| Reaction Details |
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 | Report a problem with these data |
| Target | Endothelial PAS domain-containing protein 1/Hypoxia-inducible factor 1-alpha |
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| Ligand | BDBM50105278 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1506505 (CHEMBL3599971) |
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| IC50 | >30000±n/a nM |
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| Citation |  Scheuermann, TH; Stroud, D; Sleet, CE; Bayeh, L; Shokri, C; Wang, H; Caldwell, CG; Longgood, J; MacMillan, JB; Bruick, RK; Gardner, KH; Tambar, UK Isoform-Selective and Stereoselective Inhibition of Hypoxia Inducible Factor-2. J Med Chem58:5930-41 (2015) [PubMed] Article |
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| More Info.: | Get all data from this article, Assay Method |
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| Endothelial PAS domain-containing protein 1/Hypoxia-inducible factor 1-alpha |
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| Name: | Endothelial PAS domain-containing protein 1/Hypoxia-inducible factor 1-alpha |
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| Synonyms: | Hypoxia inducible factors; HIF-1-alpha, HIF-2-alpha |
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| Type: | n/a |
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| Mol. Mass.: | n/a |
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| Description: | ASSAY_ID of ChEMBL is 799337 |
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| Components: | This complex has 2 components. |
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| Component 1 |
| Name: | Hypoxia-inducible factor 1-alpha |
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| 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 |
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| Type: | Protein |
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| Mol. Mass.: | 92647.24 |
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| Organism: | Homo sapiens (Human) |
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| Description: | Q16665 |
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| Residue: | 826 |
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| Sequence: | MEGAGGANDKKKISSERRKEKSRDAARSRRSKESEVFYELAHQLPLPHNVSSHLDKASVM
RLTISYLRVRKLLDAGDLDIEDDMKAQMNCFYLKALDGFVMVLTDDGDMIYISDNVNKYM
GLTQFELTGHSVFDFTHPCDHEEMREMLTHRNGLVKKGKEQNTQRSFFLRMKCTLTSRGR
TMNIKSATWKVLHCTGHIHVYDTNSNQPQCGYKKPPMTCLVLICEPIPHPSNIEIPLDSK
TFLSRHSLDMKFSYCDERITELMGYEPEELLGRSIYEYYHALDSDHLTKTHHDMFTKGQV
TTGQYRMLAKRGGYVWVETQATVIYNTKNSQPQCIVCVNYVVSGIIQHDLIFSLQQTECV
LKPVESSDMKMTQLFTKVESEDTSSLFDKLKKEPDALTLLAPAAGDTIISLDFGSNDTET
DDQQLEEVPLYNDVMLPSPNEKLQNINLAMSPLPTAETPKPLRSSADPALNQEVALKLEP
NPESLELSFTMPQIQDQTPSPSDGSTRQSSPEPNSPSEYCFYVDSDMVNEFKLELVEKLF
AEDTEAKNPFSTQDTDLDLEMLAPYIPMDDDFQLRSFDQLSPLESSSASPESASPQSTVT
VFQQTQIQEPTANATTTTATTDELKTVTKDRMEDIKILIASPSPTHIHKETTSATSSPYR
DTQSRTASPNRAGKGVIEQTEKSHPRSPNVLSVALSQRTTVPEEELNPKILALQNAQRKR
KMEHDGSLFQAVGIGTLLQQPDDHAATTSLSWKRVKGCKSSEQNGMEQKTIILIPSDLAC
RLLGQSMDESGLPQLTSYDCEVNAPIQGSRNLLQGEELLRALDQVN
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| Component 2 |
| Name: | Endothelial PAS domain-containing protein 1 |
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| Synonyms: | BHLHE73 | EPAS1 | EPAS1_HUMAN | HIF2A | MOP2 | PASD2 | endothelial PAS domain-containing protein 1 |
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| Type: | PROTEIN |
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| Mol. Mass.: | 96453.58 |
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| Organism: | Homo sapiens (Human) |
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| Description: | ChEMBL_1506501 |
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| Residue: | 870 |
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| Sequence: | MTADKEKKRSSSERRKEKSRDAARCRRSKETEVFYELAHELPLPHSVSSHLDKASIMRLA
ISFLRTHKLLSSVCSENESEAEADQQMDNLYLKALEGFIAVVTQDGDMIFLSENISKFMG
LTQVELTGHSIFDFTHPCDHEEIRENLSLKNGSGFGKKSKDMSTERDFFMRMKCTVTNRG
RTVNLKSATWKVLHCTGQVKVYNNCPPHNSLCGYKEPLLSCLIIMCEPIQHPSHMDIPLD
SKTFLSRHSMDMKFTYCDDRITELIGYHPEELLGRSAYEFYHALDSENMTKSHQNLCTKG
QVVSGQYRMLAKHGGYVWLETQGTVIYNPRNLQPQCIMCVNYVLSEIEKNDVVFSMDQTE
SLFKPHLMAMNSIFDSSGKGAVSEKSNFLFTKLKEEPEELAQLAPTPGDAIISLDFGNQN
FEESSAYGKAILPPSQPWATELRSHSTQSEAGSLPAFTVPQAAAPGSTTPSATSSSSSCS
TPNSPEDYYTSLDNDLKIEVIEKLFAMDTEAKDQCSTQTDFNELDLETLAPYIPMDGEDF
QLSPICPEERLLAENPQSTPQHCFSAMTNIFQPLAPVAPHSPFLLDKFQQQLESKKTEPE
HRPMSSIFFDAGSKASLPPCCGQASTPLSSMGGRSNTQWPPDPPLHFGPTKWAVGDQRTE
FLGAAPLGPPVSPPHVSTFKTRSAKGFGARGPDVLSPAMVALSNKLKLKRQLEYEEQAFQ
DLSGGDPPGGSTSHLMWKRMKNLRGGSCPLMPDKPLSANVPNDKFTQNPMRGLGHPLRHL
PLPQPPSAISPGENSKSRFPPQCYATQYQDYSLSSAHKVSGMASRLLGPSFESYLLPELT
RYDCEVNVPVLGSSTLLQGGDLLRALDQAT
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| BDBM50105278 |
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| n/a |
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| Name | BDBM50105278 |
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| Synonyms: | CHEMBL3597778 |
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| Type | Small organic molecule |
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| Emp. Form. | C16H13BrIN5 |
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| Mol. Mass. | 482.116 |
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| SMILES | Brc1cccc(c1)[C@@H]1C[C@H](c2cccc(I)c2)n2nnnc2N1 |r| |
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| Structure | 
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