| Reaction Details |
|---|
 | Report a problem with these data |
| Target | Platelet-derived growth factor receptor alpha/beta |
|---|
| Ligand | BDBM50132391 |
|---|
| Substrate/Competitor | n/a |
|---|
| Meas. Tech. | ChEMBL_158494 (CHEMBL764773) |
|---|
| IC50 | 76±n/a nM |
|---|
| Citation |  Myers, MR; He, W; Hanney, B; Setzer, N; Maguire, MP; Zulli, A; Bilder, G; Galzcinski, H; Amin, D; Needle, S; Spada, AP Potent quinoxaline-based inhibitors of PDGF receptor tyrosine kinase activity. Part 1: SAR exploration and effective bioisosteric replacement of a phenyl substituent. Bioorg Med Chem Lett13:3091-5 (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
|
|
|
|---|
| BDBM50132391 |
|---|
| n/a |
|---|
| Name | BDBM50132391 |
|---|
| Synonyms: | 4-((R)-6,7-Dimethoxy-quinoxalin-2-ylamino)-cyclohexanol | 4-(6,7-Dimethoxy-quinoxalin-2-ylamino)-cyclohexanol | CHEMBL104466 | RP-127963 |
|---|
| Type | Small organic molecule |
|---|
| Emp. Form. | C16H21N3O3 |
|---|
| Mol. Mass. | 303.3562 |
|---|
| SMILES | COc1cc2ncc(N[C@H]3CC[C@H](O)CC3)nc2cc1OC |wU:12.12,wD:9.8,(-.13,-6.56,;-.13,-5.02,;1.2,-4.25,;2.53,-5.02,;3.88,-4.23,;5.21,-5,;6.54,-4.23,;6.54,-2.69,;7.85,-1.9,;9.2,-2.67,;9.2,-4.21,;10.53,-4.98,;11.86,-4.21,;13.19,-4.98,;11.86,-2.67,;10.53,-1.9,;5.19,-1.92,;3.88,-2.69,;2.53,-1.92,;1.2,-2.71,;-.13,-1.94,;-.13,-.4,)| |
|---|
| Structure | 
|
|---|
Search and Browse
