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Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform [144-1102]
Ligand
BDBM489244
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
1.10±n/a nM
Citation
 Perry, M; Tyrchan, C; Karabelas, K; Nikitidis, A; Mogemark, M; Petersen, J; Bold, P; Borjesson, U (S)-2-(1-cyclopropylethyl)-5-(4-methyl-2-((6-(2-oxopyrrolidin-1-yl)pyridin-2-yl)amino) thiazol-5-yl)-7-(methylsulfonyl)isoindolin-1-one as a phosphatidylinositol 3-kinase inhibitor US Patent  US10961236 Publication Date 3/30/2021
Target
Name:
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform [144-1102]
Synonyms:
PIK3CG | PK3CG_HUMAN | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (144-1102)
Type:
Enzyme Catalytic Domain
Mol. Mass.:
109626.89
Organism:
Homo sapiens (Human)
Description:
aa144-1102
Residue:
959
Sequence:
SEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGLVTPRMAEVASRDPKLYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDTPGAILQSFFTKMAKKKSLMDIPESQSEQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNGEEIHVVLDTPPDPALDEVRKEEWPLVDDCTGVTGYHEQLTIHGKDHESVFTVSLWDCDRKFRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQVLCQRRTSPKPFTEEVLWNVWLEFSIKIKDLPKGALLNLQIYCGKAPALSSKASAESPSSESKGKVQLLYYVNLLLIDHRFLLRRGEYVLHMWQISGKGEDQGSFNADKLTSATNPDKENSMSISILLDNYCHPIALPKHQPTPDPEGDRVRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQQEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLHYLLQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRHYQQRFAVILEAYLRGCGTAMLHDFTQQVQVIEMLQKVTLDIKSLSAEKYDVSSQVISQLKQKLENLQNSQLPESFRVPYDPGLKAGALAIEKCKVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQDMLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTVGNTGAFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMITETGNLFHIDFGHILGNYKSFLGINKERVPFVLTPDFLFVMGTSGKKTSPHFQKFQDICVKAYLALRHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKNEEDAKKYFLDQIEVCRDKGWTVQFNWFLHLVLGIKQGEKHSA
  
Inhibitor
Name:
BDBM489244
Synonyms:
N-{6-[(5-{2-[(1S)-1-Cyclopropylethyl]-7-(methylsulfamoyl)-1-oxo-2,3-dihydro-1H-isoindol-5-yl}-4-methyl-1,3-thiazol-2-yl)amino]pyridin-2-yl}-2-ethoxy-N-methylacetamide | US10961236, Example 17
Type:
Small organic molecule
Emp. Form.:
C28H34N6O5S2
Mol. Mass.:
598.737
SMILES:
CCOCC(=O)N(C)c1cccc(Nc2nc(C)c(s2)-c2cc3CN([C@@H](C)C4CC4)C(=O)c3c(c2)S(=O)(=O)NC)n1 |r|
Structure:
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