Reaction Details |
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Target | Platelet-derived growth factor receptor alpha/beta |
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Ligand | BDBM50187343 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_357669 (CHEMBL854265) |
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IC50 | 6100±n/a nM |
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Citation | Mahboobi, S; Uecker, A; Sellmer, A; Cénac, C; Höcher, H; Pongratz, H; Eichhorn, E; Hufsky, H; Trümpler, A; Sicker, M; Heidel, F; Fischer, T; Stocking, C; Elz, S; Böhmer, FD; Dove, S Novel bis(1H-indol-2-yl)methanones as potent inhibitors of FLT3 and platelet-derived growth factor receptor tyrosine kinase. J Med Chem49:3101-15 (2006) [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/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 |
Type: | n/a |
Mol. Mass.: | n/a |
Description: | ASSAY_ID of EBI is 454 |
Components: | This complex has 2 components. |
Component 1 |
Name: | Platelet-derived growth factor receptor beta |
Synonyms: | 2.7.10.1 | Beta platelet-derived growth factor receptor | Beta-type platelet-derived growth factor receptor | CD140 antigen-like family member B | CD140b antigen | CD_antigen=CD140b | PDGF-R-beta | PDGFR-1 | PDGFR-beta | PGFRB_MOUSE | Pdgfr | Pdgfr1 | Pdgfrb | Platelet-Derived Growth Factor Receptor, beta | Platelet-derived growth factor receptor | Platelet-derived growth factor receptor 1 |
Type: | Enzyme |
Mol. Mass.: | 122771.00 |
Organism: | Mus musculus (mouse) |
Description: | P05622 |
Residue: | 1098 |
Sequence: | MGLPGVIPALVLRGQLLLSVLWLLGPQTSRGLVITPPGPEFVLNISSTFVLTCSGSAPVM
WEQMSQVPWQEAAMNQDGTFSSVLTLTNVTGGDTGEYFCVYNNSLGPELSERKRIYIFVP
DPTMGFLPMDSEDLFIFVTDVTETTIPCRVTDPQLEVTLHEKKVDIPLHVPYDHQRGFTG
TFEDKTYICKTTIGDREVDSDTYYVYSLQVSSINVSVNAVQTVVRQGESITIRCIVMGND
VVNFQWTYPRMKSGRLVEPVTDYLFGVPSRIGSILHIPTAELSDSGTYTCNVSVSVNDHG
DEKAINISVIENGYVRLLETLGDVEIAELHRSRTLRVVFEAYPMPSVLWLKDNRTLGDSG
AGELVLSTRNMSETRYVSELILVRVKVSEAGYYTMRAFHEDDEVQLSFKLQVNVPVRVLE
LSESHPANGEQTIRCRGRGMPQPNVTWSTCRDLKRCPRKLSPTPLGNSSKEESQLETNVT
FWEEDQEYEVVSTLRLRHVDQPLSVRCMLQNSMGGDSQEVTVVPHSLPFKVVVISAILAL
VVLTVISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPVQLPYDSTWELPRDQLV
LGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGPH
LNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQRHSNKHCPPSAELYSNALP
VGFSLPSHLNLTGESDGGYMDMSKDESIDYVPMLDMKGDIKYADIESPSYMAPYDNYVPS
APERTYRATLINDSPVLSYTDLVGFSYQVANGMDFLASKNCVHRDLAARNVLICEGKLVK
ICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLGG
TPYPELPMNDQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFETRPPFSQLVLLLERL
LGEGYKKKYQQVDEEFLRSDHPAILRSQARFPGIHSLRSPLDTSSVLYTAVQPNESDNDY
IIPLPDPKPDVADEGLPEGSPSLASSTLNEVNTSSTISCDSPLELQEEPQQAEPEAQLEQ
PQDSGCPGPLAEAEDSFL
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Component 2 |
Name: | Platelet-derived growth factor receptor alpha |
Synonyms: | PGFRA_MOUSE | Pdgfra | Platelet-derived growth factor receptor |
Type: | PROTEIN |
Mol. Mass.: | 122646.66 |
Organism: | Mus musculus |
Description: | EBI_12628 |
Residue: | 1089 |
Sequence: | MGTSHQVFLVLSCLLTGPGLISCQLLLPSILPNENEKIVQLNSSFSLRCVGESEVSWQHP
MSEEDDPNVEIRSEENNSGLFVTVLEVVNASAAHTGWYTCYYNHTQTDESEIEGRHIYIY
VPDPDMAFVPLGMTDSLVIVEEDDSAIIPCRTTDPETQVTLHNNGRLVPASYDSRQGFNG
TFSVGPYICEATVKGRTFKTSEFNVYALKATSELNLEMDARQTVYKAGETIVVTCAVFNN
EVVDLQWTYPGEVRNKGITMLEEIKLPSIKLVYTLTVPKATVKDSGEYECAARQATKEVK
EMKRVTISVHEKGFVEIEPTFGQLEAVNLHEVREFVVEVQAYPTPRISWLKDNLTLIENL
TEITTDVQKSQETRYQSKLKLIRAKEEDSGHYTIIVQNEDDVKSYTFELSTLVPASILDL
VDDHHGSGGGQTVRCTAEGTPLPEIDWMICKHIKKCNNDTSWTVLASNVSNIITELPRRG
RSTVEGRVSFAKVEETIAVRCLAKNNLSVVARELKLVAPTLRSELTVAAAVLVLLVIVIV
SLIVLVVIWKQKPRYEIRWRVIESISPDGHEYIYVDPMQLPYDSRWEFPRDGLVLGRILG
SGAFGKVVEGTAYGLSRSQPVMKVAVKMLKPTARSSEKQALMSELKIMTHLGPHLNIVNL
LGACTKSGPIYIITEYCFYGDLVNYLHKNRDSFMSQHPEKPKKDLDIFGLNPADESTRSY
VILSFENNGDYMDMKQADTTQYVPMLERKEVSKYSDIQRSLYDRPASYKKKSMLDSEVKN
LLSDDDSEGLTLLDLLSFTYQVARGMEFLASKNCVHRDLAARNVLLAQGKIVKICDFGLA
RDIMHDSNYVSKGSTFLPVKWMAPESIFDNLYTTLSDVWSYGILLWEIFSLGGTPYPGMM
VDSTFYNKIKSGYRMAKPDHATSEVYEIMVQCWNSEPEKRPSFYHLSEIVENLLPGQYKK
SYEKIHLDFLKSDHPAVARMRVDSDNAYIGVTYKNEEDKLKDWEGGLDEQRLSADSGYII
PLPDIDPVPEEEDLGKRNRHSSQTSEESAIETGSSSSTFIKREDETIEDIDMMDDIGIDS
SDLVEDSFL
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BDBM50187343 |
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n/a |
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Name | BDBM50187343 |
Synonyms: | (4-Bromo-1H-indol-2-yl)-(5-hydroxy-1H-indol-2-yl)-methanone | CHEMBL210726 |
Type | Small organic molecule |
Emp. Form. | C17H11BrN2O2 |
Mol. Mass. | 355.185 |
SMILES | Oc1ccc2[nH]c(cc2c1)C(=O)c1cc2c(Br)cccc2[nH]1 |
Structure |
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