LGB321 [Ligand Id: 9367] activity data from GtoPdb and ChEMBL
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: CHEMBL3105022 |
|---|
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 |
|---|---|---|---|---|---|---|---|---|
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Inhibition of PIM1 kinase (unknown origin) using NH2-AGAGRSRHSSYPAGT-OH as substrate by kinase-Glo assay | B | 9 | pKi | <1 | nM | Ki | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| ChEMBL | Inhibition of Pim1 (unknown origin) using BAD peptide preincubated for 15 mins followed by ATP addition measured after 60 to 100 mins by Kinase-Glo reagent based luminescence assay | B | 9 | pKi | <1 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 2328-2332 [PMID:26995528] |
| ChEMBL | Inhibition of PIM1 (unknown origin) using Bad peptide NH2-AGAGRSRHSSYPAGT-OH as substrate measured after 10 mins in presence of ATP by luciferase-luciferin based Kinase-Glo luminescence assay | B | 9 | pKi | <1 | nM | Ki | J Med Chem (2020) 63: 14885-14904 [PMID:33258605] |
| GtoPdb | Assayed at 400μM ATP | - | 12 | pKi | 0 | nM | Ki | Clin Cancer Res (2014) 20: 1834-45 [PMID:24474669] |
| ChEMBL | ATP Depletion Assay: The activity of PIM1, PIM2, and PIM3 is measured using a luciferase-luciferin based ATP detection reagent to quantify ATP depletion resulting from kinase-catalyzed phosphoryl transfer to a peptide substrate. | B | 9 | pIC50 | 1 | nM | IC50 | US-8592455-B2. Kinase inhibitors and methods of their use (2013) |
| Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
| ChEMBL | Inhibition of PIM2 kinase (unknown origin) using NH2-AGAGRSRHSSYPAGT-OH as substrate by kinase-Glo assay | B | 8.52 | pKi | <3 | nM | Ki | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| ChEMBL | Inhibition of PIM2 (unknown origin) using Bad peptide NH2-AGAGRSRHSSYPAGT-OH as substrate measured after 10 mins in presence of ATP by luciferase-luciferin based Kinase-Glo luminescence assay | B | 8.52 | pKi | <3 | nM | Ki | J Med Chem (2020) 63: 14885-14904 [PMID:33258605] |
| ChEMBL | Inhibition of Pim2 (unknown origin) using BAD peptide preincubated for 15 mins followed by ATP addition measured after 60 to 100 mins by Kinase-Glo reagent based luminescence assay | B | 9 | pKi | <1 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 2328-2332 [PMID:26995528] |
| GtoPdb | Assayed at 4μM ATP | - | 11.68 | pKi | 0 | nM | Ki | Clin Cancer Res (2014) 20: 1834-45 [PMID:24474669] |
| ChEMBL | ATP Depletion Assay: The activity of PIM1, PIM2, and PIM3 is measured using a luciferase-luciferin based ATP detection reagent to quantify ATP depletion resulting from kinase-catalyzed phosphoryl transfer to a peptide substrate. | B | 9 | pIC50 | 1 | nM | IC50 | US-8592455-B2. Kinase inhibitors and methods of their use (2013) |
| Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86] | ||||||||
| ChEMBL | Inhibition of PIM3 kinase (unknown origin) using NH2-AGAGRSRHSSYPAGT-OH as substrate by kinase-Glo assay | B | 8.52 | pKi | <3 | nM | Ki | J Med Chem (2015) 58: 8373-8386 [PMID:26505898] |
| ChEMBL | Inhibition of PIM3 (unknown origin) using Bad peptide NH2-AGAGRSRHSSYPAGT-OH as substrate measured after 10 mins in presence of ATP by luciferase-luciferin based Kinase-Glo luminescence assay | B | 8.52 | pKi | <3 | nM | Ki | J Med Chem (2020) 63: 14885-14904 [PMID:33258605] |
| ChEMBL | Inhibition of Pim3 (unknown origin) using BAD peptide preincubated for 15 mins followed by ATP addition measured after 60 to 100 mins by Kinase-Glo reagent based luminescence assay | B | 9 | pKi | <1 | nM | Ki | Bioorg Med Chem Lett (2016) 26: 2328-2332 [PMID:26995528] |
| GtoPdb | Assayed at 40μM ATP | - | 12.1 | pKi | 0 | nM | Ki | Clin Cancer Res (2014) 20: 1834-45 [PMID:24474669] |
| ChEMBL | ATP Depletion Assay: The activity of PIM1, PIM2, and PIM3 is measured using a luciferase-luciferin based ATP detection reagent to quantify ATP depletion resulting from kinase-catalyzed phosphoryl transfer to a peptide substrate. | B | 9 | pIC50 | 1 | nM | IC50 | US-8592455-B2. Kinase inhibitors and methods of their use (2013) |
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]
