salirasib [Ligand Id: 6281] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL23293 (FTS, Salirasib)
  • Isoprenylcysteine carboxyl methyltransferase in Human [ChEMBL: CHEMBL4699] [UniProtKB: O60725]
  • Isoprenylcysteine carboxyl methyltransferase in Rat [ChEMBL: CHEMBL2298] [UniProtKB: Q9WVM4]
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  • TRPA1/Transient receptor potential cation channel subfamily A member 1 in Human [ChEMBL: CHEMBL6007] [GtoPdb: 485] [UniProtKB: O75762]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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]