PHT-427 [Ligand Id: 8009] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL595583
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  • AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Mouse [ChEMBL: CHEMBL5859] [GtoPdb: 1479] [UniProtKB: P31750]
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  • AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
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  • AKT serine/threonine kinase 2 in Human [GtoPdb: 1480] [UniProtKB: P31751]
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  • 3-phosphoinositide dependent protein kinase 1 in Human [GtoPdb: 1519] [UniProtKB: O15530]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
GRB2-associated-binding protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523286] [UniProtKB: Q13480]
ChEMBL Binding affinity to recombinant human GAB1 PH domain expressed in Escherichia coli BL21 (DE3) by surface plasmon resonance assay B 5.88 pKd 1330 nM Kd US-20170311597-A1. Inhibitors of grb2-associated binding protein 1 (gab1) and methods of treating cancer using the same (2017)
AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5859] [GtoPdb: 1479] [UniProtKB: P31750]
ChEMBL Displacement of biotinylated phosphatidylinositol-3,4,5-phosphate from mouse AKT1 PH domain by surface plasmon resonance competitive binding assay B 5.62 pKi 2400 nM Ki Bioorg Med Chem (2011) 19: 2046-2054 [PMID:21353784]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL Inhibition of pleckstrin homology domain of AKT by surface plasmon resonance spectroscopy B 4.39 pKd 40800 nM Kd Bioorg Med Chem (2009) 17: 6983-6992 [PMID:19734051]
ChEMBL SPR Competitive Binding Assay: SPR interaction analyses were performed with a Biacore 2000, using Biacore 2000 Control Software v3.2 and BIAevaluation v4.1 analysis software (Biacore) as described in Mol Cancer Ther 7:2621 (2008). For the competitive binding assays and the Ki determination, PtdIns(3,4,5)phosphate-biotin labeled liposomes (Echelon Biosciences) and SA chips were used with increasing concentrations of the compound tested. B 4.39 pKd 40800 nM Kd US-9320734-B2. Small molecule inhibitors of the pleckstrin homology domain and methods for using same (2016)
ChEMBL SPR Competitive Binding Assay: SPR interaction analyses were performed with a Biacore 2000, using Biacore 2000 Control Software v3.2 and BIAevaluation v4.1 analysis software (Biacore) as described in Mol Cancer Ther 7:2621 (2008). For the competitive binding assays and the Ki determination, PtdIns(3,4,5)phosphate-biotin labeled liposomes (Echelon Biosciences) and SA chips were used with increasing concentrations of the compound tested. B 4.39 pKd 40800 nM Kd US-9320734-B2. Small molecule inhibitors of the pleckstrin homology domain and methods for using same (2016)
ChEMBL SPR Competitive Binding Assay: SPR interaction analyses were performed with a Biacore 2000, using Biacore 2000 Control Software v3.2 and BIAevaluation v4.1 analysis software (Biacore) as described in Mol Cancer Ther 7:2621 (2008). For the competitive binding assays and the Ki determination, PtdIns(3,4,5)phosphate-biotin labeled liposomes (Echelon Biosciences) and SA chips were used with increasing concentrations of the compound tested. B 4.87 pKd 13490 nM Kd US-9320734-B2. Small molecule inhibitors of the pleckstrin homology domain and methods for using same (2016)
ChEMBL SPR Competitive Binding Assay: SPR interaction analyses were performed with a Biacore 2000, using Biacore 2000 Control Software v3.2 and BIAevaluation v4.1 analysis software (Biacore) as described in Mol Cancer Ther 7:2621 (2008). For the competitive binding assays and the Ki determination, PtdIns(3,4,5)phosphate-biotin labeled liposomes (Echelon Biosciences) and SA chips were used with increasing concentrations of the compound tested. B 4.87 pKd 13490 nM Kd US-9320734-B2. Small molecule inhibitors of the pleckstrin homology domain and methods for using same (2016)
ChEMBL SPR Competitive Binding Assay: SPR interaction analyses were performed with a Biacore 2000, using Biacore 2000 Control Software v3.2 and BIAevaluation v4.1 analysis software (Biacore) as described in Mol Cancer Ther 7:2621 (2008). For the competitive binding assays and the Ki determination, PtdIns(3,4,5)phosphate-biotin labeled liposomes (Echelon Biosciences) and SA chips were used with increasing concentrations of the compound tested. B 5.62 pKi 2400 nM Ki US-9320734-B2. Small molecule inhibitors of the pleckstrin homology domain and methods for using same (2016)
ChEMBL SPR Competitive Binding Assay: SPR interaction analyses were performed with a Biacore 2000, using Biacore 2000 Control Software v3.2 and BIAevaluation v4.1 analysis software (Biacore) as described in Mol Cancer Ther 7:2621 (2008). For the competitive binding assays and the Ki determination, PtdIns(3,4,5)phosphate-biotin labeled liposomes (Echelon Biosciences) and SA chips were used with increasing concentrations of the compound tested. B 5.62 pKi 2400 nM Ki US-9320734-B2. Small molecule inhibitors of the pleckstrin homology domain and methods for using same (2016)
ChEMBL Binding affinity to AKT1 (unknown origin) by surface plasmon resonance assay B 5.62 pKi 2400 nM Ki US-20170311597-A1. Inhibitors of grb2-associated binding protein 1 (gab1) and methods of treating cancer using the same (2017)
ChEMBL Cellular Assay: Inhibition of AKT was measured by Western blots using specific antibodies against phospho-Ser473-AKT in HT-29 lung cancer cells. Inhibition of the phosphorylation of AKT and its downstream targets was measured by Western blotting using rabbit polyclonal antibodies to phospho-Ser473-AKT, phospho-Thr308-AKT, total-AKT, phospho-Ser9-GSK3β, phospho-Ser21-GSK3β, phospho-Ser241-PDK1 and phospho-Thr389p70S6-kinase (New England Biolabs/Cell Signaling Technology Inc.) using β-Actin as a loading control as described in Mol Cancer Ther 7:2621 (2008). Bands corresponding to phospho-Ser473-AKT and total AKT were quantified using Eagle Eye software (BioRad) and Kodak X-Omat™ Blue XB (NEN™, Life Science Products). Cell growth inhibition was determined using a microcytotoxicity assay and apoptosis was measured as described in Mol Cancer Ther 7:2621 (2008). B 5 pIC50 10000 nM IC50 US-9320734-B2. Small molecule inhibitors of the pleckstrin homology domain and methods for using same (2016)
ChEMBL Inhibition of Akt phosphorylation in human BxPC3 cells by Western blotting B 5.2 pIC50 6300 nM IC50 Bioorg Med Chem (2009) 17: 6983-6992 [PMID:19734051]
ChEMBL Cellular Assay: Inhibition of AKT was measured by Western blots using specific antibodies against phospho-Ser473-AKT in HT-29 lung cancer cells. Inhibition of the phosphorylation of AKT and its downstream targets was measured by Western blotting using rabbit polyclonal antibodies to phospho-Ser473-AKT, phospho-Thr308-AKT, total-AKT, phospho-Ser9-GSK3β, phospho-Ser21-GSK3β, phospho-Ser241-PDK1 and phospho-Thr389p70S6-kinase (New England Biolabs/Cell Signaling Technology Inc.) using β-Actin as a loading control as described in Mol Cancer Ther 7:2621 (2008). Bands corresponding to phospho-Ser473-AKT and total AKT were quantified using Eagle Eye software (BioRad) and Kodak X-Omat™ Blue XB (NEN™, Life Science Products). Cell growth inhibition was determined using a microcytotoxicity assay and apoptosis was measured as described in Mol Cancer Ther 7:2621 (2008). B 5.2 pIC50 6300 nM IC50 US-9320734-B2. Small molecule inhibitors of the pleckstrin homology domain and methods for using same (2016)
AKT serine/threonine kinase 2 in Human [GtoPdb: 1480] [UniProtKB: P31751]
GtoPdb Assay using purified recombinant pleckstrin homology domain of human Akt2 - 5.57 pKi 2670 nM Ki Mol Cancer Ther (2010) 9: 706-17 [PMID:20197390]
3-phosphoinositide dependent protein kinase 1 in Human [GtoPdb: 1519] [UniProtKB: O15530]
GtoPdb Assay using purified recombinant pleckstrin homology domain of human PDK1 - 5.28 pKi 5200 nM Ki Mol Cancer Ther (2010) 9: 706-17 [PMID:20197390]

ChEMBL data shown on this page come from version 34:

Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]