Reaction Details
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Ligand
BDBM549585
Substrate
n/a
Meas. Tech.
PI3Kgamma Scintillation Proximity Assay
IC50
<100±n/a nM
Citation
Shvartsbart, A; Combs, AP; Falahatpisheh, N; Polam, P; Shao, L; Shepard, S 3-(5-amino-pyrazin-2-yl)-benzenesulfonamide derivatives and related compounds as PI3K-gamma kinase inhibitors US Patent US11306079 Publication Date 4/19/2022 More Info.:
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:
BDBM549585
Synonyms:
3-(5-Amino-6-(2-methylthiazol-5-yl)pyrazin-2- yl)-N-(4-cyanobicyclo[2.1.1]hexan-1-yl)-4- methylbenzenesulfonamide trifluoroacetate salt | US11306079, Example 2 | US11306079, Example 65
Type:
Small organic molecule
Emp. Form.:
C22H22N6O2S2
Mol. Mass.:
466.579
SMILES:
Cc1ncc(s1)-c1nc(cnc1N)-c1cc(ccc1C)S(=O)(=O)NC12CC(C1)(CC2)C#N |(-11.04,11.19,;-10.01,10.05,;-10.33,8.54,;-9,7.77,;-7.85,8.8,;-8.48,10.21,;-6.35,8.48,;-5.87,7.02,;-4.36,6.7,;-3.33,7.84,;-3.81,9.31,;-5.32,9.63,;-5.79,11.09,;-3.89,5.23,;-2.38,4.91,;-1.91,3.45,;-2.94,2.3,;-4.44,2.62,;-4.92,4.09,;-6.42,4.41,;-.4,3.13,;-.72,1.62,;-.08,4.63,;1.11,2.81,;1.58,1.34,;.68,.1,;1.58,-1.15,;1.27,.1,;3.05,-.67,;3.05,.87,;1.11,-2.61,;.63,-4.08,)|
Structure:
