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Target
Elongin-B/Elongin-C [17-112]/von Hippel-Lindau disease tumor suppressor [55-213]
Ligand
BDBM536239
Substrate
n/a
Meas. Tech.
Fluorescence Polarization (FP) VHL Binding Assay
IC50
19900±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:
BDBM536239
Synonyms:
(2R)-1-((4R)-2-(3,4-dihydro-2H,4'H-spiro[naphthalene-1,5'-[1,2,4]oxadiazol]-3'-yl)-4-hydroxypyrrolidin-1-yl)-3-methyl-2-(3-methylisoxazol-5-yl)butan-1-one | US11242344, Example 131.3 | US11242344, Example 131.4
Type:
Small organic molecule
Emp. Form.:
C24H30N4O4
Mol. Mass.:
438.5194
SMILES:
CC(C)[C@@H](C(=O)N1C[C@H](O)CC1C1=NOC2(CCCc3ccccc23)N1)c1cc(C)no1 |r,t:13|
Structure:
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