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Target
Endothelial PAS domain-containing protein 1/Hypoxia-inducible factor 1-alpha
Ligand
BDBM51317
Substrate
n/a
Meas. Tech.
ChEMBL_439941 (CHEMBL890258)
IC50
8510±n/a nM
Citation
 Dat, NT; Jin, X; Lee, JH; Lee, D; Hong, YS; Lee, K; Kim, YH; Lee, JJ Abietane diterpenes from Salvia miltiorrhiza inhibit the activation of hypoxia-inducible factor-1. J Nat Prod 70:1093-7 (2007) [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:
BDBM51317
Synonyms:
1,6-dimethylnaphtho[1,2-g][1]benzofuran-10,11-dione | 1,6-dimethylnaphtho[1,2-g]benzofuran-10,11-dione | 1,6-dimethylnaphtho[1,2-g]benzofuran-10,11-quinone | MLS000697676 | SMR000445578 | TANSHINONE I | acs.jmedchem.1c00409_ST.675 | cid_114917
Type:
Small organic molecule
Emp. Form.:
C18H12O3
Mol. Mass.:
276.2861
SMILES:
Cc1coc-2c1C(=O)C(=O)c1c-2ccc2c(C)cccc12
Structure:
Search PDB for entries with ligand similarity: