Gö 6976 [Ligand Id: 5973] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL302449 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Inhibition of Aurora-A (unknown origin) by kinase-glo luminescent assay | B | 6.93 | pIC50 | 118.2 | nM | IC50 | J Med Chem (2020) 63: 12403-12428 [PMID:32659083] |
| aurora kinase B/Aurora kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
| ChEMBL | Inhibition of Aurora-B (unknown origin) by kinase-glo luminescent assay | B | 7.11 | pIC50 | 77.7 | nM | IC50 | J Med Chem (2020) 63: 12403-12428 [PMID:32659083] |
| cAMP-dependent protein kinase catalytic subunit alpha in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2654] [UniProtKB: P00517] | ||||||||
| ChEMBL | In vitro for inhibitory activity against cAMP-dependent protein kinase from bovine heart (A-kinase) | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 1959-1964 |
| cGMP-dependent protein kinase 1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3183] [UniProtKB: P00516] | ||||||||
| ChEMBL | In vitro for inhibitory activity against cGMP-dependent protein kinase from bovine lung (G-kinase) | B | 5.21 | pIC50 | 6200 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 1959-1964 |
| ChEMBL | Tested for inhibition of cGMP-dependent protein kinase from bovine lung | B | 5.21 | pIC50 | 6200 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 55-60 |
| TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] | ||||||||
| ChEMBL | Inhibition of MPS1 in human taxol-arrested U2OS cells assessed as effect on histone H3 phosphorylation at ser10 residue incubated for 2 hrs by arrayscan analysis | B | 5.7 | pEC50 | 1990 | nM | EC50 | Cancer Res (2010) 70: 10255-10264 [PMID:21159646] |
| Myosin light chain kinase, smooth muscle in Chicken (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3062] [UniProtKB: P11799] | ||||||||
| ChEMBL | In vitro for inhibitory activity against myosin light-chain kinase from chicken gizzard (M-kinase) | B | 5.24 | pIC50 | 5800 | nM | IC50 | Bioorg Med Chem Lett (1993) 3: 1959-1964 |
| myosin light chain kinase/Myosin light chain kinase, smooth muscle in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2428] [GtoPdb: 1552] [UniProtKB: Q15746] | ||||||||
| ChEMBL | Tested for inhibition of Myosin light chain kinase from chicken gizzard | B | 5.24 | pIC50 | 5800 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 55-60 |
| sirtuin 2/NAD-dependent protein deacetylase sirtuin-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6] | ||||||||
| ChEMBL | Inhibition of human recombinant SIRT2 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| protein kinase C alpha/Protein kinase C alpha type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Inhibition of PKCalpha by TR-FRET assay | B | 8.43 | pIC50 | 3.7 | nM | IC50 | J Med Chem (2010) 53: 5400-5421 [PMID:20684591] |
| ChEMBL | Inhibition of PKCalpha | B | 8.64 | pIC50 | 2.3 | nM | IC50 | J Biol Chem (2007) 282: 15208-15216 [PMID:17395590] |
| GtoPdb | - | - | 8.64 | pIC50 | 2.3 | nM | IC50 | J Biol Chem (1993) 268: 9194-7 [PMID:8486620] |
| ChEMBL | Inhibition of PKCalpha | B | 8.7 | pIC50 | 2 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| protein kinase C beta/Protein kinase C beta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] | ||||||||
| ChEMBL | Inhibition of PKCbeta1 | B | 8.21 | pIC50 | 6.2 | nM | IC50 | J Biol Chem (2007) 282: 15208-15216 [PMID:17395590] |
| ChEMBL | Inhibition of PKCbeta | B | 8.7 | pIC50 | 2 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| protein kinase C delta/Protein kinase C delta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655] | ||||||||
| ChEMBL | Inhibition of PKCdelta by TR-FRET assay | B | 6.35 | pIC50 | 446 | nM | IC50 | J Med Chem (2010) 53: 5400-5421 [PMID:20684591] |
| protein kinase C gamma/Protein kinase C gamma type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129] | ||||||||
| ChEMBL | Inhibition of PKCgamma | B | 8.7 | pIC50 | 2 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| GtoPdb | Inhibitory activity against recombinant FLT3 in an in vitro kinase assay. | - | 9.15 | pIC50 | 0.7 | nM | IC50 | Biochem Pharmacol (2014) 90: 16-24 [PMID:24735609] |
| ChEMBL | Inhibition of FLT3 (unknown origin) | B | 9.15 | pIC50 | 0.7 | nM | IC50 | J Med Chem (2020) 63: 12403-12428 [PMID:32659083] |
| protein kinase D1/Serine/threonine-protein kinase D1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139] | ||||||||
| ChEMBL | Inhibition of PKD1 assessed as HDAC5 neuclear export | B | 7.21 | pIC50 | 62 | nM | IC50 | J Med Chem (2010) 53: 5400-5421 [PMID:20684591] |
| ChEMBL | Inhibition of PKD1 by TR-FRET assay | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2010) 53: 5400-5421 [PMID:20684591] |
| ChEMBL | Inhibition of PKD1 (unknown origin) | B | 7.7 | pIC50 | 20 | nM | IC50 | J Med Chem (2023) 66: 122-139 [PMID:36538005] |
| GtoPdb | - | - | 7.7 | pIC50 | 20 | nM | IC50 | FEBS Lett (1996) 392: 77-80 [PMID:8772178] |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Inhibition of full length PLK1 (unknown origin) | B | 5.1 | pIC50 | >8000 | nM | IC50 | Eur J Med Chem (2024) 265: 116115-116115 [PMID:38199166] |
| polo like kinase 2/Serine/threonine-protein kinase PLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5938] [GtoPdb: 2169] [UniProtKB: Q9NYY3] | ||||||||
| ChEMBL | Inhibition of full length PLK2 (unknown origin) | B | 4.72 | pIC50 | >19000 | nM | IC50 | Eur J Med Chem (2024) 265: 116115-116115 [PMID:38199166] |
| polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4] | ||||||||
| ChEMBL | Inhibition of full length PLK3 (unknown origin) | B | 4.8 | pIC50 | >16000 | nM | IC50 | Eur J Med Chem (2024) 265: 116115-116115 [PMID:38199166] |
| polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444] | ||||||||
| ChEMBL | Inhibition of human PLK4 | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2013) 56: 6069-6087 [PMID:23829549] |
| ChEMBL | Binding affinity to full length PLK4 (unknown origin) using (TPSDSLIYDDGLS) biotinylated peptide as substrate assessed as inhibition constant | B | 8.47 | pKi | 3.4 | nM | Ki | Eur J Med Chem (2024) 265: 116115-116115 [PMID:38199166] |
| BLK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Blk in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3343] [GtoPdb: 1940] [UniProtKB: P16277] | ||||||||
| ChEMBL | Tested for inhibition of general tyrosine-specific protein kinase activity from murine B cell lysate | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 55-60 |
| Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
| ChEMBL | Inhibition of JAK2 (unknown origin) in presence of ATP | B | 7.17 | pIC50 | 67.2 | nM | IC50 | J Med Chem (2020) 63: 12403-12428 [PMID:32659083] |
ChEMBL data shown on this page come from version 36:
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]
