Reaction Details
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform
Ligand
BDBM421075
Substrate
n/a
Meas. Tech.
Scintillation Proximity Assay
IC50
<100±n/a nM
Citation
Buesking, AW; Sparks, RB; Combs, AP; Douty, B; Falahatpisheh, N; Shao, L; Shepard, S; Yue, EW; Shvartsbart, A; Burns, DM; Levy, D Substituted imidazo[2,1-f][1,2,4]triazines, substituted imidazo[1,2-a]pyridines and substituted imidazo[1,2-b]pyridazines as PI3K-gamma inhibitors US Patent US10479795 Publication Date 11/19/2019 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:
BDBM421075
Synonyms:
3-{8-amino-6-[1-(1-cyano-1-methylethyl)-1H-pyrazol-4- yl]imidazo[1,2-a]pyrazin-3-yl}-N-(trans-4-hydroxycyclohexyl)- 4-methylbenzenesulfonamide | 3-{8-amino-6-[1-(1-cyano-1-methylethyl)-1H-pyrazol-4-yl]imidazo[1,2-a]pyrazin-3-yl}-N-(4-hydroxycyclohexyl)-4-methylbenzenesulfonamide | US10479795, Example 78
Type:
Small organic molecule
Emp. Form.:
C26H30N8O3S
Mol. Mass.:
534.633
SMILES:
Cc1ccc(cc1-c1cnc2c(N)nc(cn12)-c1cnn(c1)C(C)(C)C#N)S(=O)(=O)NC1CCC(O)CC1 |(.6,4.3,;-.91,4.63,;-1.39,6.09,;-2.89,6.41,;-3.92,5.27,;-3.45,3.8,;-1.94,3.48,;-1.46,2.02,;-2.37,.77,;-1.46,-.48,;;1.33,-.77,;1.33,-2.31,;2.67,,;2.67,1.54,;1.33,2.31,;,1.54,;4,2.31,;4.16,3.84,;5.67,4.16,;6.44,2.83,;5.41,1.68,;7.97,2.67,;8.13,4.2,;7.81,1.14,;9.5,2.51,;11.03,2.35,;-5.43,5.59,;-5.11,7.09,;-5.75,4.08,;-6.94,5.91,;-7.41,7.37,;-8.92,7.69,;-9.39,9.16,;-8.36,10.3,;-8.84,11.76,;-6.86,9.98,;-6.38,8.51,)|
Structure:
