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

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ChEMBL ligand: CHEMBL595583
  • 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
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 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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]