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Target
Platelet-derived growth factor receptor beta
Ligand
BDBM50377352
Substrate
n/a
Meas. Tech.
ChEMBL_479561 (CHEMBL929425)
IC50
>2000±n/a nM
Citation
 Ruel, R; Thibeault, C; L'Heureux, A; Martel, A; Cai, ZW; Wei, D; Qian, L; Barrish, JC; Mathur, A; D'Arienzo, C; Hunt, JT; Kamath, A; Marathe, P; Zhang, Y; Derbin, G; Wautlet, B; Mortillo, S; Jeyaseelan, R; Henley, B; Tejwani, R; Bhide, RS; Trainor, GL; Fargnoli, J; Lombardo, LJ Discovery and preclinical studies of 5-isopropyl-6-(5-methyl-1,3,4-oxadiazol-2-yl)-N-(2-methyl-1H-pyrrolo[2,3-b]pyridin-5-yl)pyrrolo[2,1-f][1,2,4]triazin-4-amine (BMS-645737), an in vivo active potent VEGFR-2 inhibitor. Bioorg Med Chem Lett 18:2985-9 (2008) [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:
BDBM50377352
Synonyms:
BMS-645737 | CHEMBL261592
Type:
Small organic molecule
Emp. Form.:
C20H20N8O
Mol. Mass.:
388.4258
SMILES:
CC(C)c1c(cn2ncnc(Nc3cnc4[nH]c(C)cc4c3)c12)-c1nnc(C)o1
Structure:
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