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Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Ligand
BDBM511018
Substrate
n/a
Meas. Tech.
Scintillation Proximity Assay
IC50
<100±n/a nM
Citation
 Shepard, S; Ai, Y; Combs, AP; Falahatpisheh, N; Shao, L; Shvartsbart, A Heterocyclic derivatives as PI3K inhibitors US Patent  US11078204 Publication Date 8/3/2021 
Target
Name:
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Synonyms:
PI3-kinase p110 subunit gamma | PI3-kinase subunit p120-gamma | PI3Kgamma | PIK3CG | PK3CG_HUMAN | Phosphatidylinositol 4,5-biphosphate 3-kinase catalytic subunit gamma (PIK3CG) | Phosphatidylinositol 4,5-bisphosphate 3-kinase (PI3K) | Phosphatidylinositol 4,5-bisphosphate 3-kinase 110 kDa catalytic subunit gamma (PI3K gamma) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma (PI3Kgamma) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (PI3K gamma) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (PI3K) | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform (PI3Kgamma) | Phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma isoform | Phosphoinositide 3-Kinase (PI3K), gamma Chain A | Phosphoinositide 3-kinases gamma (PI3K gamma) | Phosphoinositide-3-kinase (PI3K gamma) | p120-PI3K
Type:
Enzyme Subunit
Mol. Mass.:
126470.30
Organism:
Homo sapiens (Human)
Description:
P48736
Residue:
1102
Sequence:
MELENYKQPVVLREDNCRRRRRMKPRSAAASLSSMELIPIEFVLPTSQRKCKSPETALLHVAGHGNVEQMKAQVWLRALETSVAADFYHRLGPHHFLLLYQKKGQWYEIYDKYQVVQTLDCLRYWKATHRSPGQIHLVQRHPPSEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGLVTPRMAEVASRDPKLYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDTPGAILQSFFTKMAKKKSLMDIPESQSEQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNGEEIHVVLDTPPDPALDEVRKEEWPLVDDCTGVTGYHEQLTIHGKDHESVFTVSLWDCDRKFRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQVLCQRRTSPKPFTEEVLWNVWLEFSIKIKDLPKGALLNLQIYCGKAPALSSKASAESPSSESKGKVQLLYYVNLLLIDHRFLLRRGEYVLHMWQISGKGEDQGSFNADKLTSATNPDKENSMSISILLDNYCHPIALPKHQPTPDPEGDRVRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQQEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLHYLLQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRHYQQRFAVILEAYLRGCGTAMLHDFTQQVQVIEMLQKVTLDIKSLSAEKYDVSSQVISQLKQKLENLQNSQLPESFRVPYDPGLKAGALAIEKCKVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQDMLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTVGNTGAFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMITETGNLFHIDFGHILGNYKSFLGINKERVPFVLTPDFLFVMGTSGKKTSPHFQKFQDICVKAYLALRHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKNEEDAKKYFLDQIEVCRDKGWTVQFNWFLHLVLGIKQGEKHSA
  
Inhibitor
Name:
BDBM511018
Synonyms:
(S)-8-Amino-3-(2-(1-cyclopropylethyl)- 1-oxoisoindolin-5-yl)-N-(3- hydroxycyclobutyl)imidazo[1,2- a]pyrazine-6-carboxamide, trifluoroacetate salt (mixture of two | US11078204, Ex. No. 31
Type:
Small organic molecule
Emp. Form.:
C24H26N6O3
Mol. Mass.:
446.5016
SMILES:
C[C@@H](C1CC1)N1Cc2cc(ccc2C1=O)-c1cnc2c(N)nc(cn12)C(=O)NC1CC(O)C1 |wU:1.0,(-3.48,1.51,;-2.71,2.84,;-3.48,4.18,;-4.82,4.95,;-3.48,5.72,;-1.17,2.84,;-.27,1.6,;1.2,2.07,;2.53,1.3,;3.86,2.07,;3.86,3.61,;2.53,4.38,;1.2,3.61,;-.27,4.09,;-.74,5.55,;5.2,1.3,;5.36,-.23,;6.87,-.55,;7.64,.78,;9.14,1.1,;10.17,-.04,;9.62,2.57,;8.59,3.71,;7.08,3.39,;6.6,1.93,;9.06,5.18,;8.03,6.32,;10.57,5.5,;11.05,6.96,;10.35,8.34,;11.72,9.03,;12.19,10.5,;12.42,7.66,)|
Structure:
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