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TargetEndothelial PAS domain-containing protein 1/Hypoxia-inducible factor 1-alpha
LigandBDBM50008935
Substrate/Competitorn/a
Meas. Tech.ChEMBL_481746 (CHEMBL1002847)
EC50 71±n/a nM
Citation Mohammed, KAHossain, CFZhang, LBruick, RKZhou, YDNagle, DG Laurenditerpenol, a new diterpene from the tropical marine alga Laurenciaintricata that potently inhibits HIF-1 mediated hypoxic signaling in breast tumor cells. J Nat Prod67:2002-7 (2004) [PubMed]  Article
More Info.:Get all data from this article,  Assay Method
 
Endothelial PAS domain-containing protein 1/Hypoxia-inducible factor 1-alpha
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:
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
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:
MTADKEKKRSSSERRKEKSRDAARCRRSKETEVFYELAHELPLPHSVSSHLDKASIMRLA
ISFLRTHKLLSSVCSENESEAEADQQMDNLYLKALEGFIAVVTQDGDMIFLSENISKFMG
LTQVELTGHSIFDFTHPCDHEEIRENLSLKNGSGFGKKSKDMSTERDFFMRMKCTVTNRG
RTVNLKSATWKVLHCTGQVKVYNNCPPHNSLCGYKEPLLSCLIIMCEPIQHPSHMDIPLD
SKTFLSRHSMDMKFTYCDDRITELIGYHPEELLGRSAYEFYHALDSENMTKSHQNLCTKG
QVVSGQYRMLAKHGGYVWLETQGTVIYNPRNLQPQCIMCVNYVLSEIEKNDVVFSMDQTE
SLFKPHLMAMNSIFDSSGKGAVSEKSNFLFTKLKEEPEELAQLAPTPGDAIISLDFGNQN
FEESSAYGKAILPPSQPWATELRSHSTQSEAGSLPAFTVPQAAAPGSTTPSATSSSSSCS
TPNSPEDYYTSLDNDLKIEVIEKLFAMDTEAKDQCSTQTDFNELDLETLAPYIPMDGEDF
QLSPICPEERLLAENPQSTPQHCFSAMTNIFQPLAPVAPHSPFLLDKFQQQLESKKTEPE
HRPMSSIFFDAGSKASLPPCCGQASTPLSSMGGRSNTQWPPDPPLHFGPTKWAVGDQRTE
FLGAAPLGPPVSPPHVSTFKTRSAKGFGARGPDVLSPAMVALSNKLKLKRQLEYEEQAFQ
DLSGGDPPGGSTSHLMWKRMKNLRGGSCPLMPDKPLSANVPNDKFTQNPMRGLGHPLRHL
PLPQPPSAISPGENSKSRFPPQCYATQYQDYSLSSAHKVSGMASRLLGPSFESYLLPELT
RYDCEVNVPVLGSSTLLQGGDLLRALDQAT
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BDBM50008935
n/a
NameBDBM50008935
Synonyms:(20S)-10-Dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione | (4-Ethyl-4,9-dihydroxy-3,13-dioxo-3,4,12,13-tetrahydro-1H-2-oxa-6,12a-diaza-dibenzo[b,h]fluoren-10-ylmethyl)-dimethyl-ammonium | (S)-10-[(DIMETHYLAMINO)METHYL]-4-ETHYL-4,9-DIHYDROXY-1H-PYRANO[3'',4'':6,7]INOLIZINO[1,2-B]-QUINOLINE-3,14(4H,12H)-DIONE | (S)-10-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione | (S)-11-Dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione | 10-Dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione | 10-Dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione (Topotecan) | 10-Dimethylaminomethyl-4-ethyl-4,9-dihydroxy-1,12-dihydro-4H-2-oxa-6,12a-diaza-dibenzo[b,h]fluorene-3,13-dione(Topotecan) | 10-dimethylaminomethyl-4-ethyl-4,9-dihydroxy-(4S)-3,4,12,14-tetrahydro-1H-pyrano[3'',4'':6,7]indolizino[1,2-b]quinoline-3,14-dione | CHEMBL84 | Hycamtin | TOPOTECAN | TOPOTECAN HYDROCHLORIDE | cid_60700
TypeSmall organic molecule
Emp. Form.C23H23N3O5
Mol. Mass.421.4458
SMILESCC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4ccc(O)c(CN(C)C)c4cc3Cn1c2=O |r|
Structure
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