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Target
Endothelial PAS domain-containing protein 1
Ligand
BDBM373008
Substrate
n/a
Meas. Tech.
ChEMBL_1742673 (CHEMBL4158423)
EC50
158±n/a nM
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 Chem 61:9691-9721 (2018) [PubMed]  Article 
Target
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:
BDBM373008
Synonyms:
US10597366, Compound 163 | US9896418, Compound 163
Type:
Small organic molecule
Emp. Form.:
C17H12F3NO4S
Mol. Mass.:
383.342
SMILES:
CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2CC(F)(F)[C@@H](O)c12 |r|
Structure:
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