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Target
Endothelial PAS domain-containing protein 1
Ligand
BDBM373008
Substrate
n/a
Meas. Tech.
ChEMBL_1812989 (CHEMBL4312563)
EC50
27±n/a nM
Citation
 Xu, R; Wang, K; Rizzi, JP; Huang, H; Grina, JA; Schlachter, ST; Wang, B; Wehn, PM; Yang, H; Dixon, DD; Czerwinski, RM; Du, X; Ged, EL; Han, G; Tan, H; Wong, T; Xie, S; Josey, JA; Wallace, EM 3-[(1 J Med Chem 62:6876-6893 (2019) [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:
Search PDB for entries with ligand similarity: