alsterpaullone [Ligand Id: 5925] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL50894 (Alsterpaullone) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493] | ||||||||
| ChEMBL | In vitro inhibitory activity against cyclin-dependent kinase 1-cyclin B (Cyclin-Dependent Kinase) harvested from starfish oocytes. | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (1999) 42: 2909-2919 [PMID:10425100] |
| ChEMBL | Inhibition of CDK1 | B | 7.46 | pIC50 | 35 | nM | IC50 | AAPS J (2006) 8: E204-E221 [PMID:16584130] |
| GtoPdb | CDK1 in association with cyclin B | - | 7.46 | pIC50 | 35 | nM | IC50 | Eur J Biochem (2000) 267: 5983-94 [PMID:10998059] |
| 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] | ||||||||
| ChEMBL | Inhibition of CDK1/cyclin B expressed in M phase starfish oocyte | B | 7.46 | pIC50 | 35 | nM | IC50 | Eur J Med Chem (2010) 45: 335-342 [PMID:19906467] |
| ChEMBL | Inhibition of CDK1/cyclinB | B | 7.46 | pIC50 | 35 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| ChEMBL | Inhibitory activity against cyclin dependent kinase 1-cyclinB extracted from M phase starfish (Marthasterias glacialis) oocytes | B | 7.46 | pIC50 | 34.99 | nM | IC50 | J Med Chem (2004) 47: 22-36 [PMID:14695817] |
| GtoPdb | CDK1 in association with cyclin B | - | 7.46 | pIC50 | 35 | nM | IC50 | Eur J Biochem (2000) 267: 5983-94 [PMID:10998059] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] | ||||||||
| ChEMBL | Inhibition of CDK2 | B | 7.82 | pIC50 | 15 | nM | IC50 | AAPS J (2006) 8: E204-E221 [PMID:16584130] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL331] [GtoPdb: 1976] [UniProtKB: P11802] | ||||||||
| ChEMBL | Inhibition of CDK4 | B | 5 | pIC50 | >10000 | nM | IC50 | AAPS J (2006) 8: E204-E221 [PMID:16584130] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
| ChEMBL | Inhibition of CDK5 | B | 7.4 | pIC50 | 40 | nM | IC50 | AAPS J (2006) 8: E204-E221 [PMID:16584130] |
| 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 | Inhibition of CDK5/p25 (unknown origin) after 30 mins by SDS-PAGE analysis | B | 6.48 | pIC50 | 330 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 5150-5154 [PMID:23927974] |
| ChEMBL | Inhibition of recombinant CDK5/p25 expressed in Escherichia coli | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2008) 51: 2196-2207 [PMID:18345612] |
| ChEMBL | Inhibition of Cyclin-dependent kinase 5-p35nck5a | B | 7.4 | pIC50 | 39.99 | nM | IC50 | J Med Chem (2004) 47: 22-36 [PMID:14695817] |
| 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 | 8.4 | pIC50 | 4 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| 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 GSK3-beta | B | 7.7 | pIC50 | 20 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| ChEMBL | Inhibition of human GSK-3beta preincubated for 3 hrs followed by ATP and substrate addition measured by serial dilution assay | B | 8.1 | pIC50 | 7.9 | nM | IC50 | Bioorg Med Chem (2021) 40: 116179-116179 [PMID:33991821] |
| ChEMBL | Inhibition of human GSK-3beta incubated with substrate in presence of ATP measured by serial dilution assay | B | 8.19 | pIC50 | 6.5 | nM | IC50 | Bioorg Med Chem (2021) 40: 116179-116179 [PMID:33991821] |
| ChEMBL | Inhibition of human recombinant GSK3beta | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2011) 54: 8461-8470 [PMID:22050263] |
| ChEMBL | Inhibition of human GSK-3beta using YRRAAVPPSPSLSRHSSPHQS(p) EDEEE substrate peptide and [gamma-33P-ATP] incubated for 40 mins by scintillation counting method | B | 8.4 | pIC50 | 4 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 160-166 [PMID:29208522] |
| ChEMBL | Inhibition of GSK3beta (unknown origin) | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2021) 210: 112949-112949 [PMID:33097303] |
| ChEMBL | Inhibition of GSK3-beta expressed in insect Sf9 cells | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2010) 45: 335-342 [PMID:19906467] |
| ChEMBL | Inhibition of GSK3-beta | B | 8.4 | pIC50 | 4 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| ChEMBL | Inhibition of Glycogen synthase kinase-3 beta purified from insect sf9 cells | B | 8.4 | pIC50 | 4 | nM | IC50 | J Med Chem (2004) 47: 22-36 [PMID:14695817] |
| GtoPdb | - | - | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Biochem (2000) 267: 5983-94 [PMID:10998059] |
| ChEMBL | Inhibition of GSK3beta (unknown origin) expressed in Sf9 cells using GS1 as substrate and [gamma32]ATP after 30 min by scinitllation counting | B | 8.4 | pIC50 | 3.98 | nM | IC50 | Med Chem Res (2007) 16: 461-467 |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Inhibitory activity against Plasmodium falciparum W2 | F | 5.37 | pIC50 | 4300 | nM | IC50 | J Med Chem (2003) 46: 3877-3882 [PMID:12930149] |
| ChEMBL | Inhibitory activity against Plasmodium falciparum D6 | F | 5.37 | pIC50 | 4300 | nM | IC50 | J Med Chem (2003) 46: 3877-3882 [PMID:12930149] |
| ChEMBL | Antimalarial activity against chloroquine-resistant Plasmodium falciparum W2 assessed as inhibition of [3H]hypoxanthine incorporation after 24 hrs by microtiter plate scintillation counting | F | 5.37 | pIC50 | 4300 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 3863-3867 [PMID:20627564] |
| ChEMBL | Antimicrobial activity against Plasmodium falciparum | F | 5.4 | pIC50 | 4000 | nM | IC50 | Bioorg Med Chem (2010) 18: 2225-2231 [PMID:20185316] |
| Protein kinase Pfmrk in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4090] [UniProtKB: P90584] | ||||||||
| ChEMBL | Inhibitory activity against Plasmodium falciparum cyclin dependent protein kinase, Pfmrk | B | 4.29 | pIC50 | 51000 | nM | IC50 | J Med Chem (2003) 46: 3877-3882 [PMID:12930149] |
| ChEMBL | Inhibition of Plasmodium falciparum cyclin-dependent kinase | B | 4.29 | pIC50 | 51000 | nM | IC50 | J Med Chem (2004) 47: 5418-5426 [PMID:15481979] |
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]
