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Target
Platelet-derived growth factor receptor beta
Ligand
BDBM4060
Substrate
Poly(E:Y)
Meas. Tech.
Kinase Inhibition Assay
IC50
6800±n/a nM
Citation
 Boschelli, DH; Wu, Z; Klutchko, SR; Showalter, HD; Hamby, JM; Lu, GH; Major, TC; Dahring, TK; Batley, B; Panek, RL; Keiser, J; Hartl, BG; Kraker, AJ; Klohs, WD; Roberts, BJ; Patmore, S; Elliott, WL; Steinkampf, R; Bradford, LA; Hallak, H; Doherty, AM Synthesis and tyrosine kinase inhibitory activity of a series of 2-amino-8H-pyrido[2,3-d]pyrimidines: identification of potent, selective platelet-derived growth factor receptor tyrosine kinase inhibitors. J Med Chem 41:4365-77 (1998) [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:
BDBM4060
Synonyms:
2-Amino-8-(3-benzyloxypropyl)-6-(2,6-dichlorophenyl)-8H-pyrido[2,3-d]pyrimidin-7-one | 2-amino-8-[3-(benzyloxy)propyl]-6-(2,6-dichlorophenyl)-7H,8H-pyrido[2,3-d]pyrimidin-7-one | pyrido[2,3-d]pyrimidin-7-one deriv. 15
Type:
Small organic molecule
Emp. Form.:
C23H20Cl2N4O2
Mol. Mass.:
455.337
SMILES:
Nc1ncc2cc(-c3c(Cl)cccc3Cl)c(=O)n(CCCOCc3ccccc3)c2n1 |(-6.98,-1.25,;-5.65,-.48,;-5.65,1.06,;-4.32,1.83,;-2.98,1.06,;-1.65,1.83,;-.32,1.06,;1.02,1.83,;1.02,3.37,;-.32,4.14,;2.35,4.14,;3.69,3.37,;3.69,1.83,;2.35,1.06,;2.35,-.48,;-.32,-.48,;1.02,-1.25,;-1.65,-1.25,;-1.65,-2.79,;-.32,-3.56,;-.32,-5.1,;1.02,-5.87,;1.02,-7.41,;2.35,-8.18,;2.35,-9.72,;3.69,-10.49,;5.02,-9.72,;5.02,-8.18,;3.69,-7.41,;-2.98,-.48,;-4.32,-1.25,)|
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