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 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]
