NS-220 [Ligand Id: 2678] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL270960 (NS-220)
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
  • Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
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  • Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
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  • Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869]
ChEMBL Agonist activity at human PPARalpha ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay B 5.15 pEC50 7000 nM EC50 Bioorg Med Chem Lett (2008) 18: 5586-5590 [PMID:18805005]
GtoPdb - - 6.73 pEC50 - - - J Pharmacol Exp Ther (2004) 309: 970-7 [PMID:14982965]
ChEMBL Agonist activity at human PPARalpha transactivation expressed in human HePG2 cells F 7.28 pEC50 52 nM EC50 Bioorg Med Chem Lett (2008) 18: 6471-6475 [PMID:18976908]
ChEMBL Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay F 8 pEC50 10 nM EC50 Bioorg Med Chem (2008) 16: 981-994 [PMID:17964792]
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204]
ChEMBL Agonist activity at mouse PPARalpha expressed in CV1 cells by transactivation assay F 7.52 pEC50 30 nM EC50 Bioorg Med Chem (2008) 16: 981-994 [PMID:17964792]
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181]
ChEMBL Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay F 4 pEC50 >100000 nM EC50 Bioorg Med Chem (2008) 16: 981-994 [PMID:17964792]
Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL235] [GtoPdb: 595] [UniProtKB: P37231]
ChEMBL Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay F 5.02 pEC50 9600 nM EC50 Bioorg Med Chem (2008) 16: 981-994 [PMID:17964792]
ChEMBL Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with PPRE3-TK-luc assessed as induction of beta-galactosidase activity by transactivation assay B 5.15 pEC50 7000 nM EC50 Bioorg Med Chem Lett (2008) 18: 5586-5590 [PMID:18805005]
ChEMBL Agonist activity at human PPARgamma transactivation expressed in human HePG2 cells F 5.16 pEC50 6850 nM EC50 Bioorg Med Chem Lett (2008) 18: 6471-6475 [PMID:18976908]

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]