GF109203X [Ligand Id: 5193] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL7463 (GF-109203, GF-109203X) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Anthrax lethal factor in Bacillus anthracis (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4372] [UniProtKB: P15917] | ||||||||
| ChEMBL | Protection against Bacillus anthracis lethal toxin-mediated cytotoxicity in mouse RAW264.7 cells assessed as change in viability after 24 hrs by WST1 dye reduction assay | B | 5.82 | pIC50 | 1500 | nM | IC50 | Antimicrob Agents Chemother (2007) 51: 2403-2411 [PMID:17485504] |
| 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 | Inhibitory concentration was determined by measuring phosphorylation of H1 histone using active human Cell division cycle 2-cyclin B complex | B | 4.72 | pIC50 | 19000 | nM | IC50 | Bioorg Med Chem Lett (1998) 8: 1019-1022 [PMID:9871700] |
| ChEMBL | Inhibition of CDK1/cyclinB | B | 5.64 | pIC50 | 2300 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| 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 | Inhibitory activity against Cyclin E-cyclin-dependent kinase 2 by measuring phosphorylation of RbING substrate | B | 4.99 | pIC50 | 10180 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3841-3846 [PMID:14552792] |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] | ||||||||
| ChEMBL | Inhibitory activity against Cyclin D1-cyclin-dependent kinase 4 by measuring phosphorylation of RbING substrate | B | 6 | pIC50 | 990 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 3841-3846 [PMID:14552792] |
| 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 GSK3beta (unknown origin) expressed in Sf9 cells using GS1 as substrate and [gamma32]ATP after 30 min by scinitllation counting | B | 6.72 | pIC50 | 190.55 | nM | IC50 | Med Chem Res (2007) 16: 461-467 |
| ChEMBL | Inhibition of GSK3-beta | B | 6.72 | pIC50 | 190 | nM | IC50 | Trends Pharmacol Sci (2004) 25: 471-480 [PMID:15559249] |
| 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 Wistar rat GSK-3beta using RRAAEELDSRAGS(P)PQL as substrate after 15 mins in presence of [gamma-32P]-ATP by scintillation counting method | B | 6.44 | pIC50 | 360 | nM | IC50 | Bioorg Med Chem (2018) 26: 4209-4224 [PMID:30026041] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 6 | pIC50 | 1000 | nM | IC50 | Eur J Med Chem (2011) 46: 618-630 [PMID:21185626] |
| sirtuin 1/NAD-dependent deacetylase sirtuin 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4506] [GtoPdb: 2707] [UniProtKB: Q96EB6] | ||||||||
| ChEMBL | Inhibition of human SIRT1 | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| ChEMBL | Inhibition of human SIRT1 by fluorescent deacetylase assay | B | 4.3 | pIC50 | >50000 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| ChEMBL | Inhibition of human SIRT1 by radioactive deacetylase assay | B | 4.64 | pIC50 | 23000 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| sirtuin 2/NAD-dependent deacetylase sirtuin 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4462] [GtoPdb: 2708] [UniProtKB: Q8IXJ6] | ||||||||
| ChEMBL | Inhibition of human recombinant SIRT2 by radioactive deacetylase assay | B | 4.93 | pIC50 | 11700 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| ChEMBL | Inhibition of human recombinant SIRT2 | B | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| ChEMBL | Inhibition of human recombinant SIRT2 by fluorescent deacetylase assay | B | 5.14 | pIC50 | 7300 | nM | IC50 | J Med Chem (2006) 49: 7307-7316 [PMID:17149860] |
| 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 | 8 | pIC50 | 10 | nM | IC50 | Bioorg Med Chem Lett (1995) 5: 497-500 |
| ChEMBL | Inhibition of PKCalpha by SPA | B | 8.64 | pIC50 | 2.3 | nM | IC50 | J Med Chem (2009) 52: 6193-6196 [PMID:19827831] |
| protein kinase C alpha in Bovine [GtoPdb: 1482] | ||||||||
| GtoPdb | - | - | 7.7 | pIC50 | 20 | nM | IC50 | J Biol Chem (1991) 266: 15771-81 [PMID:1874734] |
| protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] | ||||||||
| ChEMBL | Inhibition of PKCbeta1 by SPA | B | 8.8 | pIC50 | 1.6 | nM | IC50 | J Med Chem (2009) 52: 6193-6196 [PMID:19827831] |
| protein kinase C beta in Bovine [GtoPdb: 1483] | ||||||||
| GtoPdb | - | - | 7.8 | pIC50 | 16 | nM | IC50 | J Biol Chem (1991) 266: 15771-81 [PMID:1874734] |
| protein kinase C delta/Protein kinase C delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655] | ||||||||
| ChEMBL | Inhibition of human PKCdelta | B | 7.49 | pIC50 | 32 | nM | IC50 | J Biol Chem (2007) 282: 33052-33063 [PMID:17875639] |
| ChEMBL | Inhibition of PKCdelta by SPA | B | 8.06 | pIC50 | 8.7 | nM | IC50 | J Med Chem (2009) 52: 6193-6196 [PMID:19827831] |
| protein kinase C epsilon/Protein kinase C epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3582] [GtoPdb: 1486] [UniProtKB: Q02156] | ||||||||
| ChEMBL | Inhibition of human PKCepsilon type M486A mutant | B | 7.92 | pIC50 | 12 | nM | IC50 | J Biol Chem (2007) 282: 33052-33063 [PMID:17875639] |
| ChEMBL | Inhibition of PKCepsilon by SPA | B | 8.18 | pIC50 | 6.6 | nM | IC50 | J Med Chem (2009) 52: 6193-6196 [PMID:19827831] |
| ChEMBL | Inhibition of human PKCepsilon | B | 8.22 | pIC50 | 6 | nM | IC50 | J Biol Chem (2007) 282: 33052-33063 [PMID:17875639] |
| protein kinase C eta/Protein kinase C eta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3616] [GtoPdb: 1487] [UniProtKB: P24723] | ||||||||
| ChEMBL | Inhibition of PKCeta by SPA | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2009) 52: 6193-6196 [PMID:19827831] |
| protein kinase C gamma/Protein kinase C gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2938] [GtoPdb: 1484] [UniProtKB: P05129] | ||||||||
| ChEMBL | Inhibition of human PKCgamma | B | 7.52 | pIC50 | 30 | nM | IC50 | J Biol Chem (2007) 282: 33052-33063 [PMID:17875639] |
| protein kinase C gamma in Bovine [GtoPdb: 1484] | ||||||||
| GtoPdb | - | - | 7.7 | pIC50 | 20 | nM | IC50 | J Biol Chem (1991) 266: 15771-81 [PMID:1874734] |
| protein kinase C iota/Protein kinase C iota in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2598] [GtoPdb: 1490] [UniProtKB: P41743] | ||||||||
| ChEMBL | Inhibition of human PKCiota | B | 5.46 | pIC50 | 3463 | nM | IC50 | J Biol Chem (2007) 282: 33052-33063 [PMID:17875639] |
| protein kinase C theta/Protein kinase C theta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3920] [GtoPdb: 1488] [UniProtKB: Q04759] | ||||||||
| ChEMBL | Inhibition of PKCtheta by SPA | B | 8.17 | pIC50 | 6.7 | nM | IC50 | J Med Chem (2009) 52: 6193-6196 [PMID:19827831] |
| protein kinase C zeta/Protein kinase C zeta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513] | ||||||||
| ChEMBL | Inhibition of PKCzeta | B | 5.24 | pIC50 | 5800 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
| Protein kinase Pfmrk in Plasmodium falciparum (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4090] [UniProtKB: P90584] | ||||||||
| ChEMBL | Inhibition of Plasmodium falciparum cyclin-dependent kinase | B | 4.62 | pIC50 | 24000 | nM | IC50 | J Med Chem (2004) 47: 5418-5426 [PMID:15481979] |
| lemur tyrosine kinase 3/Serine/threonine-protein kinase LMTK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523432] [GtoPdb: 2057] [UniProtKB: Q96Q04] | ||||||||
| ChEMBL | Inhibition of N-terminal GST tag LMTK3 kinase domain (133 to 415 amino acids) (unknown origin) expressed in insect cells incubated for 120 mins by radiometric fluorescent detection based CisBio KinEASE STK-S1 kit based assay | B | 9.88 | pIC50 | 0.13 | nM | IC50 | EP-2556169-B1. Methods for categorising cancer such as breast cancer (null) |
| 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 | Binding affinity to non phosphorylated PIM1 | B | 8 | pKd | 10 | nM | Kd | J Med Chem (2005) 48: 7604-7614 [PMID:16302800] |
| ChEMBL | Inhibitory activity against PIM1 | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2005) 48: 7604-7614 [PMID:16302800] |
| ChEMBL | Inhibition of human recombinant Pim1 by ATP depletion assay | B | 7.57 | pIC50 | 27 | nM | IC50 | J Med Chem (2009) 52: 74-86 [PMID:19072652] |
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]
