Reaction Details |
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Target | Hexokinase-4 |
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Ligand | BDBM50394689 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_858378 (CHEMBL2168593) |
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EC50 | >10000±n/a nM |
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Citation | Pfefferkorn, JA; Guzman-Perez, A; Litchfield, J; Aiello, R; Treadway, JL; Pettersen, J; Minich, ML; Filipski, KJ; Jones, CS; Tu, M; Aspnes, G; Risley, H; Bian, J; Stevens, BD; Bourassa, P; D'Aquila, T; Baker, L; Barucci, N; Robertson, AS; Bourbonais, F; Derksen, DR; Macdougall, M; Cabrera, O; Chen, J; Lapworth, AL; Landro, JA; Zavadoski, WJ; Atkinson, K; Haddish-Berhane, N; Tan, B; Yao, L; Kosa, RE; Varma, MV; Feng, B; Duignan, DB; El-Kattan, A; Murdande, S; Liu, S; Ammirati, M; Knafels, J; Dasilva-Jardine, P; Sweet, L; Liras, S; Rolph, TP Discovery of (S)-6-(3-cyclopentyl-2-(4-(trifluoromethyl)-1H-imidazol-1-yl)propanamido)nicotinic acid as a hepatoselective glucokinase activator clinical candidate for treating type 2 diabetes mellitus. J Med Chem55:1318-33 (2012) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Hexokinase-4 |
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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: | MLDDRARMEAAKKEKVEQILAEFQLQEEDLKKVMRRMQKEMDRGLRLETHEEASVKMLPT
YVRSTPEGSEVGDFLSLDLGGTNFRVMLVKVGEGEEGQWSVKTKHQMYSIPEDAMTGTAE
MLFDYISECISDFLDKHQMKHKKLPLGFTFSFPVRHEDIDKGILLNWTKGFKASGAEGNN
VVGLLRDAIKRRGDFEMDVVAMVNDTVATMISCYYEDHQCEVGMIVGTGCNACYMEEMQN
VELVEGDEGRMCVNTEWGAFGDSGELDEFLLEYDRLVDESSANPGQQLYEKLIGGKYMGE
LVRLVLLRLVDENLLFHGEASEQLRTRGAFETRFVSQVESDTGDRKQIYNILSTLGLRPS
TTDCDIVRRACESVSTRAAHMCSAGLAGVINRMRESRSEDVMRITVGVDGSVYKLHPSFK
ERFHASVRRLTPSCEITFIESEEGSGRGAALVSAVACKKACMLGQ
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BDBM50394689 |
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n/a |
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Name | BDBM50394689 |
Synonyms: | CHEMBL2165625 |
Type | Small organic molecule |
Emp. Form. | C17H20F3N4O4P |
Mol. Mass. | 432.3341 |
SMILES | OP(O)(=O)c1ccc(NC(=O)[C@H](CC2CCCC2)n2cnc(c2)C(F)(F)F)nc1 |r| |
Structure |
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