| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Platelet-derived growth factor receptor alpha/beta |
|---|
| Ligand | BDBM50132408 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_158496 (CHEMBL765709) |
|---|
| IC50 | 3100±n/a nM |
|---|
| Citation |  He, W; Myers, MR; Hanney, B; Spada, AP; Bilder, G; Galzcinski, H; Amin, D; Needle, S; Page, K; Jayyosi, Z; Perrone, MH Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 2: the synthesis and biological activities of RPR127963 an orally bioavailable inhibitor. Bioorg Med Chem Lett13:3097-100 (2003) [PubMed] |
|---|
| More Info.: | Get all data from this article, Assay Method |
|---|
| |
| Platelet-derived growth factor receptor alpha/beta |
|---|
| Name: | Platelet-derived growth factor receptor alpha/beta |
|---|
| Synonyms: | PDGFR-beta/Platelet-derived growth factor receptor alpha | Platelet-derived growth factor receptor | Platelet-derived growth factor receptor alpha /beta |
|---|
| Type: | n/a |
|---|
| Mol. Mass.: | n/a |
|---|
| Description: | ASSAY_ID of EBI is 29498 |
|---|
| Components: | This complex has 2 components. |
|---|
| Component 1 |
| 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: | MRLPGAMPALALKGELLLLSLLLLLEPQISQGLVVTPPGPELVLNVSSTFVLTCSGSAPV
VWERMSQEPPQEMAKAQDGTFSSVLTLTNLTGLDTGEYFCTHNDSRGLETDERKRLYIFV
PDPTVGFLPNDAEELFIFLTEITEITIPCRVTDPQLVVTLHEKKGDVALPVPYDHQRGFS
GIFEDRSYICKTTIGDREVDSDAYYVYRLQVSSINVSVNAVQTVVRQGENITLMCIVIGN
EVVNFEWTYPRKESGRLVEPVTDFLLDMPYHIRSILHIPSAELEDSGTYTCNVTESVNDH
QDEKAINITVVESGYVRLLGEVGTLQFAELHRSRTLQVVFEAYPPPTVLWFKDNRTLGDS
SAGEIALSTRNVSETRYVSELTLVRVKVAEAGHYTMRAFHEDAEVQLSFQLQINVPVRVL
ELSESHPDSGEQTVRCRGRGMPQPNIIWSACRDLKRCPRELPPTLLGNSSEEESQLETNV
TYWEEEQEFEVVSTLRLQHVDRPLSVRCTLRNAVGQDTQEVIVVPHSLPFKVVVISAILA
LVVLTIISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPMQLPYDSTWELPRDQL
VLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGP
HLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQHHSDKRRPPSAELYSNAL
PVGLPLPSHVSLTGESDGGYMDMSKDESVDYVPMLDMKGDVKYADIESSNYMAPYDNYVP
SAPERTCRATLINESPVLSYMDLVGFSYQVANGMEFLASKNCVHRDLAARNVLICEGKLV
KICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLG
GTPYPELPMNEQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFEIRPPFSQLVLLLER
LLGEGYKKKYQQVDEEFLRSDHPAILRSQARLPGFHGLRSPLDTSSVLYTAVQPNEGDND
YIIPLPDPKPEVADEGPLEGSPSLASSTLNEVNTSSTISCDSPLEPQDEPEPEPQLELQV
EPEPELEQLPDSGCPAPRAEAEDSFL
|
|
|
|---|
| Component 2 |
| Name: | Platelet-derived growth factor receptor alpha |
|---|
| Synonyms: | Alpha-type platelet-derived growth factor receptor | PDGFR2 | PDGFRA | PDGFRalpha | PGFRA_HUMAN | Platelet-derived growth factor receptor alpha (PDGFR-alpha) | Platelet-derived growth factor receptor alpha (PDGFRA) | Platelet-derived growth factor receptor, alpha polypeptid | RHEPDGFRA |
|---|
| Type: | Protein |
|---|
| Mol. Mass.: | 122633.38 |
|---|
| Organism: | Homo sapiens (Human) |
|---|
| Description: | P16234 |
|---|
| Residue: | 1089 |
|---|
| Sequence: | MGTSHPAFLVLGCLLTGLSLILCQLSLPSILPNENEKVVQLNSSFSLRCFGESEVSWQYP
MSEEESSDVEIRNEENNSGLFVTVLEVSSASAAHTGLYTCYYNHTQTEENELEGRHIYIY
VPDPDVAFVPLGMTDYLVIVEDDDSAIIPCRTTDPETPVTLHNSEGVVPASYDSRQGFNG
TFTVGPYICEATVKGKKFQTIPFNVYALKATSELDLEMEALKTVYKSGETIVVTCAVFNN
EVVDLQWTYPGEVKGKGITMLEEIKVPSIKLVYTLTVPEATVKDSGDYECAARQATREVK
EMKKVTISVHEKGFIEIKPTFSQLEAVNLHEVKHFVVEVRAYPPPRISWLKNNLTLIENL
TEITTDVEKIQEIRYRSKLKLIRAKEEDSGHYTIVAQNEDAVKSYTFELLTQVPSSILDL
VDDHHGSTGGQTVRCTAEGTPLPDIEWMICKDIKKCNNETSWTILANNVSNIITEIHSRD
RSTVEGRVTFAKVEETIAVRCLAKNLLGAENRELKLVAPTLRSELTVAAAVLVLLVIVII
SLIVLVVIWKQKPRYEIRWRVIESISPDGHEYIYVDPMQLPYDSRWEFPRDGLVLGRVLG
SGAFGKVVEGTAYGLSRSQPVMKVAVKMLKPTARSSEKQALMSELKIMTHLGPHLNIVNL
LGACTKSGPIYIITEYCFYGDLVNYLHKNRDSFLSHHPEKPKKELDIFGLNPADESTRSY
VILSFENNGDYMDMKQADTTQYVPMLERKEVSKYSDIQRSLYDRPASYKKKSMLDSEVKN
LLSDDNSEGLTLLDLLSFTYQVARGMEFLASKNCVHRDLAARNVLLAQGKIVKICDFGLA
RDIMHDSNYVSKGSTFLPVKWMAPESIFDNLYTTLSDVWSYGILLWEIFSLGGTPYPGMM
VDSTFYNKIKSGYRMAKPDHATSEVYEIMVKCWNSEPEKRPSFYHLSEIVENLLPGQYKK
SYEKIHLDFLKSDHPAVARMRVDSDNAYIGVTYKNEEDKLKDWEGGLDEQRLSADSGYII
PLPDIDPVPEEEDLGKRNRHSSQTSEESAIETGSSSSTFIKREDETIEDIDMMDDIGIDS
SDLVEDSFL
|
|
|
|---|
| BDBM50132408 |
|---|
| n/a |
|---|
| Name | BDBM50132408 |
|---|
| Synonyms: | 4-(6,7-Dimethoxy-quinoxalin-2-ylamino)-cyclohexanecarboxylic acid methylamide | CHEMBL104581 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C18H24N4O3 |
|---|
| Mol. Mass. | 344.4082 |
|---|
| SMILES | CNC(=O)C1CCC(CC1)Nc1cnc2cc(OC)c(OC)cc2n1 |(7.11,-2.19,;5.77,-1.42,;5.76,.12,;7.1,.88,;4.43,.88,;4.43,2.42,;3.1,3.19,;1.78,2.41,;1.78,.88,;3.1,.11,;.44,3.18,;-.88,2.4,;-.88,.85,;-2.23,.07,;-3.55,.84,;-4.89,.07,;-6.22,.84,;-7.56,.07,;-7.56,-1.47,;-6.22,2.37,;-7.56,3.16,;-8.88,2.39,;-4.89,3.16,;-3.55,2.39,;-2.23,3.16,)| |
|---|
| Structure | 
|
|---|
Search and Browse
