Target
Prolyl hydroxylase EGLN2
Ligand
BDBM50385825
Substrate
n/a
Meas. Tech.
ChEMBL_823544 (CHEMBL2045987)
IC50
0.4±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:
BDBM50385825
Synonyms:
CHEMBL2040897
Type:
Small organic molecule
Emp. Form.:
C29H29N7O3S
Mol. Mass.:
555.651
SMILES:
Cc1nc(C)c(s1)-c1ccc(cc1)N1C(=O)N(c2cc(=O)[nH]cn2)C2(CCN(Cc3ncccc3C)CC2)C1=O
Structure:
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