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Target
Platelet-derived growth factor receptor beta
Ligand
BDBM227812
Substrate
n/a
Meas. Tech.
PDGFRbeta Kinase Assay
pH
7.5±n/a
Temperature
295.15±n/a K
IC50
0.475±n/a nM
Comments
extracted
Citation
 Schall, A; Klar, J; Lobell, M; Schirok, H; Telser, J; Müller, S; Brohm, D; Briem, H; Jörißen, H; Keldenich, J; Böttger, M; Von Degenfeld, G; Schlange, T; Bömer, U; Lindner, N; Eilken, H; Hristodorov, D; Wasnaire, P; Gericke, KM; Bärfacker, L Substituted pyridobenzodiazepinone-derivatives and use thereof US Patent  US10047096 Publication Date 8/14/2018 
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:
BDBM227812
Synonyms:
4-[(2-Fluoro-5-hydroxy-4-methylphenyl)amino]-8-({[2-(pyridin-4-yl)ethyl]amino}methyl)-6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-one | US10047096, 74
Type:
Small organic molecule
Emp. Form.:
C27H25FN6O2
Mol. Mass.:
484.5248
SMILES:
Cc1cc(F)c(Nc2ccnc3Nc4ccc(CNCCc5ccncc5)cc4NC(=O)c23)cc1O
Structure:
Search PDB for entries with ligand similarity: