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Target
Glucokinase regulatory protein
Ligand
BDBM50009121
Substrate
n/a
Meas. Tech.
ChEMBL_1338436 (CHEMBL3240702)
EC50
202±n/a nM
Citation
 Nishimura, N; Norman, MH; Liu, L; Yang, KC; Ashton, KS; Bartberger, MD; Chmait, S; Chen, J; Cupples, R; Fotsch, C; Helmering, J; Jordan, SR; Kunz, RK; Pennington, LD; Poon, SF; Siegmund, A; Sivits, G; Lloyd, DJ; Hale, C; St Jean, DJ Small molecule disruptors of the glucokinase-glucokinase regulatory protein interaction: 3. Structure-activity relationships within the aryl carbinol region of the N-arylsulfonamido-N'-arylpiperazine series. J Med Chem 57:3094-116 (2014) [PubMed]  Article 
Target
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:
MPSTKRYQHVIETPEPGEWELSGYEAAVPITEKSNPLTRNLDKADAEKIVQLLGQCDAEIFQEEGQIMPTYQRLYSESVLTTMLQVAGKVQEVLKEPDGGLVVLSGGGTSGRMAFLMSVSFNQLMKGLGQKPLYTYLIAGGDRSVVASRERTEDSALHGIEELKKVAAGKKRVVVIGISVGLSAPFVAGQMDYCMDNTAVFLPVLVGFNPVSMARNDPIEDWRSTFRQVAERMQKMQEKQEAFVLNPAIGPEGLSGSSRMKGGSATKILLETLLLAAHKTVDQGVVSSQRCLLEILRTFERAHQVTYSQSSKIATLTKQVGISLEKKGHVHLVGWQTLGIIAIMDGVECIHTFGADFRDIRGFLIGDHNDMFNQKDELSNQGPQFTFSQDDFLTSVLPSLTEIDTVVFIFTLDDNLAEVQALAERVREKSWNIQALVHSTVGQSLPAPLKKLFPSLISITWPLLFFDYEGSYVQKFQRELSTKWVLNTRFSGQSKARCIESLLQVIHFPQPLSNDVRAAPISCHVQVAHEKEKVIPTALLSLLLRCSITEAKERLAAASSVCEVVRSALSGPGQKRSIQAFGDPVVP
  
Inhibitor
Name:
BDBM50009121
Synonyms:
CHEMBL3237985
Type:
Small organic molecule
Emp. Form.:
C22H25F3N4O4S
Mol. Mass.:
498.519
SMILES:
COCC(O)(c1ccc(cc1)N1CCN(C[C@@H]1C#CC)S(=O)(=O)c1ccc(N)nc1)C(F)(F)F |r|
Structure:
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