Target
Prolyl hydroxylase EGLN2
Ligand
BDBM50385796
Substrate
n/a
Meas. Tech.
ChEMBL_823544 (CHEMBL2045987)
IC50
0.2±n/a nM
Citation
 Vachal, PMiao, SPierce, JMGuiadeen, DColandrea, VJWyvratt, MJSalowe, SPSonatore, LMMilligan, JAHajdu, RGollapudi, AKeohane, CALingham, RBMandala, SMDeMartino, JATong, XWolff, MSteinhuebel, DKieczykowski, GRFleitz, FJChapman, KAthanasopoulos, JAdam, GAkyuz, CDJena, DKLusen, JWMeng, JStein, BDXia, LSherer, ECHale, JJ 1,3,8-Triazaspiro[4.5]decane-2,4-diones as efficacious pan-inhibitors of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) for the treatment of anemia. J Med Chem 55:2945-59 (2012) [PubMed]  Article 
Target
Name:
Prolyl hydroxylase EGLN2
Synonyms:
EGLN2 | EGLN2_HUMAN | EIT6 | Egl nine homolog 2 | Estrogen-induced tag 6 | HIF prolyl hydroxylase | HIF-PH1 | HIF-prolyl hydroxylase 1 | HPH-3 | Hypoxia-inducible factor prolyl hydroxylase | PHD1 | Prolyl hydroxylase domain-containing protein 1 | Prolyl hydroxylase domain-containing protein 1 (PHD1)
Type:
Protein
Mol. Mass.:
43657.01
Organism:
Homo sapiens (Human)
Description:
Q96KS0
Residue:
407
Sequence:
MDSPCQPQPLSQALPQLPGSSSEPLEPEPGRARMGVESYLPCPLLPSYHCPGVPSEASAGSGTPRATATSTTASPLRDGFGGQDGGELRPLQSEGAAALVTKGCQRLAAQGARPEAPKRKWAEDGGDAPSPSKRPWARQENQEAEREGGMSCSCSSGSGEASAGLMEEALPSAPERLALDYIVPCMRYYGICVKDSFLGAALGGRVLAEVEALKRGGRLRDGQLVSQRAIPPRSIRGDQIAWVEGHEPGCRSIGALMAHVDAVIRHCAGRLGSYVINGRTKAMVACYPGNGLGYVRHVDNPHGDGRCITCIYYLNQNWDVKVHGGLLQIFPEGRPVVANIEPLFDRLLIFWSDRRNPHEVKPAYATRYAITVWYFDAKERAAAKDKYQLASGQKGVQVPVSQPPTPT
  
Inhibitor
Name:
BDBM50385796
Synonyms:
CHEMBL2041182
Type:
Small organic molecule
Emp. Form.:
C33H32N6O4
Mol. Mass.:
576.645
SMILES:
Cc1cc(ncn1)N1C(=O)N(C(=O)C11CCN(Cc2ncccc2C)CC1)c1ccc(cc1)-c1ccc(cc1C)C(O)=O
Structure:
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