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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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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]