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Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform [144-1102]
Ligand
BDBM489234
Substrate
n/a
Meas. Tech.
Enzymatic Activity Assay
IC50
0.900±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:
BDBM489234
Synonyms:
2-[(1S)-1-Cyclopropylethyl]-5-(4-methyl-2-{[6-(3-oxomorpholin-4-yl)pyridin-2-yl]amino}-1,3-thiazol-5-yl)-7-(methylsulfonyl)-2,3-dihydro-1H-isoindol-1-one | US10961236, Example 7
Type:
Small organic molecule
Emp. Form.:
C27H29N5O5S2
Mol. Mass.:
567.68
SMILES:
C[C@@H](C1CC1)N1Cc2cc(cc(c2C1=O)S(C)(=O)=O)-c1sc(Nc2cccc(n2)N2CCOCC2=O)nc1C |r|
Structure:
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