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ChEMBL ligand: CHEMBL34241 (Rottlerin) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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chymotrypsinogen B1/Beta-chymotrypsin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4796] [GtoPdb: 3272] [UniProtKB: P17538] | ||||||||
ChEMBL | Inhibitory activity against Chymotrypsinogen from Thermus flavus | B | 4.6 | pIC50 | 25000 | nM | IC50 | J Med Chem (2003) 46: 1478-1483 [PMID:12672248] |
Beta-lactamase in Enterobacter cloacae (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2725] [UniProtKB: P05364] | ||||||||
ChEMBL | Inhibition of Enterobacter cloacae beta-lactamase incubated for 10 mins followed by nitrocefin substrate challenge and measured for 5 mins by spectrophotometric analysis | B | 4.02 | pIC50 | 96000 | nM | IC50 | ACS Med Chem Lett (2019) 10: 923-928 [PMID:31223449] |
Beta-lactamase AmpC in Escherichia coli (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2026] [UniProtKB: P00811] | ||||||||
ChEMBL | Inhibition of 30 nM AmpC beta lactamase | B | 4.12 | pIC50 | 76000 | nM | IC50 | J Med Chem (2006) 49: 7274-7277 [PMID:17149857] |
ChEMBL | Inhibition of 10 nM AmpC beta lactamase | B | 4.68 | pIC50 | 21000 | nM | IC50 | J Med Chem (2006) 49: 7274-7277 [PMID:17149857] |
ChEMBL | Inhibition of 1 nM AmpC beta lactamase | B | 5.74 | pIC50 | 1800 | nM | IC50 | J Med Chem (2006) 49: 7274-7277 [PMID:17149857] |
ChEMBL | Inhibitory activity against Amp C beta-Lactamase | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2003) 46: 4265-4272 [PMID:13678405] |
Malate dehydrogenase in Thermus thermophilus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4255] [UniProtKB: P10584] | ||||||||
ChEMBL | Inhibitory activity against malate dehydrogenase (MDH) from Thermus flavus | B | 6.15 | pIC50 | 700 | nM | IC50 | J Med Chem (2003) 46: 1478-1483 [PMID:12672248] |
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
ChEMBL | Inhibition of His-tagged human MAPKAPK2 expressed in Escherichia coli at 10 uM | B | 5.27 | pIC50 | 5400 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41] | ||||||||
ChEMBL | Inhibition of p38-regulated activated kinase (PRAK) | B | 5.72 | pIC50 | 1900 | nM | IC50 | J Med Chem (2003) 46: 1478-1483 [PMID:12672248] |
ChEMBL | Inhibition of His-tagged human PRAK expressed in Sf9 cells | B | 5.72 | pIC50 | 1900 | nM | IC50 | Biochem J (2000) 351: 95-105 [PMID:10998351] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 5.3 | pIC50 | 5011.87 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5.4 | pIC50 | 3981.07 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5.5 | pIC50 | 3162.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5.5 | pIC50 | 3162.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5.5 | pIC50 | 3162.28 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
protein kinase C delta/Protein kinase C delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2996] [GtoPdb: 1485] [UniProtKB: Q05655] | ||||||||
GtoPdb | - | - | 5.52 | pIC50 | 3020 | nM | IC50 | Biochem Biophys Res Commun (1994) 199: 93-8 [PMID:8123051] |
ChEMBL | Inhibition of Protein kinase C delta (PKCdelta) | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2003) 46: 1478-1483 [PMID:12672248] |
ChEMBL | Inhibition of PKCdelta (unknown origin) by IMAP kinase assay | B | 5.52 | pIC50 | 3000 | nM | IC50 | J Med Chem (2022) 65: 3134-3150 [PMID:35167283] |
RuvB-like 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3259467] [UniProtKB: Q9Y265] | ||||||||
ChEMBL | Inhibition of RUVBL1 (unknown origin) | B | 5 | pIC50 | 10000 | nM | IC50 | Bioorg Med Chem (2022) 62: 116726-116726 [PMID:35364523] |
eukaryotic elongation factor 2 kinase/Serine/threonine-protein kinase EEF2K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418] | ||||||||
ChEMBL | Inhibition of eEF2K (unknown origin) | B | 5.28 | pIC50 | 5300 | nM | IC50 | Eur J Med Chem (2020) 204: 112505-112505 [PMID:32717479] |
ubiquitin specific peptidase 1/Ubiquitin carboxyl-terminal hydrolase 1/WD repeat-containing protein 48 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3430885] [GtoPdb: 2428] [UniProtKB: O94782, Q8TAF3] | ||||||||
ChEMBL | Inhibition of human USP1/UAF1 complex using Ub-Rho as substrate by qHTS assay | B | 5.1 | pIC50 | 8000 | nM | IC50 | J Med Chem (2016) 59: 9321-9336 [PMID:27362876] |
Kv11.1 in Human [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
GtoPdb | - | - | 6.5 | pEC50 | - | - | - | J Pharmacol Exp Ther (2006) 319: 957-62 [PMID:16928897] |
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]