L-165041 [Ligand Id: 2691] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL153057 (L-165041) |
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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 for Human PPAR alpha receptor in transcriptional activation assay | F | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | Activity at PPARalpha by luciferase reporter gene transactivation assay in COS7 cells | F | 6.01 | pEC50 | 977 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4528-4532 [PMID:16797985] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
| ChEMBL | Binding affinity to PPARdelta (unknown origin) assessed as thermodynamic dissociation constant by SPR assay | B | 7.12 | pKd | 76.4 | nM | Kd | Eur J Med Chem (2017) 127: 379-397 [PMID:28076827] |
| GtoPdb | - | - | 8.2 | pKi | - | - | - |
J Med Chem (2000) 43: 527-50 [PMID:10691680]; J Biol Chem (1999) 274: 6718-25 [PMID:10037770] |
| ChEMBL | Agonist activity at GAL4 DNA-binding domain fused PPARdelta receptor (unknown origin) ligand binding domain expressed in UAS-bla HEK 293T cells assessed as beta-lactamase transcriptional activation by FRET-based GeneBLAzer assay | B | 7.9 | pIC50 | 12.6 | nM | IC50 | Eur J Med Chem (2018) 157: 791-804 [PMID:30144697] |
| ChEMBL | Transactivation of GAL4-fused PPARbeta (delta) ligand binding domain transfected in human HepG2 cells after 20 hrs by luciferase reporter gene assay | B | 6.19 | pEC50 | 650 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 6681-6687 [PMID:23031596] |
| ChEMBL | Transactivation of GAL4-fused PPARbeta LBD expressed in HepG2 cells after 20 hrs by luminescence assay | B | 6.19 | pEC50 | 640 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 2527-2533 [PMID:22381047] |
| ChEMBL | Agonist activity for Human PPAR delta receptor in transcriptional activation assay | F | 6.28 | pEC50 | 530 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | Transactivation of GAL4-tagged human PPARdelta LBD expressed in human HepG2 cells at 100 nM to 100 uM incubated for 20 to 22 hrs by luciferase reporter gene assay | B | 6.68 | pEC50 | 210 | nM | EC50 | ACS Med Chem Lett (2019) 10: 545-551 [PMID:30996794] |
| ChEMBL | Activity at PPARbeta/delta by luciferase reporter gene transactivation assay in COS7 cells | F | 6.9 | pEC50 | 125 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4528-4532 [PMID:16797985] |
| ChEMBL | Agonist activity at PPARbeta (unknown origin) incubated for 3 to 16 hrs by pathhunter nuclear hormone receptor assay | B | 7.21 | pEC50 | 61 | nM | EC50 | ACS Med Chem Lett (2019) 10: 1068-1073 [PMID:31312410] |
| ChEMBL | Transactivation of human PPARdelta expressed in African green monkey COS7 cells incubated overnight by dual-glo luciferase reporter gene assay | B | 7.41 | pEC50 | 39 | nM | EC50 | J Med Chem (2016) 59: 61-81 [PMID:26595749] |
| ChEMBL | Transactivation of GAL4-fused human PPARdelta ligand binding domain transfected in african green monkey COS7 cells by luciferase reporter gene assay | B | 7.41 | pEC50 | 39 | nM | EC50 | J Med Chem (2012) 55: 10771-10775 [PMID:23130964] |
| ChEMBL | Agonist activity at human GAL4-fused PPARdelta ligand binding domain expressed in COS-1 cells after 20 hrs by luciferase reporter gene transactivation assay | B | 7.68 | pEC50 | 21 | nM | EC50 | J Med Chem (2012) 55: 37-54 [PMID:22081932] |
| ChEMBL | Agonist activity at human GAL4-PPARdelta ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay | B | 7.68 | pEC50 | 21 | nM | EC50 | Eur J Med Chem (2015) 89: 817-825 [PMID:25462281] |
| ChEMBL | Transactivation of human PPARdelta expressed in HEK293 cells incubated for 18 hrs by dual luciferase reporter gene assay | B | 7.68 | pEC50 | 21 | nM | EC50 | Medchemcomm (2015) 6: 1513-1517 |
| ChEMBL | Transactivation of GAL4-fused human PPARdelta LBD expressed in human HepG2 cells after 20 hrs by luciferase reporter gene assay | B | 7.7 | pEC50 | 20 | nM | EC50 | Eur J Med Chem (2017) 127: 379-397 [PMID:28076827] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396] | ||||||||
| ChEMBL | Agonist activity for murine PPAR delta receptor in transcriptional activation assay | F | 5.42 | pEC50 | 3800 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| 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 for Human PPAR gamma receptor in transcriptional activation assay | F | 5.26 | pEC50 | 5500 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | Activity at PPARgamma by luciferase reporter gene transactivation assay in COS7 cells | F | 5.74 | pEC50 | 1824 | nM | EC50 | Bioorg Med Chem Lett (2006) 16: 4528-4532 [PMID:16797985] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238] | ||||||||
| ChEMBL | Agonist activity for murine PPAR gamma receptor in transcriptional activation assay | F | 5 | pEC50 | 10000 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
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]
