Reaction Details Report a problem with these data
Target
Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Ligand
BDBM295213
Substrate
n/a
Meas. Tech.
TR-FRET Adapta Assay for PI 3-Kinase Gamma (E), PI 3-Kinase Delta (F)
pH
7.5±n/a
IC50
13.0±n/a nM
Comments
extracted
Citation
 Bellenie, BR; Bloomfield, GC; Bruce, I; Culshaw, AJ; Hall, EC; Hollingworth, GJ; Neef, J; Spendiff, M; Watson, SJ Amino pyridine derivatives as phosphatidylinositol 3-kinase inhibitors US Patent  US10112926 Publication Date 10/30/2018 
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:
BDBM295213
Synonyms:
3-(6-Amino-5-(2-methylthiazol-4-yl)pyridin-3-yl)-N-((1r,4r)-4-hydroxycyclohexyl)-4-methylbenzenesulfonamide | US10112926, Example 92
Type:
Small organic molecule
Emp. Form.:
C22H26N4O3S2
Mol. Mass.:
458.597
SMILES:
Cc1nc(cs1)-c1cc(cnc1N)-c1cc(ccc1C)S(=O)(=O)N[C@H]1CC[C@H](O)CC1 |r,wU:27.30,wD:24.26,(6.06,2.56,;4.52,2.56,;3.61,3.81,;2.15,3.33,;2.15,1.79,;3.61,1.32,;.82,4.1,;-.52,3.33,;-1.85,4.1,;-1.85,5.64,;-.52,6.41,;.82,5.64,;2.15,6.41,;-3.19,3.33,;-3.19,1.79,;-4.52,1.02,;-5.85,1.79,;-5.85,3.33,;-4.52,4.1,;-4.52,5.64,;-4.52,-.52,;-2.98,-.52,;-6.06,-.52,;-4.52,-2.06,;-3.43,-3.15,;-3.83,-4.63,;-2.74,-5.72,;-1.25,-5.32,;-.16,-6.41,;-.85,-3.84,;-1.94,-2.75,)|
Structure:
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