Target
Platelet-derived growth factor receptor beta
Ligand
BDBM50265752
Substrate
n/a
Meas. Tech.
ChEMBL_559890 (CHEMBL1011001)
IC50
14±n/a nM
Citation
 Renhowe, PAPecchi, SShafer, CMMachajewski, TDJazan, EMTaylor, CAntonios-McCrea, WMcBride, CMFrazier, KWiesmann, MLapointe, GRFeucht, PHWarne, RLHeise, CCMenezes, DAardalen, KYe, HHe, MLe, VVora, JJansen, JMWernette-Hammond, MEHarris, 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:
BDBM50265752
Synonyms:
4-Amino-8-fluoro-3-[6-(4-methylpiperazinyl)benzimidazol-2-yl]hydroquinolin-2-one | CHEMBL526836
Type:
Small organic molecule
Emp. Form.:
C21H21FN6O
Mol. Mass.:
392.4294
SMILES:
CN1CCN(CC1)c1ccc2nc([nH]c2c1)-c1c(N)c2cccc(F)c2[nH]c1=O
Structure:
Search PDB for entries with ligand similarity: