| Assay: | Inhibition of human PTEN (1 to 403 residues) expressed in Escherichia coli strain BL21(DE3) using DiFMUP as substrate preincubated for 10 mins followed by substrate addition and measured after 10 mins by fluorescence assay | Type: | IC50 | SMILES: | CC1=C(O)C(=O)C=C2C1=CC=C1[C@@]3(C)CC[C@@]4(C)CC[C@@](C)(C(=O)O)C[C@H]4[C@]3(C)CC[C@@]21C | Value: | =13300nM | Source: | Homo sapiens |
|
| Assay: | Inhibitory concentration of compound (dissolved in 0.3 % DMSO) against IGF1-mediated AKT phosphorylation at T308 position by PTEN-null in PC3 cells upon incubation at 37 degree C for 3 h by ELISA | Type: | IC50 | SMILES: | CCNC1=NC2=CC(=CC=C2N1)C1=CC=C2OCCN(CC2=C1)C1=C2C=CC(F)=CC2=NC=C1 | Value: | =2871nM | Source: | |
|
| Assay: | Inhibitory concentration of compound (dissolved in 0.3 % DMSO) against LPA-mediated AKT phosphorylation at T308 position by PTEN-null in PC3 cells upon incubation at 37 degree C for 3 h by ELISA | Type: | IC50 | SMILES: | CCNC1=NC2=CC(=CC=C2N1)C1=CC=C2OCCN(CC2=C1)C1=C2C=CC(F)=CC2=NC=C1 | Value: | =4539nM | Source: | |
|
| Assay: | Inhibitory concentration of compound (dissolved in 0.3 % DMSO) against IGF1-mediated AKT phosphorylation at T308 position by PTEN-null in PC3 cells upon incubation at 37 degree C for 3 h by ELISA | Type: | IC50 | SMILES: | COC1CCC2=C(C1)N=C(CN(C)C)N=C2N1CCOC2=CC=C(C=C2C1)C1=CN=C2NC(C)=NC2=C1 | Value: | =1685nM | Source: | |
|
| Assay: | Inhibitory concentration of compound (dissolved in 0.3 % DMSO) against LPA-mediated AKT phosphorylation at T308 position by PTEN-null in PC3 cells upon incubation at 37 degree C for 3 h by ELISA | Type: | IC50 | SMILES: | COC1CCC2=C(C1)N=C(CN(C)C)N=C2N1CCOC2=CC=C(C=C2C1)C1=CN=C2NC(C)=NC2=C1 | Value: | =1865nM | Source: | |
|
| Assay: | Inhibitory concentration of compound (dissolved in 0.3 % DMSO) against IGF1-mediated AKT phosphorylation at T308 position by PTEN-null in PC3 cells upon incubation at 37 degree C for 3 h by ELISA | Type: | IC50 | SMILES: | CCNC1=NC2=CC(=CN=C2N1)C1=CC=C2OCCN(CC2=C1)C1=C(C)C(NCC)=NC=N1 | Value: | =2120nM | Source: | |
|
| Assay: | Inhibitory concentration of compound (dissolved in 0.3 % DMSO) against LPA-mediated AKT phosphorylation at T308 position by PTEN-null in PC3 cells upon incubation at 37 degree C for 3 h by ELISA | Type: | IC50 | SMILES: | CCNC1=NC2=CC(=CN=C2N1)C1=CC=C2OCCN(CC2=C1)C1=C(C)C(NCC)=NC=N1 | Value: | =3805nM | Source: | |
|
| Assay: | Inhibitory concentration of compound (dissolved in 0.3 % DMSO) against IGF1-mediated AKT phosphorylation at T308 position by PTEN-null in PC3 cells upon incubation at 37 degree C for 3 h by ELISA | Type: | IC50 | SMILES: | CC(NC1=CC=CC=C1)C1=CC(C)=CN2C(=O)C=C(N=C12)N1CCOCC1 | Value: | =11226nM | Source: | |
|
| Assay: | Inhibitory concentration of compound (dissolved in 0.3 % DMSO) against LPA-mediated AKT phosphorylation at T308 position by PTEN-null in PC3 cells upon incubation at 37 degree C for 3 h by ELISA | Type: | IC50 | SMILES: | CC(NC1=CC=CC=C1)C1=CC(C)=CN2C(=O)C=C(N=C12)N1CCOCC1 | Value: | =16nM | Source: | |
|
| Assay: | Inhibitory concentration of compound (dissolved in 0.3 % DMSO) against IGF1-mediated AKT phosphorylation at T308 position by PTEN-null in PC3 cells upon incubation at 37 degree C for 3 h by ELISA | Type: | IC50 | SMILES: | CC(C)C1=C(C)N=C(CN(C)C)N=C1N1CCOC2=CC=C(C=C2C1)C1=CN=C2NC(C)=NC2=C1 | Value: | =231nM | Source: | |
|
| Assay: | Inhibitory concentration of compound (dissolved in 0.3 % DMSO) against LPA-mediated AKT phosphorylation at T308 position by PTEN-null in PC3 cells upon incubation at 37 degree C for 3 h by ELISA | Type: | IC50 | SMILES: | CC(C)C1=C(C)N=C(CN(C)C)N=C1N1CCOC2=CC=C(C=C2C1)C1=CN=C2NC(C)=NC2=C1 | Value: | =571nM | Source: | |
|
| Assay: | In vitro inhibitory concentration of compound against human PTEN upon incubation for 20 min at RT in 10 mM HEPES, pH 7.25 was determined by Malachite green assay | Type: | IC50 | SMILES: | FC1=CC=CC(F)=C1CNC(=O)C1=C(OCC2=C(Cl)C=C(Cl)C=C2)C=CS1 | Value: | >50uM | Source: | Human |
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| Assay: | Invitro inhibitory concentration of the compound against human PTEN using 250 uM PtdIns (3,4,5)P3 ( D-myo-phosphatidylinositol-3,4,5-trisphosphate) as substrate upon incubation in 10 mM HEPES, pH 7.25 at RT for 25 min by malachite green assay | Type: | IC50 | SMILES: | C[C@H](NC(=O)C1=C(OCC2=CC=C(Cl)C=C2)C=CS1)C1=CC=CC=C1 | Value: | >50uM | Source: | Human |
|
| Assay: | Inhibitory concentration against human cloned PTEN | Type: | IC50 | SMILES: | [H]OC1=[O][V-]23(=O)(OO2)(OO3)[N@H]4=C1C=CC=C4 | Value: | =31nM | Source: | Human |
|
| Assay: | Inhibitory concentration against human cloned PTEN | Type: | IC50 | SMILES: | [H]OC1=CC=C[N@@H]2=C1C(O[H])=[O][V-]2345(=O)OO3.O4O5 | Value: | =14nM | Source: | Human |
|
| Assay: | Inhibitory concentration against human cloned PTEN | Type: | IC50 | SMILES: | O=[V-]12345OO1.O2O3.C6=CC7=CC=C8C=CC=[N@H]4C8=C7[N@H]5=C6 | Value: | =38nM | Source: | Human |
|
| Assay: | Inhibitory activity of compound against mutant PTEN expressed in murine IC2 mast cells by PI3 kinase/Akt pathway | Type: | IC50 | SMILES: | [K+].[H]O[H].COO[V]1([O-])[N@@H]2=CC=CC3=C2C4=C(C=CC=[N@@H]14)C=C3 | Value: | =2.7uM | Source: | |
|
| Assay: | Inhibitory activity of compound against wild type PTEN expressed in murine IC2 mast cells by PI3 kinase/Akt pathway | Type: | IC50 | SMILES: | [K+].[H]O[H].COO[V]1([O-])[N@@H]2=CC=CC3=C2C4=C(C=CC=[N@@H]14)C=C3 | Value: | =2.1uM | Source: | |
|
| Assay: | Inhibitory activity of compound against mutant PTEN expressed in murine IC2 mast cells by PI3 kinase/Akt pathway | Type: | IC50 | SMILES: | [K+].[K+].[H]O[H].OO[V]1([O-])(OO1)[N]2=CC=CC=C2C([O-])=O | Value: | =3.6uM | Source: | |
|
| Assay: | Inhibitory activity of compound against wild type PTEN expressed in murine IC2 mast cells by PI3 kinase/Akt pathway | Type: | IC50 | SMILES: | [K+].[K+].[H]O[H].OO[V]1([O-])(OO1)[N]2=CC=CC=C2C([O-])=O | Value: | =9.2uM | Source: | |
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