Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL2177390 (GDC-0068, Ipatasertib, Rg-7440, RG7440, RG-7440) |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
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 | 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 | 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 | 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 31:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]