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Target
Elongin-B/Elongin-C/Hypoxia-inducible factor 1-alpha/von Hippel-Lindau disease tumor suppressor
Ligand
BDBM50459907
Substrate
n/a
Meas. Tech.
ChEMBL_1767523 (CHEMBL4219635)
IC50
5500±n/a nM
Citation
 Crew, AP; Raina, K; Dong, H; Qian, Y; Wang, J; Vigil, D; Serebrenik, YV; Hamman, BD; Morgan, A; Ferraro, C; Siu, K; Neklesa, TK; Winkler, JD; Coleman, KG; Crews, CM Identification and Characterization of Von Hippel-Lindau-Recruiting Proteolysis Targeting Chimeras (PROTACs) of TANK-Binding Kinase 1. J Med Chem 61:583-598 (2018) [PubMed]  Article 
Target
Name:
Elongin-B/Elongin-C/Hypoxia-inducible factor 1-alpha/von Hippel-Lindau disease tumor suppressor
Synonyms:
von Hippel-Lindau disease tumor suppressor/Elongin-C/Elongin-B/HIF1A
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 1767523
Components:
This complex has 4 components.
Component 1
Name:
Hypoxia-inducible factor 1-alpha
Synonyms:
BHLHE78 | HIF-1-alpha | HIF-1-alpha, HIF-2-alpha | HIF1A | HIF1A_HUMAN | Hypoxia inducible factors | Hypoxia-inducible factor 1 alpha | Hypoxia-inducible factor 1-alpha | MOP1 | PASD8 | von Hippel-Lindau disease tumor suppressor/Elongin-C/Elongin-B/HIF1A
Type:
Protein
Mol. Mass.:
92647.24
Organism:
Homo sapiens (Human)
Description:
Q16665
Residue:
826
Sequence:
MEGAGGANDKKKISSERRKEKSRDAARSRRSKESEVFYELAHQLPLPHNVSSHLDKASVMRLTISYLRVRKLLDAGDLDIEDDMKAQMNCFYLKALDGFVMVLTDDGDMIYISDNVNKYMGLTQFELTGHSVFDFTHPCDHEEMREMLTHRNGLVKKGKEQNTQRSFFLRMKCTLTSRGRTMNIKSATWKVLHCTGHIHVYDTNSNQPQCGYKKPPMTCLVLICEPIPHPSNIEIPLDSKTFLSRHSLDMKFSYCDERITELMGYEPEELLGRSIYEYYHALDSDHLTKTHHDMFTKGQVTTGQYRMLAKRGGYVWVETQATVIYNTKNSQPQCIVCVNYVVSGIIQHDLIFSLQQTECVLKPVESSDMKMTQLFTKVESEDTSSLFDKLKKEPDALTLLAPAAGDTIISLDFGSNDTETDDQQLEEVPLYNDVMLPSPNEKLQNINLAMSPLPTAETPKPLRSSADPALNQEVALKLEPNPESLELSFTMPQIQDQTPSPSDGSTRQSSPEPNSPSEYCFYVDSDMVNEFKLELVEKLFAEDTEAKNPFSTQDTDLDLEMLAPYIPMDDDFQLRSFDQLSPLESSSASPESASPQSTVTVFQQTQIQEPTANATTTTATTDELKTVTKDRMEDIKILIASPSPTHIHKETTSATSSPYRDTQSRTASPNRAGKGVIEQTEKSHPRSPNVLSVALSQRTTVPEEELNPKILALQNAQRKRKMEHDGSLFQAVGIGTLLQQPDDHAATTSLSWKRVKGCKSSEQNGMEQKTIILIPSDLACRLLGQSMDESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRALDQVN
  
Component 2
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 3
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 4
Name:
Elongin-C
Synonyms:
ELOC | ELOC_HUMAN | Elongin 15 kDa subunit | Elongin-C | RNA polymerase II transcription factor SIII subunit C | SIII p15 | TCEB1 | Transcription elongation factor B polypeptide 1
Type:
PROTEIN
Mol. Mass.:
12466.49
Organism:
Homo sapiens (Human)
Description:
ChEMBL_108414
Residue:
112
Sequence:
MDGEEKTYGGCEGPDAMYVKLISSDGHEFIVKREHALTSGTIKAMLSGPGQFAENETNEVNFREIPSHVLSKVCMYFTYKVRYTNSSTEIPEFPIAPEIALELLMAANFLDC
  
Inhibitor
Name:
BDBM50459907
Synonyms:
CHEMBL4225691
Type:
Small organic molecule
Emp. Form.:
C52H72BrN9O9S
Mol. Mass.:
1079.152
SMILES:
CC(C)[C@H](NC(=O)COCCCOCCCCOCCCOc1ccc(Nc2ncc(Br)c(NCCCN(C)C(=O)C3CCC3)n2)cc1)C(=O)N1C[C@H](O)C[C@H]1C(=O)NCc1ccc(cc1)-c1scnc1C |r|
Structure:
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