ChEMBL ligand: CHEMBL595583
GRB2-associated-binding protein 1 in Human [ChEMBL: CHEMBL4523286] [UniProtKB: Q13480] There should be some charts here, you may need to enable JavaScript!
AKT serine/threonine kinase 1/RAC-alpha serine/threonine-protein kinase in Mouse [ChEMBL: CHEMBL5859] [GtoPdb: 1479] [UniProtKB: P31750] There should be some charts here, you may need to enable JavaScript!
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] There should be some charts here, you may need to enable JavaScript!
AKT serine/threonine kinase 2 in Human [GtoPdb: 1480] [UniProtKB: P31751] There should be some charts here, you may need to enable JavaScript!
3-phosphoinositide dependent protein kinase 1 in Human [GtoPdb: 1519] [UniProtKB: O15530] There should be some charts here, you may need to enable JavaScript!

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 (null)
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 (null)
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 33:

Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]