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Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Ligand
BDBM50239117
Substrate
n/a
Meas. Tech.
ChEMBL_1665245 (CHEMBL4015041)
IC50
1500±n/a nM
Citation
 Barlaam, B; Cosulich, S; Degorce, S; Ellston, R; Fitzek, M; Green, S; Hancox, U; Lambert-van der Brempt, C; Lohmann, JJ; Maudet, M; Morgentin, R; Plé, P; Ward, L; Warin, N Discovery of a series of 8-(1-phenylpyrrolidin-2-yl)-6-carboxamide-2-morpholino-4H-chromen-4-one as PI3K?/? inhibitors for the treatment of PTEN-deficient tumours. Bioorg Med Chem Lett 27:1949-1954 (2017) [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:
BDBM50239117
Synonyms:
CHEMBL4060768
Type:
Small organic molecule
Emp. Form.:
C28H29F2N3O5
Mol. Mass.:
525.5438
SMILES:
Fc1cc(F)cc(c1)N1CCC[C@@H]1c1cc(cc2c1oc(cc2=O)N1CCOCC1)C(=O)N1CCOCC1 |r|
Structure:
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