GF109203X [Ligand Id: 5193] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL7463 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| protein kinase, cAMP-dependent, catalytic, alpha subunit/cAMP-dependent protein kinase catalytic subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4101] [GtoPdb: 1476] [UniProtKB: P17612] | ||||||||
| ChEMBL | Inhibition of human PKAC-alpha | B | 8.3 | pIC50 | 5 | nM | IC50 | Eur J Med Chem (2022) 243: 114668-114668 [PMID:36055000] |
| 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] |
| epidermal growth factor receptor/Epidermal growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Inhibition of EGFR in human A-431 cells in presence of ATP | B | 4 | pIC50 | >100000 | nM | IC50 | J Biol Chem (1991) 266: 15771-15781 [PMID:1874734] |
| 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] |
| 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] |
| sirtuin 1/NAD-dependent protein 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 protein 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 type 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 type in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2213] [UniProtKB: P04409] | ||||||||
| ChEMBL | Inhibition of bovine PKCalpha expressed in baculovirus infected Sf9 insect cells in presence of [p32-gamma]-ATP measured after 10 mins by scintillation counter analysis | B | 7.7 | pIC50 | 20 | nM | IC50 | J Biol Chem (1991) 266: 15771-15781 [PMID:1874734] |
| protein kinase C beta/Protein kinase C beta type in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] | ||||||||
| ChEMBL | Inhibition of human PKCbeta1 expressed in baculovirus infected Sf9 insect cells in presence of [p32-gamma]-ATP measured after 10 mins by scintillation counter analysis | B | 7.77 | pIC50 | 17 | nM | IC50 | J Biol Chem (1991) 266: 15771-15781 [PMID:1874734] |
| ChEMBL | Inhibition of human PKCbeta2 expressed in baculovirus infected Sf9 insect cells in presence of [p32-gamma]-ATP measured after 10 mins by scintillation counter analysis | B | 7.8 | pIC50 | 16 | nM | IC50 | J Biol Chem (1991) 266: 15771-15781 [PMID:1874734] |
| 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 type 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 type 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 type 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 type 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 type 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 type 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 type 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] |
| ribosomal protein S6 kinase A1/Ribosomal protein S6 kinase alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2553] [GtoPdb: 1527] [UniProtKB: Q15418] | ||||||||
| ChEMBL | Inhibition of RSK1 (unknown origin) | B | 6.21 | pIC50 | 610 | nM | IC50 | Eur J Med Chem (2023) 251: 115229-115229 [PMID:36898330] |
| 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 (2018) |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 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] |
| Kv11.1/Voltage-gated inwardly rectifying potassium channel KCNH2 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] |
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]
