Reaction Details |
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Target | Platelet-derived growth factor receptor alpha/beta |
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Ligand | BDBM370121 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2276750 |
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Ki | 20±n/a nM |
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Citation | Freeman-Cook, KD; Hoffman, RL; Behenna, DC; Boras, B; Carelli, J; Diehl, W; Ferre, RA; He, YA; Hui, A; Huang, B; Huser, N; Jones, R; Kephart, SE; Lapek, J; McTigue, M; Miller, N; Murray, BW; Nagata, A; Nguyen, L; Niessen, S; Ninkovic, S; O'Doherty, I; Ornelas, MA; Solowiej, J; Sutton, SC; Tran, K; Tseng, E; Visswanathan, R; Xu, M; Zehnder, L; Zhang, Q; Zhang, C; Dann, S Discovery of PF-06873600, a CDK2/4/6 Inhibitor for the Treatment of Cancer. J Med Chem64:9056-9077 (2021) [PubMed] |
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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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BDBM370121 |
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n/a |
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Name | BDBM370121 |
Synonyms: | 6-(difluoromethyl)-8-[(1R,2R)-2-hydroxy-2-methylcyclopentyl]-2-{[1-(methylsulfonyl)piperidin-4-yl]amino}pyrido[2,3-d]pyrimidin-7(8H)-one | US10233188, Example 10 | US10800783, Example 10 | US11396512, Example 10 |
Type | Small organic molecule |
Emp. Form. | C20H27F2N5O4S |
Mol. Mass. | 471.521 |
SMILES | C[C@@]1(O)CCC[C@H]1n1c2nc(NC3CCN(CC3)S(C)(=O)=O)ncc2cc(C(F)F)c1=O |r| |
Structure |
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