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Target
Endothelial PAS domain-containing protein 1/Hypoxia-inducible factor 1-alpha
Ligand
BDBM50478890
Substrate
n/a
Meas. Tech.
ChEMBL_526045 (CHEMBL967263)
IC50
8.7±n/a nM
Citation
 Cai, XF; Jin, X; Lee, D; Yang, YT; Lee, K; Hong, YS; Lee, JH; Lee, JJ Phenanthroquinolizidine alkaloids from the roots of Boehmeria pannosa potently inhibit hypoxia-inducible factor-1 in AGS human gastric cancer cells. J Nat Prod 69:1095-7 (2006) [PubMed]  Article 
Target
Name:
Endothelial PAS domain-containing protein 1/Hypoxia-inducible factor 1-alpha
Synonyms:
Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha
Type:
n/a
Mol. Mass.:
n/a
Description:
ASSAY_ID of ChEMBL is 799337
Components:
This complex has 2 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:
Endothelial PAS domain-containing protein 1
Synonyms:
BHLHE73 | EPAS1 | EPAS1_HUMAN | HIF2A | MOP2 | PASD2 | endothelial PAS domain-containing protein 1
Type:
PROTEIN
Mol. Mass.:
96453.58
Organism:
Homo sapiens (Human)
Description:
ChEMBL_1506501
Residue:
870
Sequence:
MTADKEKKRSSSERRKEKSRDAARCRRSKETEVFYELAHELPLPHSVSSHLDKASIMRLAISFLRTHKLLSSVCSENESEAEADQQMDNLYLKALEGFIAVVTQDGDMIFLSENISKFMGLTQVELTGHSIFDFTHPCDHEEIRENLSLKNGSGFGKKSKDMSTERDFFMRMKCTVTNRGRTVNLKSATWKVLHCTGQVKVYNNCPPHNSLCGYKEPLLSCLIIMCEPIQHPSHMDIPLDSKTFLSRHSMDMKFTYCDDRITELIGYHPEELLGRSAYEFYHALDSENMTKSHQNLCTKGQVVSGQYRMLAKHGGYVWLETQGTVIYNPRNLQPQCIMCVNYVLSEIEKNDVVFSMDQTESLFKPHLMAMNSIFDSSGKGAVSEKSNFLFTKLKEEPEELAQLAPTPGDAIISLDFGNQNFEESSAYGKAILPPSQPWATELRSHSTQSEAGSLPAFTVPQAAAPGSTTPSATSSSSSCSTPNSPEDYYTSLDNDLKIEVIEKLFAMDTEAKDQCSTQTDFNELDLETLAPYIPMDGEDFQLSPICPEERLLAENPQSTPQHCFSAMTNIFQPLAPVAPHSPFLLDKFQQQLESKKTEPEHRPMSSIFFDAGSKASLPPCCGQASTPLSSMGGRSNTQWPPDPPLHFGPTKWAVGDQRTEFLGAAPLGPPVSPPHVSTFKTRSAKGFGARGPDVLSPAMVALSNKLKLKRQLEYEEQAFQDLSGGDPPGGSTSHLMWKRMKNLRGGSCPLMPDKPLSANVPNDKFTQNPMRGLGHPLRHLPLPQPPSAISPGENSKSRFPPQCYATQYQDYSLSSAHKVSGMASRLLGPSFESYLLPELTRYDCEVNVPVLGSSTLLQGGDLLRALDQAT
  
Inhibitor
Name:
BDBM50478890
Synonyms:
(-)-Cryptopleurine | CHEBI:3932 | Cryptopleurine | R-Cryptopleurine
Type:
Small organic molecule
Emp. Form.:
C24H27NO3
Mol. Mass.:
377.4761
SMILES:
[H][C@]12CCCCN1Cc1c(C2)c2cc(OC)c(OC)cc2c2cc(OC)ccc12 |r|
Structure:
Search PDB for entries with ligand similarity: