| Reaction Details |
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 | Report a problem with these data |
| Target | VHL complex |
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| Ligand | BDBM454897 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | Fluorescence Polarization Assay (10% in DMSO) |
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| IC50 | 293±n/a nM |
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| Citation |  Crew, AP; Crews, CM; Chen, X; Dong, H; Ferraro, C; Qian, Y; Siu, K; Wang, J; Jin, M; Berlin, M; Zimmermann, K Compounds and methods for the enhanced degradation of targeted proteins US Patent US11512083 Publication Date 11/29/2022 |
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| More Info.: | Get all data from this article, Assay Method |
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| VHL complex |
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| Name: | VHL complex |
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| Synonyms: | n/a |
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| Type: | Protein |
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| Mol. Mass.: | n/a |
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| Description: | n/a |
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| Components: | This complex has 3 components. |
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| Component 1 |
| Name: | von Hippel-Lindau disease tumor suppressor |
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| Synonyms: | Protein G7 | VHL | VHL_HUMAN | Von Hippel-Lindau disease tumor suppressor | Von Hippel-Lindau disease tumor suppressor protein (VBC) | pVHL |
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| Type: | Protein |
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| Mol. Mass.: | 24136.87 |
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| Organism: | Homo sapiens (Human) |
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| Description: | P40337 |
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| Residue: | 213 |
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| Sequence: | MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPR
PVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFR
DAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDI
VRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
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| Component 2 |
| Name: | Cullin-2 |
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| Synonyms: | CUL-2 | CUL2 | CUL2_HUMAN |
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| Type: | Protein |
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| Mol. Mass.: | 86987.14 |
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| Organism: | Human |
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| Description: | Q13617 |
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| Residue: | 745 |
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| Sequence: | MSLKPRVVDFDETWNKLLTTIKAVVMLEYVERATWNDRFSDIYALCVAYPEPLGERLYTE
TKIFLENHVRHLHKRVLESEEQVLVMYHRYWEEYSKGADYMDCLYRYLNTQFIKKNKLTE
ADLQYGYGGVDMNEPLMEIGELALDMWRKLMVEPLQAILIRMLLREIKNDRGGEDPNQKV
IHGVINSFVHVEQYKKKFPLKFYQEIFESPFLTETGEYYKQEASNLLQESNCSQYMEKVL
GRLKDEEIRCRKYLHPSSYTKVIHECQQRMVADHLQFLHAECHNIIRQEKKNDMANMYVL
LRAVSTGLPHMIQELQNHIHDEGLRATSNLTQENMPTLFVESVLEVHGKFVQLINTVLNG
DQHFMSALDKALTSVVNYREPKSVCKAPELLAKYCDNLLKKSAKGMTENEVEDRLTSFIT
VFKYIDDKDVFQKFYARMLAKRLIHGLSMSMDSEEAMINKLKQACGYEFTSKLHRMYTDM
SVSADLNNKFNNFIKNQDTVIDLGISFQIYVLQAGAWPLTQAPSSTFAIPQELEKSVQMF
ELFYSQHFSGRKLTWLHYLCTGEVKMNYLGKPYVAMVTTYQMAVLLAFNNSETVSYKELQ
DSTQMNEKELTKTIKSLLDVKMINHDSEKEDIDAESSFSLNMNFSSKRTKFKITTSMQKD
TPQEMEQTRSAVDEDRKMYLQAAIVRIMKARKVLRHNALIQEVISQSRARFNPSISMIKK
CIEVLIDKQYIERSQASADEYSYVA
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| Component 3 |
| Name: | E3 ubiquitin-protein ligase RBX1 |
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| Synonyms: | E3 ubiquitin-protein transferase RBX1 | Protein ZYP | RBX1 | RBX1_HUMAN | RING finger protein 75 | RING-box protein 1 | RNF75 | ROC1 | Regulator of cullins 1 |
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| Type: | Protein |
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| Mol. Mass.: | 12275.36 |
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| Organism: | Human |
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| Description: | P62877 |
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| Residue: | 108 |
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| Sequence: | MAAAMDVDTPSGTNSGAGKKRFEVKKWNAVALWAWDIVVDNCAICRNHIMDLCIECQANQ
ASATSEECTVAWGVCNHAFHFHCISRWLKTRQVCPLDNREWEFQKYGH
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| BDBM454897 |
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| n/a |
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| Name | BDBM454897 |
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| Synonyms: | US10730870, Example 60 | US11512083, Example 60 |
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| Type | Small organic molecule |
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| Emp. Form. | C50H66N8O8S4 |
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| Mol. Mass. | 1035.368 |
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| SMILES | CC(C)CCC(=O)N[C@H](CSSC[C@H](NC(=O)CCC(C)C)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(cc1)-c1scnc1C)C(=O)N1C[C@@H](O)C[C@@H]1C(=O)NCc1ccc(cc1)-c1scnc1C |r| |
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| Structure | 
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