YS121 [Ligand Id: 5293] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL518038 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-LOX/Arachidonate 5-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL215] [GtoPdb: 1385] [UniProtKB: P09917] | ||||||||
| ChEMBL | Inhibition of human recombinant 5-LO expressed in Escherichia coli by cell-free assay | B | 5.19 | pIC50 | 6500 | nM | IC50 | J Med Chem (2008) 51: 8068-8076 [PMID:19053751] |
| ChEMBL | Inhibition of 5-lipoxygenase in human intact polymorphonuclear leukocytes assessed as suppression of A23187-induced product formation | B | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2008) 51: 5449-5453 [PMID:18710209] |
| ChEMBL | Inhibition of 5-LO in PMNL cells | B | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2008) 51: 8068-8076 [PMID:19053751] |
| ChEMBL | Inhibition of 5-lipoxygenase in human polymorphonuclear leukocytes | B | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2013) 56: 9031-9044 [PMID:24171493] |
| ChEMBL | Inhibition of 5-lipoxygenase in A23187-stimulated human polymorphonuclear leukocytes using arachidonic acid as substrate incubated 15 mins prior to substrate addition measured after 10 mins by HPLC analysis | B | 5.41 | pIC50 | 3900 | nM | IC50 | J Med Chem (2013) 56: 9031-9044 [PMID:24171493] |
| ChEMBL | Inhibition of 5-lipooxygenase (unknown origin) | B | 5.7 | pIC50 | 2000 | nM | IC50 | Medchemcomm (2015) 6: 2081-2123 |
| Cyclooxygenase-1 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2949] [UniProtKB: P05979] | ||||||||
| ChEMBL | Inhibition of ovine COX1 | B | 8 | pIC50 | >10 | nM | IC50 | J Med Chem (2008) 51: 8068-8076 [PMID:19053751] |
| COX-2 /Cyclooxygenase-2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL230] [GtoPdb: 1376] [UniProtKB: P35354] | ||||||||
| ChEMBL | Inhibition of human recombinant COX2 | B | 8 | pIC50 | >10 | nM | IC50 | J Med Chem (2008) 51: 8068-8076 [PMID:19053751] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
| ChEMBL | Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay | B | 6 | pIC50 | 1000 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3757-3763 [PMID:25037914] |
| ChEMBL | Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay | B | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4048-4052 [PMID:25022880] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231] | ||||||||
| ChEMBL | Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay | B | 5.44 | pIC50 | 3600 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3757-3763 [PMID:25037914] |
| ChEMBL | Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay | B | 5.44 | pEC50 | 3600 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 2469-2473 [PMID:20307981] |
| ChEMBL | Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay | B | 5.44 | pEC50 | 3600 | nM | EC50 | Bioorg Med Chem Lett (2014) 24: 4048-4052 [PMID:25022880] |
| mPGES1/Prostaglandin E synthase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5658] [GtoPdb: 1377] [UniProtKB: O14684] | ||||||||
| ChEMBL | Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation by cell-intact assay | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Med Chem (2008) 51: 8068-8076 [PMID:19053751] |
| ChEMBL | Inhibition of PGES1 in human A549 cell microsome assessed as PGE2 formation by cell-free assay | B | 5.41 | pIC50 | 3900 | nM | IC50 | J Med Chem (2008) 51: 8068-8076 [PMID:19053751] |
| ChEMBL | Reversible non-competitive inhibition of human microsomal PGES1 using PGH2 as substrate by Lineweaver-Burk plot analysis | B | 5.47 | pIC50 | 3400 | nM | IC50 | Medchemcomm (2015) 6: 2081-2123 |
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]
