| Reaction Details |
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 | Report a problem with these data |
| Target | Endothelial PAS domain-containing protein 1 |
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| Ligand | BDBM282572 |
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| Substrate/Competitor | n/a |
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| Meas. Tech. | ChEMBL_1742628 (CHEMBL4158378) |
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| EC50 | 16±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 |
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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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| BDBM282572 |
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| n/a |
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| Name | BDBM282572 |
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| Synonyms: | (R)-3-((4-(difluoromethyl)-2,2-difluoro-3-hydroxy- 1,1-dioxido-2,3-dihydrobenzo[b]thiophen-5-yl)oxy)- 5-fluorobenzonitrile | US9884843, Compound 3 | US9884843, Compound 43 |
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| Type | Small organic molecule |
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| Emp. Form. | C16H8F5NO4S |
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| Mol. Mass. | 405.296 |
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| SMILES | O[C@@H]1c2c(ccc(Oc3cc(F)cc(c3)C#N)c2C(F)F)S(=O)(=O)C1(F)F |r| |
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| Structure | 
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