ChEMBL ligand: CHEMBL2177390 (GDC-0068, Ipatasertib, Rg-7440, RG7440, RG-7440)
Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 beta in Human [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976] 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/Serine/threonine-protein kinase AKT2 in Human [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751] There should be some charts here, you may need to enable JavaScript!
AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243] 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
Protein kinase G (PKG) 1/cGMP-dependent protein kinase 1 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4273] [GtoPdb: 1492] [UniProtKB: Q13976]
ChEMBL	Inhibition of PRKG1alpha	B	7.01	pIC50	98	nM	IC50	J Med Chem (2012) 55: 8110-8127 [PMID:22934575]
GtoPdb	-	-	7.16	pIC50	69	nM	IC50	J Med Chem (2012) 55: 8110-27 [PMID:22934575]
ChEMBL	Inhibition of PRKG1beta	B	7.16	pIC50	69	nM	IC50	J Med Chem (2012) 55: 8110-8127 [PMID:22934575]
AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749]
ChEMBL	Binding affinity to wild-type human partial length AKT1 expressed in bacterial expression system assessed as residual binding level by Kinomescan method	B	9.19	pKd	0.64	nM	Kd	J Med Chem (2021) 64: 18054-18081 [PMID:34855399]
ChEMBL	Inhibition of Akt1 in human LNCAP cells assessed as phosphorylation of PRAS40 at Thr246 after 1.5 hrs	B	6.8	pIC50	157	nM	IC50	J Med Chem (2012) 55: 8110-8127 [PMID:22934575]
ChEMBL	Competitive inhibition of wild-type full-length amino-terminal polyhistidine-tagged human Akt1 expressed in recombinant baculovirus system using fluorescence labeled substrate after 60 mins by fluorescence polarization assay in presence of ATP	B	8.3	pIC50	5	nM	IC50	J Med Chem (2012) 55: 8110-8127 [PMID:22934575]
ChEMBL	Inhibition of N-terminal GST-tagged human AKT1 (104 to 408 residues) expressed in baculovirus infected Sf21 cells incubated for 1 hr in presence of ATP by mobility shift assay	B	8.89	pIC50	1.3	nM	IC50	J Med Chem (2021) 64: 12163-12180 [PMID:34375113]
GtoPdb	-	-	9	pIC50	1	nM	IC50	J Med Chem (2012) 55: 8110-27 [PMID:22934575]
AKT serine/threonine kinase 2/Serine/threonine-protein kinase AKT2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2431] [GtoPdb: 1480] [UniProtKB: P31751]
ChEMBL	Binding affinity to wild-type human partial length AKT2 expressed in bacterial expression system assessed as residual binding level by Kinomescan method	B	7.46	pKd	35	nM	Kd	J Med Chem (2021) 64: 18054-18081 [PMID:34855399]
ChEMBL	Inhibition of full length human Akt2 S474D mutant using GRPRTSSFAEGKK as substrate incubated for 40 mins by scintillation counting method	B	7.49	pIC50	32	nM	IC50	Eur J Med Chem (2020) 189: 112076-112076 [PMID:32007668]
GtoPdb	-	-	7.74	pIC50	18	nM	IC50	J Med Chem (2012) 55: 8110-27 [PMID:22934575]
ChEMBL	Competitive inhibition of wild-type full-length amino-terminal polyhistidine-tagged human Akt2 expressed in recombinant baculovirus system using fluorescence labeled substrate after 60 mins by fluorescence polarization assay in presence of ATP	B	7.74	pIC50	18	nM	IC50	J Med Chem (2012) 55: 8110-8127 [PMID:22934575]
ChEMBL	Inhibition of N-terminal GST-tagged human AKT2 (120 to 481 residues) expressed in baculovirus infected Sf21 cells incubated for 1 hr in presence of ATP by mobility shift assay	B	8.42	pIC50	3.8	nM	IC50	J Med Chem (2021) 64: 12163-12180 [PMID:34375113]
AKT serine/threonine kinase 3/Serine/threonine-protein kinase AKT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4816] [GtoPdb: 2286] [UniProtKB: Q9Y243]
ChEMBL	Binding affinity to wild-type human partial length AKT3 expressed in bacterial expression system assessed as residual binding level by Kinomescan method	B	8.6	pKd	2.5	nM	Kd	J Med Chem (2021) 64: 18054-18081 [PMID:34855399]
ChEMBL	Inhibition of full length human Akt3 S472D mutant using GRPRTSSFAEGKK as substrate incubated for 40 mins by scintillation counting method	B	7.59	pIC50	26	nM	IC50	Eur J Med Chem (2020) 189: 112076-112076 [PMID:32007668]
ChEMBL	Competitive inhibition of wild-type full-length amino-terminal polyhistidine-tagged human Akt3 expressed in recombinant baculovirus system using fluorescence labeled Crosstide as substrate after 60 mins by fluorescence polarization assay in presence of ATP	B	8.1	pIC50	8	nM	IC50	J Med Chem (2012) 55: 8110-8127 [PMID:22934575]
GtoPdb	-	-	8.1	pIC50	8	nM	IC50	J Med Chem (2012) 55: 8110-27 [PMID:22934575]

ChEMBL data shown on this page come from version 32:

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]