Ki Summary

Reaction Details

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Target

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

Ligand

BDBM141194

Substrate

n/a

Meas. Tech.

PI 3-Kinase HTRF Assay

Temperature

298.15±n/a K

IC50

<100±n/a nM

Comments

extracted

Citation

Jessen, K; Guo, X; Ren, P; Rommel, C; Liu, Y Combination of kinase inhibitors and uses thereof US Patent US9682141 Publication Date 6/20/2017

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:

BDBM141194

Synonyms:

US9682141, 538

Type:

Small organic molecule

Emp. Form.:

C22H20N6O3

Mol. Mass.:

416.4326

SMILES:

CCOC(=O)N1CCC(=CC1)c1cnc2ccc(nc2n1)-c1ccc2oc(N)nc2c1 |c:8,(-2.64,-1.93,;-2.64,-3.47,;-3.98,-4.23,;-5.31,-3.47,;-6.65,-4.23,;-5.31,-1.93,;-3.98,-1.15,;-3.98,.38,;-5.31,1.15,;-6.65,.38,;-6.65,-1.15,;-3.98,1.93,;-3.98,3.47,;-2.64,4.23,;-1.31,3.47,;.02,4.23,;1.36,3.47,;1.36,1.93,;.02,1.15,;-1.31,1.93,;-2.64,1.15,;2.69,1.15,;4.02,1.93,;5.36,1.15,;5.36,-.38,;6.5,-1.42,;5.88,-2.82,;6.65,-4.16,;4.34,-2.66,;4.02,-1.15,;2.69,-.38,)|

Structure: