Reaction Details Report a problem with these data
Target
Prolyl hydroxylase EGLN2
Ligand
BDBM50239914
Substrate
n/a
Meas. Tech.
ChEMBL_1667508 (CHEMBL4017304)
IC50
160±n/a nM
Citation
 Ahmed, S; Ayscough, A; Barker, GR; Canning, HE; Davenport, R; Downham, R; Harrison, D; Jenkins, K; Kinsella, N; Livermore, DG; Wright, S; Ivetac, AD; Skene, R; Wilkens, SJ; Webster, NA; Hendrick, AG 1,2,4-Triazolo-[1,5-a]pyridine HIF Prolylhydroxylase Domain-1 (PHD-1) Inhibitors With a Novel Monodentate Binding Interaction. J Med Chem 60:5663-5672 (2017) [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:
BDBM50239914
Synonyms:
CHEMBL4078461 | US10287286, Example 222
Type:
Small organic molecule
Emp. Form.:
C13H6F2N4
Mol. Mass.:
256.2103
SMILES:
Fc1cc(cc(F)c1-c1cccc2ncnn12)C#N |(8.14,-23.81,;9.49,-23.07,;9.52,-21.53,;10.88,-20.79,;12.2,-21.6,;12.16,-23.14,;13.47,-23.94,;10.8,-23.87,;10.76,-25.41,;12.07,-26.21,;12.03,-27.75,;10.68,-28.48,;9.37,-27.67,;7.9,-28.12,;7.03,-26.85,;7.96,-25.62,;9.41,-26.14,;10.92,-19.25,;10.96,-17.71,)|
Structure:
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