Reaction Details |
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Target | Endothelial PAS domain-containing protein 1 |
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Ligand | BDBM282691 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1742626 (CHEMBL4158376) |
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IC50 | 350±n/a nM |
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Citation | Wehn, PM; Rizzi, JP; Dixon, DD; Grina, JA; Schlachter, ST; Wang, B; Xu, R; Yang, H; Du, X; Han, G; Wang, K; Cao, Z; Cheng, T; Czerwinski, RM; Goggin, BS; Huang, H; Halfmann, MM; Maddie, MA; Morton, EL; Olive, SR; Tan, H; Xie, S; Wong, T; Josey, JA; Wallace, EM Design and Activity of Specific Hypoxia-Inducible Factor-2? (HIF-2?) Inhibitors for the Treatment of Clear Cell Renal Cell Carcinoma: Discovery of Clinical Candidate ( S)-3-((2,2-Difluoro-1-hydroxy-7-(methylsulfonyl)-2,3-dihydro-1 H-inden-4-yl)oxy)-5-fluorobenzonitrile (PT2385). J Med Chem61:9691-9721 (2018) [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 |
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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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BDBM282691 |
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n/a |
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Name | BDBM282691 |
Synonyms: | 5-((5-Chloropyridin-3-yl)oxy)-4-(difluoromethyl)- 2,2-difluoro-3-hydroxy-2,3- dihydrobenzo[b]thiophene 1,1-dioxide | US9884843, Compound 35 |
Type | Small organic molecule |
Emp. Form. | C14H8ClF4NO4S |
Mol. Mass. | 397.729 |
SMILES | OC1c2c(ccc(Oc3cncc(Cl)c3)c2C(F)F)S(=O)(=O)C1(F)F |
Structure |
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