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Target
Platelet-derived growth factor receptor beta
Ligand
BDBM3487
Substrate
Poly(E:Y)
Meas. Tech.
Kinase Inhibition Assay
IC50
680±n/a nM
Citation
 Schroeder, MC; Hamby, JM; Connolly, CJ; Grohar, PJ; Winters, RT; Barvian, MR; Moore, CW; Boushelle, SL; Crean, SM; Kraker, AJ; Driscoll, DL; Vincent, PW; Elliott, WL; Lu, GH; Batley, BL; Dahring, TK; Major, TC; Panek, RL; Doherty, AM; Showalter, HD 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. J Med Chem 44:1915-26 (2001) [PubMed]  Article
Target
Name:
Platelet-derived growth factor receptor beta
Synonyms:
Beta-type platelet-derived growth factor receptor | CD140 antigen-like family member B | CD140b antigen | CD_antigen=CD140b | PDGF Receptor Substrate | PDGF-R-beta | PDGFR | PDGFR substrate | PDGFR-1 | PDGFR1 | PDGFRB | PDGFRbeta | PGFRB_HUMAN | Platelet-Derived Growth Factor Receptor, beta | Platelet-derived growth factor receptor 1 | Platelet-derived growth factor receptor beta | Platelet-derived growth factor receptor beta (PDGFR-beta) | Platelet-derived growth factor receptor beta (PDGFRB) | Platelet-derived growth factor receptor beta (PDGFRbeta) | VHL/PDGFRB
Type:
Enzyme
Mol. Mass.:
123922.25
Organism:
Homo sapiens (Human)
Description:
P09619
Residue:
1106
Sequence:
MRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTFVLTCSGSAPVVWERMSQEPPQEMAKAQDGTFSSVLTLTNLTGLDTGEYFCTHNDSRGLETDERKRLYIFVPDPTVGFLPNDAEELFIFLTEITEITIPCRVTDPQLVVTLHEKKGDVALPVPYDHQRGFSGIFEDRSYICKTTIGDREVDSDAYYVYRLQVSSINVSVNAVQTVVRQGENITLMCIVIGNEVVNFEWTYPRKESGRLVEPVTDFLLDMPYHIRSILHIPSAELEDSGTYTCNVTESVNDHQDEKAINITVVESGYVRLLGEVGTLQFAELHRSRTLQVVFEAYPPPTVLWFKDNRTLGDSSAGEIALSTRNVSETRYVSELTLVRVKVAEAGHYTMRAFHEDAEVQLSFQLQINVPVRVLELSESHPDSGEQTVRCRGRGMPQPNIIWSACRDLKRCPRELPPTLLGNSSEEESQLETNVTYWEEEQEFEVVSTLRLQHVDRPLSVRCTLRNAVGQDTQEVIVVPHSLPFKVVVISAILALVVLTIISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPMQLPYDSTWELPRDQLVLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGPHLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQHHSDKRRPPSAELYSNALPVGLPLPSHVSLTGESDGGYMDMSKDESVDYVPMLDMKGDVKYADIESSNYMAPYDNYVPSAPERTCRATLINESPVLSYMDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLVKICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLGGTPYPELPMNEQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFEIRPPFSQLVLLLERLLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGFHGLRSPLDTSSVLYTAVQPNEGDNDYIIPLPDPKPEVADEGPLEGSPSLASSTLNEVNTSSTISCDSPLEPQDEPEPEPQLELQVEPEPELEQLPDSGCPAPRAEAEDSFL
  
Inhibitor
Name:
BDBM3487
Synonyms:
3-[6-(2,6-dichlorophenyl)-2-{[3-(4-methylpiperazin-1-yl)propyl]amino}pyrido[2,3-d]pyrimidin-7-yl]-1-(4-methoxyphenyl)urea | 6-arylpyrido[2,3-d]pyrimidine deriv. 69 | CHEMBL298679
Type:
Small organic molecule
Emp. Form.:
C29H32Cl2N8O2
Mol. Mass.:
595.523
SMILES:
COc1ccc(NC(=O)Nc2nc3nc(NCCCN4CCN(C)CC4)ncc3cc2-c2c(Cl)cccc2Cl)cc1 |(30.19,-24.55,;28.88,-23.74,;28.93,-22.2,;27.62,-21.39,;27.67,-19.85,;29.03,-19.12,;29.03,-17.58,;27.69,-16.81,;26.36,-17.58,;27.69,-15.27,;26.36,-14.5,;25.03,-15.27,;23.69,-14.5,;22.36,-15.27,;21.03,-14.5,;19.69,-15.27,;18.36,-14.5,;16.87,-14.9,;15.78,-13.81,;14.29,-14.21,;13,-13.38,;11.63,-14.08,;11.56,-15.62,;10.23,-16.39,;12.86,-16.45,;14.22,-15.75,;21.03,-12.96,;22.36,-12.19,;23.69,-12.96,;25.03,-12.19,;26.36,-12.96,;27.69,-12.19,;27.69,-10.65,;26.36,-9.88,;29.03,-9.88,;30.36,-10.65,;30.36,-12.19,;29.03,-12.96,;29.03,-14.5,;30.34,-19.93,;30.29,-21.47,)|
Structure:
Search PDB for entries with ligand similarity:
Substrate
Name:
Poly(E:Y)
Synonyms:
n/a
Type:
Random polymer
Mol. Mass.:
358.43
Organism:
n/a
Description:
Random copolymer of glutamic acid and tyrosine (4:1). 50 uM ATP containing 0.4 uCi of [gamma-32P]ATP as co-substrate
Residue:
3
Sequence:
NA