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Target
Transmembrane prolyl 4-hydroxylase
Ligand
BDBM3543
Substrate
n/a
Meas. Tech.
In Vitro Inhibition Assay
pH
7.5±0
Temperature
298.15±0 K
IC50
4.8e+2±n/a nM
Citation
 Thede, K; Flamme, I; Oehme, F; Ergüden, J; Stoll, F; Schuhmacher, J; Wild, H; Kolkhof, P; Beck, H; Akbaba, M; Jeske, M Substituted dihydropyrazolones and use thereof as HIF-prolyl-4-hydroxylase inhibitors US Patent  US8524699 Publication Date 9/3/2013 
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:
BDBM3543
Synonyms:
US8524699, 16
Type:
n/a
Emp. Form.:
C16H15ClN6O2
Mol. Mass.:
358.782
SMILES:
Clc1ccc(cn1)-c1c[nH]n(-c2cc(ncn2)N2CCOCC2)c1=O
Structure:
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