Reaction Details |
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Target | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform |
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Ligand | BDBM50274655 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_1714175 (CHEMBL4124224) |
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IC50 | 251±n/a nM |
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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 Chem61:5435-5441 (2018) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform |
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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: | MELENYEQPVVLREDNLRRRRRMKPRSAAGSLSSMELIPIEFVLPTSQRISKTPETALLH
VAGHGNVEQMKAQVWLRALETSVAAEFYHRLGPDQFLLLYQKKGQWYEIYDRYQVVQTLD
CLHYWKLMHKSPGQIHVVQRHVPSEETLAFQKQLTSLIGYDVTDISNVHDDELEFTRRRL
VTPRMAEVAGRDAKLYAMHPWVTSKPLPDYLSKKIANNCIFIVIHRGTTSQTIKVSADDT
PGTILQSFFTKMAKKKSLMNISESQSEQDFVLRVCGRDEYLVGETPLKNFQWVRQCLKNG
DEIHLVLDTPPDPALDEVRKEEWPLVDDCTGVTGYHEQLTIHGKDHESVFTVSLWDCDRK
FRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQVLCQRRTSPKPFAEEVLWNVWLEFGIKI
KDLPKGALLNLQIYCCKTPSLSSKASAETPGSESKGKAQLLYYVNLLLIDHRFLLRHGDY
VLHMWQISGKAEEQGSFNADKLTSATNPDKENSMSISILLDNYCHPIALPKHRPTPDPEG
DRVRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQ
QEIVAKTYQLLARREIWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLHYL
LQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRHYQQRFAVILEAY
LRGCGTAMLQDFTQQVHVIEMLQKVTIDIKSLSAEKYDVSSQVISQLKQKLESLQNSNLP
ESFRVPYDPGLKAGTLVIEKCKVMASKKKPLWLEFKCADPTVLSNETIGIIFKHGDDLRQ
DMLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAQIQQSTVGNTG
AFKDEVLNHWLKEKCPIEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMISETGNL
FHIDFGHILGNYKSFLGINKERVPFVLTPDFLFVMGSSGKKTSPHFQKFQDVCVRAYLAL
RHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKSEEDAKKYFLDQIEVCRDKGW
TVQFNWFLHLVLGIKQGEKHSA
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BDBM50274655 |
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n/a |
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Name | BDBM50274655 |
Synonyms: | CHEMBL4129457 |
Type | Small organic molecule |
Emp. Form. | C22H27N3O5S2 |
Mol. Mass. | 477.597 |
SMILES | C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(=O)(=O)CCCO)-c1sc(NC(C)=O)nc1C |r| |
Structure |
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