Reaction Details |
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Target | Platelet-derived growth factor receptor alpha |
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Ligand | BDBM50604039 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2246340 (CHEMBL5160550) |
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IC50 | 102±n/a nM |
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Citation | Chen, X; Liu, L; Liu, P; Chen, Y; Lin, D; Yan, H; Yan, Q; Wang, Y; Qiu, Y; Fang, B; Huang, H; Qian, J; Zhao, Y; Du, Z; Zhang, Q; Li, X; Zheng, X; Liu, Z Discovery of Potent and Orally Bioavailable Platelet-Derived Growth Factor Receptor (PDGFR) Inhibitors for the Treatment of Osteosarcoma. J Med Chem65:5374-5391 (2022) [PubMed] 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 |
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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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BDBM50604039 |
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n/a |
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Name | BDBM50604039 |
Synonyms: | CHEMBL5177453 | US20230312529, Compound 6b |
Type | Small organic molecule |
Emp. Form. | C22H24N8 |
Mol. Mass. | 400.4796 |
SMILES | Cc1cnc(Nc2ccc(cc2)N2CCNCC2)nc1Nc1ccc2cn[nH]c2c1 |
Structure |
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