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Target
Platelet-derived growth factor receptor beta
Ligand
BDBM50265539
Substrate
n/a
Meas. Tech.
ChEMBL_559890 (CHEMBL1011001)
IC50
1100±n/a nM
Citation
 Renhowe, PA; Pecchi, S; Shafer, CM; Machajewski, TD; Jazan, EM; Taylor, C; Antonios-McCrea, W; McBride, CM; Frazier, K; Wiesmann, M; Lapointe, GR; Feucht, PH; Warne, RL; Heise, CC; Menezes, D; Aardalen, K; Ye, H; He, M; Le, V; Vora, J; Jansen, JM; Wernette-Hammond, ME; Harris, AL Design, structure-activity relationships and in vivo characterization of 4-amino-3-benzimidazol-2-ylhydroquinolin-2-ones: a novel class of receptor tyrosine kinase inhibitors. J Med Chem 52:278-92 (2009) [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:
BDBM50265539
Synonyms:
4-hydroxy-3-(1-methyl-1H-benzo[d]imidazol-2-yl)quinolin-2(1H)-one | CHEMBL496172
Type:
Small organic molecule
Emp. Form.:
C17H13N3O2
Mol. Mass.:
291.304
SMILES:
Cn1c(nc2ccccc12)-c1c(O)c2ccccc2[nH]c1=O |(24.88,1.17,;24.55,2.67,;23.14,3.29,;23.3,4.82,;24.81,5.15,;25.56,6.48,;27.09,6.49,;27.87,5.16,;27.11,3.82,;25.57,3.82,;21.82,2.52,;20.47,3.3,;20.46,4.84,;19.13,2.51,;17.8,3.28,;16.47,2.5,;16.47,.96,;17.8,.19,;19.14,.96,;20.48,.19,;21.83,.97,;23.16,.2,)|
Structure:
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