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Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Ligand
BDBM50274642
Substrate
n/a
Meas. Tech.
ChEMBL_1714175 (CHEMBL4124224)
IC50
32±n/a nM
Citation
 Pemberton, N; Mogemark, M; Arlbrandt, S; Bold, P; Cox, RJ; Gardelli, C; Holden, NS; Karabelas, K; Karlsson, J; Lever, S; Li, X; Lindmark, H; Norberg, M; Perry, MWD; Petersen, J; Rodrigo Blomqvist, S; Thomas, M; Tyrchan, C; Westin Eriksson, A; Zlatoidsky, P; ึster, L Discovery of Highly Isoform Selective Orally Bioavailable Phosphoinositide 3-Kinase (PI3K)-? Inhibitors. J Med Chem 61:5435-5441 (2018) [PubMed]  Article 
Target
Name:
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Synonyms:
PI3-kinase subunit gamma | PI3K-gamma | PI3Kgamma | PK3CG_MOUSE | Phosphatidylinositol 3-kinase p110γ (p110γ) | Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | Phosphoinositide-3-kinase catalytic gamma polypeptide | Pi3kg1 | Pik3cg | PtdIns-3-kinase subunit gamma | PtdIns-3-kinase subunit p110-gamma | Serine/threonine protein kinase PIK3CG | p110gamma | p120-PI3K
Type:
Enzyme
Mol. Mass.:
126411.77
Organism:
Mus musculus (Mouse)
Description:
Q9JHG7
Residue:
1102
Sequence:
MELENYEQPVVLREDNLRRRRRMKPRSAAGSLSSMELIPIEFVLPTSQRISKTPETALLHVAGHGNVEQMKAQVWLRALETSVAAEFYHRLGPDQFLLLYQKKGQWYEIYDRYQVVQTLDCLHYWKLMHKSPGQIHVVQRHVPSEETLAFQKQLTSLIGYDVTDISNVHDDELEFTRRRLVTPRMAEVAGRDAKLYAMHPWVTSKPLPDYLSKKIANNCIFIVIHRGTTSQTIKVSADDTPGTILQSFFTKMAKKKSLMNISESQSEQDFVLRVCGRDEYLVGETPLKNFQWVRQCLKNGDEIHLVLDTPPDPALDEVRKEEWPLVDDCTGVTGYHEQLTIHGKDHESVFTVSLWDCDRKFRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQVLCQRRTSPKPFAEEVLWNVWLEFGIKIKDLPKGALLNLQIYCCKTPSLSSKASAETPGSESKGKAQLLYYVNLLLIDHRFLLRHGDYVLHMWQISGKAEEQGSFNADKLTSATNPDKENSMSISILLDNYCHPIALPKHRPTPDPEGDRVRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQQEIVAKTYQLLARREIWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLHYLLQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRHYQQRFAVILEAYLRGCGTAMLQDFTQQVHVIEMLQKVTIDIKSLSAEKYDVSSQVISQLKQKLESLQNSNLPESFRVPYDPGLKAGTLVIEKCKVMASKKKPLWLEFKCADPTVLSNETIGIIFKHGDDLRQDMLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAQIQQSTVGNTGAFKDEVLNHWLKEKCPIEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMISETGNLFHIDFGHILGNYKSFLGINKERVPFVLTPDFLFVMGSSGKKTSPHFQKFQDVCVRAYLALRHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKSEEDAKKYFLDQIEVCRDKGWTVQFNWFLHLVLGIKQGEKHSA
  
Inhibitor
Name:
BDBM50274642
Synonyms:
CHEMBL4129877
Type:
Small organic molecule
Emp. Form.:
C18H18ClN3O2S
Mol. Mass.:
375.872
SMILES:
C[C@@H](C1CC1)N1Cc2cc(cc(Cl)c2C1=O)-c1cnc(NC(C)=O)s1 |r|
Structure:
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