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ChEMBL ligand: CHEMBL23293 (FTS, Salirasib) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Isoprenylcysteine carboxyl methyltransferase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4699] [UniProtKB: O60725] | ||||||||
ChEMBL | Inhibition of ICMT in cell free system | B | 4.59 | pIC50 | 25500 | nM | IC50 | ACS Med Chem Lett (2012) 3: 15-19 [PMID:22754607] |
Isoprenylcysteine carboxyl methyltransferase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2298] [UniProtKB: Q9WVM4] | ||||||||
ChEMBL | Ability to inhibit prenylated protein methyltransferase (PPMTase) in cell free systems | B | 5.55 | pKi | 2800 | nM | Ki | J Med Chem (1995) 38: 1267-1272 [PMID:7731012] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antimalarial activity against synchronized ring stage Plasmodium falciparum 3D7 transfected with nano-luciferase assessed as parasite growth inhibition after 72 hrs by Nano-Glo luciferase assay | F | 4.69 | pIC50 | 20340 | nM | IC50 | Medchemcomm (2019) 10: 1599-1605 [PMID:31803400] |
ChEMBL | Antimalarial activity against synchronized ring stage Plasmodium falciparum 3D7 assessed as parasite growth inhibition measured after 24 to 96 hrs | F | 4.85 | pIC50 | 14000 | nM | IC50 | Medchemcomm (2019) 10: 1599-1605 [PMID:31803400] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | 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 | 4.9 | pIC50 | 12589.25 | 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 | 4.9 | pIC50 | 12589.25 | 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 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762] | ||||||||
ChEMBL | Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-3/acetoxymethyl ester dye based FLIPR analysis | B | 5.15 | pEC50 | 7000 | nM | EC50 | Eur J Med Chem (2019) 170: 141-156 [PMID:30878828] |
GtoPdb | FLIPR calcium-influx assay | - | 5.3 | pEC50 | - | - | - | Mol Pharmacol (2008) 73: 1225-34 [PMID:18171730] |
ChEMBL | Agonist activity at human TRPA1 channel expressed in CHO cells assessed as increase in intracellular calcium levels | F | 5.3 | pEC50 | 5000 | nM | EC50 | J Med Chem (2010) 53: 5085-5107 [PMID:20356305] |
ChEMBL | Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay | B | 6.08 | pEC50 | 831.76 | nM | EC50 | Eur J Med Chem (2019) 170: 141-156 [PMID:30878828] |
ChEMBL | Agonist activity at human TRPA1 expressed in HEK293 cells assessed as increase in calcium influx by Fluo-4-AM dye based fluorescence assay | B | 6.1 | pEC50 | 800 | nM | EC50 | Eur J Med Chem (2019) 170: 141-156 [PMID:30878828] |
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]