Reaction Details |
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Target | Platelet-derived growth factor receptor alpha/beta |
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Ligand | BDBM4850 |
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Substrate/Competitor | n/a |
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Meas. Tech. | Kinase Inhibition Assay |
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IC50 | >50000±n/a nM |
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Citation | Connolly, CJ; Hamby, JM; Schroeder, MC; Barvian, M; Lu, GH; Panek, RL; Amar, A; Shen, C; Kraker, AJ; Fry, DW; Klohs, WD; Doherty, AM DISCOVERY AND STRUCTURE-ACTIVITY STUDIES OF A NOVEL SERIES OF PYRIDO[2,3-d]PYRIMIDINE TYROSINE KINASE INHIBITORS Bioorg Med Chem Lett7:2415-20 (1997) Article |
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More Info.: | Get all data from this article, Assay Method |
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Platelet-derived growth factor receptor alpha/beta |
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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
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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
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BDBM4850 |
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n/a |
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Name | BDBM4850 |
Synonyms: | 1-{2-amino-6-[3,5-bis(dimethylamino)phenyl]pyrido[2,3-d]pyrimidin-7-yl}-3-tert-butylurea | CHEMBL50371 | PD089828 analog 31 |
Type | Small organic molecule |
Emp. Form. | C22H30N8O |
Mol. Mass. | 422.5266 |
SMILES | CN(C)c1cc(cc(c1)-c1cc2cnc(N)nc2nc1NC(=O)NC(C)(C)C)N(C)C |
Structure |
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