Reaction Details |
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Target | Glucokinase regulatory protein |
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Ligand | BDBM50500194 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1545298 (CHEMBL3751191) |
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EC50 | >12500±n/a nM |
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Citation | Pennington, LD; Bartberger, MD; Croghan, MD; Andrews, KL; Ashton, KS; Bourbeau, MP; Chen, J; Chmait, S; Cupples, R; Fotsch, C; Helmering, J; Hong, FT; Hungate, RW; Jordan, SR; Kong, K; Liu, L; Michelsen, K; Moyer, C; Nishimura, N; Norman, MH; Reichelt, A; Siegmund, AC; Sivits, G; Tadesse, S; Tegley, CM; Van, G; Yang, KC; Yao, G; Zhang, J; Lloyd, DJ; Hale, C; St Jean, DJ Discovery and Structure-Guided Optimization of Diarylmethanesulfonamide Disrupters of Glucokinase-Glucokinase Regulatory Protein (GK-GKRP) Binding: Strategic Use of a N ? S (nN ? ?*S-X) Interaction for Conformational Constraint. J Med Chem58:9663-79 (2015) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Glucokinase regulatory protein |
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Name: | Glucokinase regulatory protein |
Synonyms: | GCKR_MOUSE | Gckr | Glucokinase regulator |
Type: | PROTEIN |
Mol. Mass.: | 64679.62 |
Organism: | Mus musculus |
Description: | ChEMBL_108288 |
Residue: | 587 |
Sequence: | MPSTKRYQHVIETPEPGEWELSGYEAAVPITEKSNPLTRNLDKADAEKIVQLLGQCDAEI
FQEEGQIMPTYQRLYSESVLTTMLQVAGKVQEVLKEPDGGLVVLSGGGTSGRMAFLMSVS
FNQLMKGLGQKPLYTYLIAGGDRSVVASRERTEDSALHGIEELKKVAAGKKRVVVIGISV
GLSAPFVAGQMDYCMDNTAVFLPVLVGFNPVSMARNDPIEDWRSTFRQVAERMQKMQEKQ
EAFVLNPAIGPEGLSGSSRMKGGSATKILLETLLLAAHKTVDQGVVSSQRCLLEILRTFE
RAHQVTYSQSSKIATLTKQVGISLEKKGHVHLVGWQTLGIIAIMDGVECIHTFGADFRDI
RGFLIGDHNDMFNQKDELSNQGPQFTFSQDDFLTSVLPSLTEIDTVVFIFTLDDNLAEVQ
ALAERVREKSWNIQALVHSTVGQSLPAPLKKLFPSLISITWPLLFFDYEGSYVQKFQREL
STKWVLNTRFSGQSKARCIESLLQVIHFPQPLSNDVRAAPISCHVQVAHEKEKVIPTALL
SLLLRCSITEAKERLAAASSVCEVVRSALSGPGQKRSIQAFGDPVVP
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BDBM50500194 |
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n/a |
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Name | BDBM50500194 |
Synonyms: | CHEMBL3746716 |
Type | Small organic molecule |
Emp. Form. | C24H21NO5S |
Mol. Mass. | 435.492 |
SMILES | O=S(=O)(N[C@@H](c1cc2ccccc2o1)c1ccccc1)c1ccc2OCCCOc2c1 |r| |
Structure |
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