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Target
Transmembrane prolyl 4-hydroxylase
Ligand
BDBM105220
Substrate
n/a
Meas. Tech.
In Vitro Inhibition Assay
IC50
90±0.0 nM
Citation
 Jeske, M; Flamme, I; Stoll, F; Beck, H; Akbaba, M Substituted dihydropyrazolones and their use US Patent  US8580778 Publication Date 11/12/2013 
Target
Name:
Transmembrane prolyl 4-hydroxylase
Synonyms:
Hypoxia-inducible factor prolyl 4-hydroxylase | Hypoxia-inducible factor prolyl hydroxylase | Hypoxia-inducible factor prolyl hydroxylase 4 | Hypoxia-inducible factor prolyl hydroxylase 4 (HIF) | P4HTM | P4HTM_HUMAN | PH4 | Transmembrane prolyl 4-hydroxylase
Type:
Enzyme
Mol. Mass.:
56654.25
Organism:
Homo sapiens (Human)
Description:
Q9NXG6
Residue:
502
Sequence:
MAAAAVTGQRPETAAAEEASRPQWAPPDHCQAQAAAGLGDGEDAPVRPLCKPRGICSRAYFLVLMVFVHLYLGNVLALLLFVHYSNGDESSDPGPQHRAQGPGPEPTLGPLTRLEGIKVGHERKVQLVTDRDHFIRTLSLKPLLFEIPGFLTDEECRLIIHLAQMKGLQRSQILPTEEYEEAMSTMQVSQLDLFRLLDQNRDGHLQLREVLAQTRLGNGWWMTPESIQEMYAAIKADPDGDGVLSLQEFSNMDLRDFHKYMRSHKAESSELVRNSHHTWLYQGEGAHHIMRAIRQRVLRLTRLSPEIVELSEPLQVVRYGEGGHYHAHVDSGPVYPETICSHTKLVANESVPFETSCRYMTVLFYLNNVTGGGETVFPVADNRTYDEMSLIQDDVDLRDTRRHCDKGNLRVKPQQGTAVFWYNYLPDGQGWVGDVDDYSLHGGCLVTRGTKWIANNWINVDPSRARQALFQQEMARLAREGGTDSQPEWALDRAYRDARVEL
  
Inhibitor
Name:
BDBM105220
Synonyms:
US8580778, 20
Type:
Small organic molecule
Emp. Form.:
C14H10F2N8O
Mol. Mass.:
344.279
SMILES:
FC1(F)CN(C1)c1cc(ncn1)-n1[nH]cc(-n2cnc(c2)C#N)c1=O
Structure:
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