aloisine A [Ligand Id: 5924] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL75680 (Aloisine A) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400] | ||||||||
| ChEMBL | Inhibition of Casein kinase II | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400] | ||||||||
| ChEMBL | Inhibition of CK1 | B | 4 | pIC50 | >=100000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| ChEMBL | Inhibition of CK2 | B | 4 | pIC50 | >=100000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| Cell division control protein 28 in Saccharomyces cerevisiae S288c (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5213] [UniProtKB: P00546] | ||||||||
| ChEMBL | Inhibition of hemagglutininin-tagged Saccharomyces cerevisiae MNY629 Cdc28/Clb2 | B | 5.6 | pIC50 | 2500 | nM | IC50 | Bioorg Med Chem (2009) 17: 5572-5582 [PMID:19596197] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067, P06493, P14635, Q8WWL7] | ||||||||
| GtoPdb | CDK1 in association with cyclin B | - | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2003) 46: 222-36 [PMID:12519061] |
| ChEMBL | Inhibitory activity against cyclin-dependent kinase 1-cyclin B in starfish | B | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| ChEMBL | Inhibition of CDK1/cyclinB | B | 6.82 | pIC50 | 150 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635] | ||||||||
| GtoPdb | CDK1 in association with cyclin B | - | 6.82 | pIC50 | 150 | nM | IC50 | J Med Chem (2003) 46: 222-36 [PMID:12519061] |
| ChEMBL | Inhibition of CDK1/cyclin B (unknown origin) | B | 6.82 | pIC50 | 150 | nM | IC50 | Eur J Med Chem (2019) 164: 615-639 [PMID:30639897] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396] | ||||||||
| GtoPdb | CDK2 in association with cyclin A | - | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2003) 46: 222-36 [PMID:12519061] |
| ChEMBL | Inhibition of Cyclin-dependent kinase 2-cyclin A | B | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020, P24864, P24941] | ||||||||
| ChEMBL | Inhibition of Cyclin-dependent kinase 2-cyclin E | B | 6.4 | pIC50 | 400 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| GtoPdb | CDK2 in association with cyclin A | - | 6.92 | pIC50 | 120 | nM | IC50 | J Med Chem (2003) 46: 222-36 [PMID:12519061] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] | ||||||||
| ChEMBL | Inhibition of Cyclin-dependent kinase 4-cyclin D1 | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078] | ||||||||
| ChEMBL | Inhibitory activity against recombinant mammalian cyclin-dependent kinase 5 (p35 NCK5a) expressed in Escherichia coli | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| ChEMBL | Inhibition of cyclin-dependent kinase 5/p25; range 0.16-0.2 | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2005) 48: 671-679 [PMID:15689152] |
| ChEMBL | Inhibition of GST-fused recombinant CDK5/p25 expressed in Escherichia coli after 30 mins by scintillation counting | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem (2009) 17: 5572-5582 [PMID:19596197] |
| ChEMBL | Inhibition of CDK5/p25 (unknown origin) | B | 6.7 | pIC50 | 200 | nM | IC50 | Eur J Med Chem (2019) 164: 615-639 [PMID:30639897] |
| ChEMBL | Inhibition of Cyclin-dependent kinase 5-p35nck5a | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| GtoPdb | CDK5 p35 | - | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2003) 46: 222-36 [PMID:12519061] |
| CFTR/Cystic fibrosis transmembrane conductance regulator in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4051] [GtoPdb: 707] [UniProtKB: P13569] | ||||||||
| ChEMBL | Activity at human wild type CFTR expressed in CHO cells assessed as forskolin stimulated iodide flux | B | 6.82 | pEC50 | 150 | nM | EC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| ChEMBL | Activity at human wild type CFTR expressed in Calu3 cells assessed as forskolin stimulated iodide flux | B | 6.85 | pEC50 | 140 | nM | EC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| ChEMBL | Activity at human wild type CFTR expressed in F508del-CF1 cells assessed as forskolin stimulated iodide flux | B | 6.95 | pEC50 | 111 | nM | EC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
| ChEMBL | Inhibition of GSK3alpha | B | 5.82 | pIC50 | 1500 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| GtoPdb | - | - | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2003) 46: 222-36 [PMID:12519061] |
| ChEMBL | Inhibition of Glycogen synthase kinase-3 alpha | B | 6.3 | pIC50 | 500 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Inhibition of Glycogen synthase kinase-3 beta | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| ChEMBL | Inhibition of GSK3-beta | B | 5.82 | pIC50 | 1500 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| ChEMBL | Inhibition of glycogen synthase kinase-3 beta, purified from porcine brain or expressed in and purified from insect Sf9 cells | B | 6.19 | pIC50 | 650 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| ChEMBL | Inhibition of GSK3beta (unknown origin) | B | 6.19 | pIC50 | 650 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 1532-1537 [PMID:24560539] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of Insulin receptor kinase | B | 4.22 | pIC50 | 60000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Inhibition of Mitogen-activated protein kinase 3 | B | 4.74 | pIC50 | 18000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Inhibition of Mitogen-activated protein kinase 1 | B | 4.66 | pIC50 | 22000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| protein kinase C alpha/Protein kinase C alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL299] [GtoPdb: 1482] [UniProtKB: P17252] | ||||||||
| ChEMBL | Inhibition of protein kinase C alpha | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] | ||||||||
| ChEMBL | Inhibition of Protein kinase C beta | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| ChEMBL | Inhibition of Protein kinase C beta | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| protein kinase C delta/Protein kinase C delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655] | ||||||||
| ChEMBL | Inhibition of protein kinase C delta | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| protein kinase C epsilon/Protein kinase C epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156] | ||||||||
| ChEMBL | Inhibition of protein kinase C epsilon | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| protein kinase C gamma/Protein kinase C gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129] | ||||||||
| ChEMBL | Inhibition of Protein kinase C gamma | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| protein kinase D1/Protein kinase C mu in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3863] [GtoPdb: 1489] [UniProtKB: Q15139] | ||||||||
| ChEMBL | Inhibition of Protein kinase C mu | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| protein kinase C zeta/Protein kinase C zeta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513] | ||||||||
| ChEMBL | Inhibition of protein kinase C zeta | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| 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 Protein kinase PIM-1 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
| Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] | ||||||||
| ChEMBL | Inhibition of RAF proto-oncogene serine/threonine-protein kinase (c-raf) | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2003) 46: 222-236 [PMID:12519061] |
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]
