Reaction Details
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Platelet-derived growth factor receptor alpha/beta
Ligand
BDBM50568726
Substrate
n/a
Meas. Tech.
ChEMBL_2290924
IC50
<10.0±n/a nM
Citation
Durcik, M; Cotman, AE; Toplak, ?; Mo?ina, ?; Skok, ?; Szili, PE; Czikkely, M; Maharramov, E; Vu, TH; Piras, MV; Zidar, N; Ila?, J; Zega, A; Trontelj, J; Pardo, LA; Hughes, D; Huseby, D; Berruga-Fernández, T; Cao, S; Simoff, I; Svensson, R; Korol, SV; Jin, Z; Vicente, F; Ramos, MC; Mundy, JEA; Maxwell, A; Stevenson, CEM; Lawson, DM; Glinghammar, B; Sjöström, E; Bohlin, M; Oreskär, J; Alvér, S; Janssen, GV; Sterk, GJ; Kikelj, D; Pal, C; Toma?i?, T; Peterlin Ma?i?, L New Dual Inhibitors of Bacterial Topoisomerases with Broad-Spectrum Antibacterial Activity and In Vivo Efficacy against Vancomycin-Intermediate J Med Chem 66:3968-3994 (2023) [PubMed] More Info.:
Target
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:
MGLPGVIPALVLRGQLLLSVLWLLGPQTSRGLVITPPGPEFVLNISSTFVLTCSGSAPVMWEQMSQVPWQEAAMNQDGTFSSVLTLTNVTGGDTGEYFCVYNNSLGPELSERKRIYIFVPDPTMGFLPMDSEDLFIFVTDVTETTIPCRVTDPQLEVTLHEKKVDIPLHVPYDHQRGFTGTFEDKTYICKTTIGDREVDSDTYYVYSLQVSSINVSVNAVQTVVRQGESITIRCIVMGNDVVNFQWTYPRMKSGRLVEPVTDYLFGVPSRIGSILHIPTAELSDSGTYTCNVSVSVNDHGDEKAINISVIENGYVRLLETLGDVEIAELHRSRTLRVVFEAYPMPSVLWLKDNRTLGDSGAGELVLSTRNMSETRYVSELILVRVKVSEAGYYTMRAFHEDDEVQLSFKLQVNVPVRVLELSESHPANGEQTIRCRGRGMPQPNVTWSTCRDLKRCPRKLSPTPLGNSSKEESQLETNVTFWEEDQEYEVVSTLRLRHVDQPLSVRCMLQNSMGGDSQEVTVVPHSLPFKVVVISAILALVVLTVISLIILIMLWQKKPRYEIRWKVIESVSSDGHEYIYVDPVQLPYDSTWELPRDQLVLGRTLGSGAFGQVVEATAHGLSHSQATMKVAVKMLKSTARSSEKQALMSELKIMSHLGPHLNVVNLLGACTKGGPIYIITEYCRYGDLVDYLHRNKHTFLQRHSNKHCPPSAELYSNALPVGFSLPSHLNLTGESDGGYMDMSKDESIDYVPMLDMKGDIKYADIESPSYMAPYDNYVPSAPERTYRATLINDSPVLSYTDLVGFSYQVANGMDFLASKNCVHRDLAARNVLICEGKLVKICDFGLARDIMRDSNYISKGSTFLPLKWMAPESIFNSLYTTLSDVWSFGILLWEIFTLGGTPYPELPMNDQFYNAIKRGYRMAQPAHASDEIYEIMQKCWEEKFETRPPFSQLVLLLERLLGEGYKKKYQQVDEEFLRSDHPAILRSQARFPGIHSLRSPLDTSSVLYTAVQPNESDNDYIIPLPDPKPDVADEGLPEGSPSLASSTLNEVNTSSTISCDSPLELQEEPQQAEPEAQLEQPQDSGCPGPLAEAEDSFL
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:
MGTSHQVFLVLSCLLTGPGLISCQLLLPSILPNENEKIVQLNSSFSLRCVGESEVSWQHPMSEEDDPNVEIRSEENNSGLFVTVLEVVNASAAHTGWYTCYYNHTQTDESEIEGRHIYIYVPDPDMAFVPLGMTDSLVIVEEDDSAIIPCRTTDPETQVTLHNNGRLVPASYDSRQGFNGTFSVGPYICEATVKGRTFKTSEFNVYALKATSELNLEMDARQTVYKAGETIVVTCAVFNNEVVDLQWTYPGEVRNKGITMLEEIKLPSIKLVYTLTVPKATVKDSGEYECAARQATKEVKEMKRVTISVHEKGFVEIEPTFGQLEAVNLHEVREFVVEVQAYPTPRISWLKDNLTLIENLTEITTDVQKSQETRYQSKLKLIRAKEEDSGHYTIIVQNEDDVKSYTFELSTLVPASILDLVDDHHGSGGGQTVRCTAEGTPLPEIDWMICKHIKKCNNDTSWTVLASNVSNIITELPRRGRSTVEGRVSFAKVEETIAVRCLAKNNLSVVARELKLVAPTLRSELTVAAAVLVLLVIVIVSLIVLVVIWKQKPRYEIRWRVIESISPDGHEYIYVDPMQLPYDSRWEFPRDGLVLGRILGSGAFGKVVEGTAYGLSRSQPVMKVAVKMLKPTARSSEKQALMSELKIMTHLGPHLNIVNLLGACTKSGPIYIITEYCFYGDLVNYLHKNRDSFMSQHPEKPKKDLDIFGLNPADESTRSYVILSFENNGDYMDMKQADTTQYVPMLERKEVSKYSDIQRSLYDRPASYKKKSMLDSEVKNLLSDDDSEGLTLLDLLSFTYQVARGMEFLASKNCVHRDLAARNVLLAQGKIVKICDFGLARDIMHDSNYVSKGSTFLPVKWMAPESIFDNLYTTLSDVWSYGILLWEIFSLGGTPYPGMMVDSTFYNKIKSGYRMAKPDHATSEVYEIMVQCWNSEPEKRPSFYHLSEIVENLLPGQYKKSYEKIHLDFLKSDHPAVARMRVDSDNAYIGVTYKNEEDKLKDWEGGLDEQRLSADSGYIIPLPDIDPVPEEEDLGKRNRHSSQTSEESAIETGSSSSTFIKREDETIEDIDMMDDIGIDSSDLVEDSFL
Inhibitor
Name:
BDBM50568726
Synonyms:
CHEMBL4854181
Type:
Small organic molecule
Emp. Form.:
C21H15Cl2N3O4S
Mol. Mass.:
476.333
SMILES:
Cc1[nH]c(C(=O)Nc2nc3c(OCc4ccccc4)cc(cc3s2)C(O)=O)c(Cl)c1Cl
Structure:
