LGB321 [Ligand Id: 9367] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3105022 |
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| 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 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
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]
