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Target
Elongin-B/Elongin-C [17-112]/von Hippel-Lindau disease tumor suppressor [55-213]
Ligand
BDBM536240
Substrate
n/a
Meas. Tech.
Fluorescence Polarization (FP) VHL Binding Assay
IC50
4970±n/a nM
Citation
 Blaquiere, N; Dragovich, P; Gazzard, LJ; Pillow, T; Staben, ST; Wei, B; Xin, J (4-hydroxypyrrolidin-2-yl)-heterocyclic compounds and methods of use thereof US Patent  US11242344 Publication Date 2/8/2022 
Target
Name:
Elongin-B/Elongin-C [17-112]/von Hippel-Lindau disease tumor suppressor [55-213]
Synonyms:
VHL Elongin B/C complex
Type:
Protein
Mol. Mass.:
n/a
Description:
n/a
Components:
This complex has 3 components.
Component 1
Name:
von Hippel-Lindau disease tumor suppressor [55-213]
Synonyms:
VHL | VHL (aa 55-213) | VHL_HUMAN
Type:
Protein
Mol. Mass.:
18405.28
Organism:
Homo sapiens (Human)
Description:
P40337[55-213]
Residue:
159
Sequence:
EAGRPRPVLRSVNSREPSQVIFCNRSPRVVLPVWLNFDGEPQPYPTLPPGTGRRIHSYRGHLWLFRDAGTHDGLLVNQTELFVPSLNVDGQPIFANITLPVYTLKERCLQVVRSLVKPENYRRLDIVRSLYEDLEDHPNVQKDLERLTQERIAHQRMGD
  
Component 2
Name:
Elongin-B
Synonyms:
ELOB | ELOB_HUMAN | Elongin 18 kDa subunit | Elongin-B | RNA polymerase II transcription factor SIII subunit B | SIII p18 | TCEB2 | Transcription elongation factor B polypeptide 2
Type:
PROTEIN
Mol. Mass.:
13127.13
Organism:
Homo sapiens (Human)
Description:
ChEMBL_108414
Residue:
118
Sequence:
MDVFLMIRRHKTTIFTDAKESSTVFELKRIVEGILKRPPDEQRLYKDDQLLDDGKTLGECGFTSQTARPQAPATVGLAFRADDTFEALCIEPFSSPPELPDVMKPQDSGSSANEQAVQ
  
Component 3
Name:
Elongin-C [17-112]
Synonyms:
ELOC | ELOC_HUMAN | TCEB1 | Transcription elongation factor B polypeptide 1 (aa 17-112)
Type:
PROTEIN
Mol. Mass.:
10829.81
Organism:
Homo sapiens (Human)
Description:
n/a
Residue:
96
Sequence:
MYVKLISSDGHEFIVKREHALTSGTIKAMLSGPGQFAENETNEVNFREIPSHVLSKVCMYFTYKVRYTNSSTEIPEFPIAPEIALELLMAANFLDC
  
Inhibitor
Name:
BDBM536240
Synonyms:
1-Cyano-N-((2S)-1-((4R)-4-hydroxy-2-((S)-5-methyl-5-(4-(4-methylthiazol-5-yl)phenyl)-4-oxo-4,5-dihydro-1H-imidazol-2-yl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)cyclopropane-1-carboxamide (2 Single Stereoisomers) | US11242344, Example 111.1 | US11242344, Example 111.2
Type:
Small organic molecule
Emp. Form.:
C29H39N5O5S
Mol. Mass.:
569.715
SMILES:
Cc1ncsc1-c1ccc(cc1)[C@]1(C)NC(=NC1=O)C1C[C@@H](O)CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)(C)C |r,c:17|
Structure:
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