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Target
VHL complex
Ligand
BDBM454884
Substrate
n/a
Meas. Tech.
Fluorescence Polarization Assay (1% in DMSO)
IC50
178±n/a nM
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 
Target
Name:
VHL complex
Synonyms:
n/a
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 3 components.
Component 1
Name:
von Hippel-Lindau disease tumor suppressor
Synonyms:
Protein G7 | VHL | VHL_HUMAN | Von Hippel-Lindau disease tumor suppressor | Von Hippel-Lindau disease tumor suppressor protein (VBC) | pVHL
Type:
Protein
Mol. Mass.:
24136.87
Organism:
Homo sapiens (Human)
Description:
P40337
Residue:
213
Sequence:
MPRRAENWDEAEVGAEEAGVEEYGPEEDGGEESGAEESGPEESGPEELGAEEEMEAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
  
Component 2
Name:
Cullin-2
Synonyms:
CUL-2 | CUL2 | CUL2_HUMAN
Type:
Protein
Mol. Mass.:
86987.14
Organism:
Human
Description:
Q13617
Residue:
745
Sequence:
MSLKPRVVDFDETWNKLLTTIKAVVMLEYVERATWNDRFSDIYALCVAYPEPLGERLYTETKIFLENHVRHLHKRVLESEEQVLVMYHRYWEEYSKGADYMDCLYRYLNTQFIKKNKLTEADLQYGYGGVDMNEPLMEIGELALDMWRKLMVEPLQAILIRMLLREIKNDRGGEDPNQKVIHGVINSFVHVEQYKKKFPLKFYQEIFESPFLTETGEYYKQEASNLLQESNCSQYMEKVLGRLKDEEIRCRKYLHPSSYTKVIHECQQRMVADHLQFLHAECHNIIRQEKKNDMANMYVLLRAVSTGLPHMIQELQNHIHDEGLRATSNLTQENMPTLFVESVLEVHGKFVQLINTVLNGDQHFMSALDKALTSVVNYREPKSVCKAPELLAKYCDNLLKKSAKGMTENEVEDRLTSFITVFKYIDDKDVFQKFYARMLAKRLIHGLSMSMDSEEAMINKLKQACGYEFTSKLHRMYTDMSVSADLNNKFNNFIKNQDTVIDLGISFQIYVLQAGAWPLTQAPSSTFAIPQELEKSVQMFELFYSQHFSGRKLTWLHYLCTGEVKMNYLGKPYVAMVTTYQMAVLLAFNNSETVSYKELQDSTQMNEKELTKTIKSLLDVKMINHDSEKEDIDAESSFSLNMNFSSKRTKFKITTSMQKDTPQEMEQTRSAVDEDRKMYLQAAIVRIMKARKVLRHNALIQEVISQSRARFNPSISMIKKCIEVLIDKQYIERSQASADEYSYVA
  
Component 3
Name:
E3 ubiquitin-protein ligase RBX1
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
Type:
Protein
Mol. Mass.:
12275.36
Organism:
Human
Description:
P62877
Residue:
108
Sequence:
MAAAMDVDTPSGTNSGAGKKRFEVKKWNAVALWAWDIVVDNCAICRNHIMDLCIECQANQASATSEECTVAWGVCNHAFHFHCISRWLKTRQVCPLDNREWEFQKYGH
  
Inhibitor
Name:
BDBM454884
Synonyms:
US10730870, Example 47 | US11512083, Example 47
Type:
Small organic molecule
Emp. Form.:
C30H31N5O4S
Mol. Mass.:
557.663
SMILES:
CC(C)[C@H](N1Cc2cccc(C#N)c2C1=O)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(cc1)-c1scnc1C |r|
Structure:
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