Target
Endothelial PAS domain-containing protein 1
Ligand
BDBM373040
Substrate
n/a
Meas. Tech.
ChEMBL_1812988 (CHEMBL4312562)
IC50
9.0±n/a nM
Citation
 Xu, RWang, KRizzi, JPHuang, HGrina, JASchlachter, STWang, BWehn, PMYang, HDixon, DDCzerwinski, RMDu, XGed, ELHan, GTan, HWong, TXie, SJosey, JAWallace, 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:
BDBM373040
Synonyms:
US10597366, Compound 289 | US9896418, Compound 289
Type:
Small organic molecule
Emp. Form.:
C17H12F3NO4S
Mol. Mass.:
383.342
SMILES:
CS(=O)(=O)c1ccc(Oc2cc(F)cc(c2)C#N)c2[C@@H](F)[C@@H](F)[C@@H](O)c12 |r|
Structure:
Search PDB for entries with ligand similarity: