Ki Summary

Reaction Details

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Target

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

Ligand

BDBM125382

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:

BDBM125382

Synonyms:

US11547697, Compound 143 | US9682141, 143

Type:

Small organic molecule

Emp. Form.:

C21H21N5O3

Mol. Mass.:

391.4231

SMILES:

Nc1nc2cc(ccc2o1)-c1ccc2ncc(C(=O)NC3CC[C@H](O)CC3)n2c1 |r,wU:23.25,(5.65,-3.53,;4.88,-2.2,;3.35,-2.04,;3.03,-.53,;1.7,.24,;1.7,1.78,;3.03,2.55,;4.37,1.78,;4.37,.24,;5.51,-.79,;.36,2.55,;.36,4.09,;-.97,4.86,;-2.3,4.09,;-3.77,4.56,;-4.67,3.32,;-3.77,2.07,;-4.17,.59,;-5.65,.19,;-3.08,-.5,;-1.99,-1.59,;-2.39,-3.08,;-1.3,-4.17,;.19,-3.77,;1.28,-4.86,;.59,-2.28,;-.5,-1.19,;-2.3,2.55,;-.97,1.78,)|

Structure: