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

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ChEMBL ligand: CHEMBL23293 (FTS, Salirasib)
  • cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
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  • 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
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL Inhibition of 8-((4-chlorophenyl)amino)naphthalene-1-sulfonic acid binding to CDK2 (unknown origin) measured after 2 hrs by fluorescence based analysis B 5.51 pIC50 3100 nM IC50 J Med Chem (2023) 66: 1928-1940 [PMID:36701569]
ChEMBL Inhibition of 8-((4-chlorophenyl)amino)naphthalene-1-sulfonic acid binding to CDK2 (unknown origin) incubated for 2 hrs in presence of staurosporine by fluorescence based analysis B 5.51 pIC50 3100 nM IC50 J Med Chem (2023) 66: 1928-1940 [PMID:36701569]
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 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]