Ki Summary

Reaction Details

Report a problem with these data

Target

Phosphatidylinositol 3-kinase C2 domain-containing subunit gamma

Ligand

BDBM657152

Substrate

n/a

Meas. Tech.

PI3K-gamma Scintillation Proximity Assay

IC50

<100±n/a nM

Citation

Shepard, S; Combs, AP; Falahatpisheh, N; Shao, L Aminopyrazine diol compounds as PI3K-γ inhibitors US Patent US11926616 Publication Date 3/12/2024

More Info.:

Get all data from this article, Assay Method

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:

BDBM657152

Synonyms:

3-Amino-N-((1s,3R)-3-cyanocyclobutyl)-6- (2-(methyl-d3)-5-((S)-1,1,1-trifluoro-2,3- dihydroxypropan-2-yl)phenyl)pyrazine-2- carboxamide, trifluoroacetate salt (single enantiomer) | 3-Amino-N-((1s,3R)-3-cyanocyclobutyl)-6-(2-(methyl-d3)-5-((S)-1,1,1-trifluoro-2,3-dihydroxypropan-2-yl)phenyl)pyrazine-2-carboxamide | US11926616, Example 26

Type:

Small organic molecule

Emp. Form.:

C20H20F3N5O3

Mol. Mass.:

435.3997

SMILES:

Cc1ccc(cc1-c1cnc(N)c(n1)C(=O)NC1CC(C1)C#N)[C@](O)(CO)C(F)(F)F |wU:23.26,wD:23.25,(-8.95,-2.54,;-8.95,-1,;-10.28,-.23,;-10.28,1.31,;-8.95,2.08,;-7.61,1.31,;-7.61,-.23,;-6.28,-1,;-4.94,-.23,;-3.61,-1,;-3.61,-2.54,;-2.28,-3.31,;-4.94,-3.31,;-6.28,-2.54,;-4.94,-4.85,;-6.28,-5.62,;-3.61,-5.62,;-3.61,-7.16,;-2.52,-8.24,;-3.61,-9.33,;-4.7,-8.24,;-3.61,-10.87,;-3.61,-12.41,;-8.95,3.62,;-7.41,3.62,;-10.49,3.62,;-11.26,4.96,;-8.95,5.16,;-8.95,6.7,;-10.49,5.16,;-7.41,5.16,)|

Structure: