Ki Summary

Reaction Details

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Target

Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform

Ligand

BDBM295044

Substrate

n/a

Meas. Tech.

TR-FRET Adapta Assay for PI 3-Kinase Gamma (E), PI 3-Kinase Delta (F)

7.5±n/a

IC50

7.00±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

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:

BDBM295044

Synonyms:

US10112926, Example 5.2 | trans 3-(6-Amino-5- (5-methyloxazol-2- yl)pyridin-3-yl)-N-(4- hydroxy cyclohexyl)- 4-methylbenzene sulfonamide hydrochloride

Type:

Small organic molecule

Emp. Form.:

C22H26N4O4S

Mol. Mass.:

442.531

SMILES:

Cc1cnc(o1)-c1cc(cnc1N)-c1cc(ccc1C)S(=O)(=O)N[C@H]1CC[C@H](O)CC1 |r,wU:24.26,wD:27.30,(7.96,1.93,;6.42,1.93,;5.51,.68,;4.05,1.15,;4.05,2.69,;5.51,3.17,;2.71,3.47,;1.38,2.69,;.05,3.47,;.05,5,;1.38,5.78,;2.71,5,;4.05,5.78,;-1.29,2.69,;-1.29,1.15,;-2.62,.38,;-3.96,1.15,;-3.96,2.69,;-2.62,3.47,;-2.62,5,;-2.62,-1.15,;-4.16,-1.15,;-1.08,-1.15,;-2.62,-2.69,;-3.96,-3.47,;-3.96,-5,;-5.29,-5.78,;-6.62,-5,;-7.96,-5.78,;-6.62,-3.47,;-5.29,-2.69,)|

Structure: