 2-anilino-6-phenylpyrido[2,3-d]pyrimidin-7(8H)-ones as inhibitors of the cellular checkpoint kinase Wee1. |
| AID161090 | Inhibition of the phosphorylation of a random glutamate-tyrosine (4:1) copolymer by isolated mouse Platelet-derived growth factor protein. | 2000 | Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22 | 3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase. |
| AID1193342 | Inhibition of FGFR4 (unknown origin) after 90 mins by TR-FRET assay | 2015 | Bioorganic & medicinal chemistry letters, Apr-01, Volume: 25, Issue:7 | Design, synthesis and preliminary biological evaluation of C-8 substituted guanine derivatives as small molecular inhibitors of FGFRs. |
| AID73441 | Inhibition of the phosphorylation of a random glutamate-tyrosine (4:1) copolymer by isolated Fibroblast growth factor receptor 1. | 2000 | Journal of medicinal chemistry, Nov-02, Volume: 43, Issue:22 | 3-(3,5-Dimethoxyphenyl)-1,6-naphthyridine-2,7-diamines and related 2-urea derivatives are potent and selective inhibitors of the FGF receptor-1 tyrosine kinase. |
| AID69732 | Inhibition of Epidermal growth factor receptor (EGFr) tyrosine kinase | 1997 | Journal of medicinal chemistry, Jul-18, Volume: 40, Issue:15 | Structure-activity relationships for a novel series of pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. |
| AID1795526 | Kinase Inhibition Assay from Article 10.1021/jm0004291: \\Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity.\\ | 2001 | Journal of medicinal chemistry, Jun-07, Volume: 44, Issue:12 | Soluble 2-substituted aminopyrido[2,3-d]pyrimidin-7-yl ureas. Structure-activity relationships against selected tyrosine kinases and exploration of in vitro and in vivo anticancer activity. |
| [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 | 2 (33.33) | 18.2507 |
| 2000's | 3 (50.00) | 29.6817 |
| 2010's | 1 (16.67) | 24.3611 |
| 2020's | 0 (0.00) | 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 | 0 (0.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 6 (100.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||