Target
Hexokinase-4
Ligand
BDBM50251450
Substrate
n/a
Meas. Tech.
ChEMBL_488153 (CHEMBL990114)
EC50
70±n/a nM
Citation
 Bertram, LSBlack, DBriner, PHChatfield, RCooke, AFyfe, MCMurray, PJNaud, FNawano, MProcter, MJRakipovski, GRasamison, CMReynet, CSchofield, KLShah, VKSpindler, FTaylor, ATurton, RWilliams, GMWong-Kai-In, PYasuda, K SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: discovery of PSN-GK1. J Med Chem 51:4340-5 (2008) [PubMed]  Article 
Target
Name:
Hexokinase-4
Synonyms:
GCK | Glucokinase (GCK) | Glucokinase (GK) | Glucokinase/Glucokinase regulatory protein | HK IV | HK4 | HXK4_HUMAN | Hexokinase-4 | Hexokinase-D
Type:
Enzyme
Mol. Mass.:
52175.81
Organism:
Homo sapiens (Human)
Description:
P35557
Residue:
465
Sequence:
MLDDRARMEAAKKEKVEQILAEFQLQEEDLKKVMRRMQKEMDRGLRLETHEEASVKMLPTYVRSTPEGSEVGDFLSLDLGGTNFRVMLVKVGEGEEGQWSVKTKHQMYSIPEDAMTGTAEMLFDYISECISDFLDKHQMKHKKLPLGFTFSFPVRHEDIDKGILLNWTKGFKASGAEGNNVVGLLRDAIKRRGDFEMDVVAMVNDTVATMISCYYEDHQCEVGMIVGTGCNACYMEEMQNVELVEGDEGRMCVNTEWGAFGDSGELDEFLLEYDRLVDESSANPGQQLYEKLIGGKYMGELVRLVLLRLVDENLLFHGEASEQLRTRGAFETRFVSQVESDTGDRKQIYNILSTLGLRPSTTDCDIVRRACESVSTRAAHMCSAGLAGVINRMRESRSEDVMRITVGVDGSVYKLHPSFKERFHASVRRLTPSCEITFIESEEGSGRGAALVSAVACKKACMLGQ
  
Inhibitor
Name:
BDBM50251450
Synonyms:
(R)-2-(4-(cyclopentylsulfonyl)phenyl)-N-(5-fluorothiazol-2-yl)-3-(tetrahydro-2H-pyran-4-yl)propanamide | CHEMBL480725
Type:
Small organic molecule
Emp. Form.:
C22H27FN2O4S2
Mol. Mass.:
466.589
SMILES:
Fc1cnc(NC(=O)[C@H](CC2CCOCC2)c2ccc(cc2)S(=O)(=O)C2CCCC2)s1 |r|
Structure:
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