Reaction Details |
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Target | Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform |
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Ligand | BDBM50598037 |
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Substrate/Competitor | n/a |
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Meas. Tech. | ChEMBL_2225494 (CHEMBL5139007) |
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IC50 | 230±n/a nM |
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Citation | Fairhurst, RA; Furet, P; Imbach-Weese, P; Stauffer, F; Rueeger, H; McCarthy, C; Ripoche, S; Oswald, S; Arnaud, B; Jary, A; Maira, M; Schnell, C; Guthy, DA; Wartmann, M; Kiffe, M; Desrayaud, S; Blasco, F; Widmer, T; Seiler, F; Gutmann, S; Knapp, M; Caravatti, G Identification of NVP-CLR457 as an Orally Bioavailable Non-CNS-Penetrant pan-Class IA Phosphoinositol-3-Kinase Inhibitor. J Med Chem65:8345-8379 (2022) [PubMed] Article |
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More Info.: | Get all data from this article, Assay Method |
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Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform |
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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: | MELENYKQPVVLREDNCRRRRRMKPRSAAASLSSMELIPIEFVLPTSQRKCKSPETALLH
VAGHGNVEQMKAQVWLRALETSVAADFYHRLGPHHFLLLYQKKGQWYEIYDKYQVVQTLD
CLRYWKATHRSPGQIHLVQRHPPSEESQAFQRQLTALIGYDVTDVSNVHDDELEFTRRGL
VTPRMAEVASRDPKLYAMHPWVTSKPLPEYLWKKIANNCIFIVIHRSTTSQTIKVSPDDT
PGAILQSFFTKMAKKKSLMDIPESQSEQDFVLRVCGRDEYLVGETPIKNFQWVRHCLKNG
EEIHVVLDTPPDPALDEVRKEEWPLVDDCTGVTGYHEQLTIHGKDHESVFTVSLWDCDRK
FRVKIRGIDIPVLPRNTDLTVFVEANIQHGQQVLCQRRTSPKPFTEEVLWNVWLEFSIKI
KDLPKGALLNLQIYCGKAPALSSKASAESPSSESKGKVQLLYYVNLLLIDHRFLLRRGEY
VLHMWQISGKGEDQGSFNADKLTSATNPDKENSMSISILLDNYCHPIALPKHQPTPDPEG
DRVRAEMPNQLRKQLEAIIATDPLNPLTAEDKELLWHFRYESLKHPKAYPKLFSSVKWGQ
QEIVAKTYQLLARREVWDQSALDVGLTMQLLDCNFSDENVRAIAVQKLESLEDDDVLHYL
LQLVQAVKFEPYHDSALARFLLKRGLRNKRIGHFLFWFLRSEIAQSRHYQQRFAVILEAY
LRGCGTAMLHDFTQQVQVIEMLQKVTLDIKSLSAEKYDVSSQVISQLKQKLENLQNSQLP
ESFRVPYDPGLKAGALAIEKCKVMASKKKPLWLEFKCADPTALSNETIGIIFKHGDDLRQ
DMLILQILRIMESIWETESLDLCLLPYGCISTGDKIGMIEIVKDATTIAKIQQSTVGNTG
AFKDEVLNHWLKEKSPTEEKFQAAVERFVYSCAGYCVATFVLGIGDRHNDNIMITETGNL
FHIDFGHILGNYKSFLGINKERVPFVLTPDFLFVMGTSGKKTSPHFQKFQDICVKAYLAL
RHHTNLLIILFSMMLMTGMPQLTSKEDIEYIRDALTVGKNEEDAKKYFLDQIEVCRDKGW
TVQFNWFLHLVLGIKQGEKHSA
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BDBM50598037 |
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n/a |
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Name | BDBM50598037 |
Synonyms: | CHEMBL5203121 |
Type | Small organic molecule |
Emp. Form. | C18H20F3N7O4 |
Mol. Mass. | 455.3911 |
SMILES | C[C@H]1OC(=O)N([C@H]1CO)c1nc(cc(n1)-c1cnc(N)nc1C(F)(F)F)N1CCOCC1 |r| |
Structure |
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