alsterpaullone [Ligand Id: 5925] 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: CHEMBL50894 (Alsterpaullone) |
|---|
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!
|
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!
|
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!
|
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!
|
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!
|
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!
|
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 |
|---|---|---|---|---|---|---|---|---|
| cyclin dependent kinase 2/CDK2/Cyclin A2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941] | ||||||||
| ChEMBL | Inhibition of CDK2/cyclin A (unknown origin) | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2022) 65: 893-921 [PMID:33539089] |
| 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] |
| ChEMBL | Inhibition of CDK1 (unknown origin) | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2022) 65: 935-954 [PMID:33970631] |
| 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 | Inhibition of CDK1/Cyclin B (unknown origin) in presence of gamma32P-ATP by scintillation counter analysis | B | 7.46 | pIC50 | 35 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| 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 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396] | ||||||||
| ChEMBL | Inhibition of CDK2/Cyclin A (unknown origin) | B | 7.82 | pIC50 | 15 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| 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 CDK2/Cyclin E (unknown origin) | B | 6.7 | pIC50 | 200 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| 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 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] | ||||||||
| ChEMBL | Inhibition of CDK4/Cyclin D1 (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| 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 CDK5/p25 (unknown origin) | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| 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] |
| ChEMBL | Inhibition of GSK3alpha (unknown origin) | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| 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 |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3669] [GtoPdb: 2030] [UniProtKB: P18266] | ||||||||
| ChEMBL | Inhibition of recombinant recombinant rat GSK3beta using GS-1 peptide as substrate in presence of [gamma-32P]ATP measured after 30 mins incubation by scintillation counting analysis | B | 8.4 | pIC50 | 4 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Inhibition of Insulin receptor tyrosine kinase (unknown origin) | B | 4 | pIC50 | >100000 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| mitogen-activated protein kinase 3/MAP kinase ERK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3385] [GtoPdb: 1494] [UniProtKB: P27361] | ||||||||
| ChEMBL | Inhibition of Erk1 (unknown origin) | B | 4.66 | pIC50 | 22000 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| ChEMBL | Inhibition of Erk1 (unknown origin) | B | 7.66 | pIC50 | 22 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Inhibition of Erk2 (unknown origin) | B | 5.35 | pIC50 | 4500 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| ChEMBL | Inhibition of Erk2 (unknown origin) | B | 8.35 | pIC50 | 4.5 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
| 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] |
| CoV Replicase polyprotein 1ab/CoV RNA-dependent RNA polymerase/CoV Non-structural protein 15/CoV Non-structural protein 13/Replicase polyprotein 1ab in Severe acute respiratory syndrome coronavirus 2 (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523582] [GtoPdb: 3125, 3139, 3206, 3261] [UniProtKB: P0DTD1] | ||||||||
| ChEMBL | Inhibition of SARS-CoV-2 M-protease | B | 5.82 | pIC50 | 1500 | nM | IC50 | J Med Chem (2022) 65: 955-982 [PMID:34081439] |
| 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 c-Raf (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2021) 220: 113445-113445 [PMID:33901899] |
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]
