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 | Agonist activity at PPARdelta (unknown origin) | B | 7.3 | pEC50 | 50 | nM | EC50 | Eur J Med Chem (2020) 197: 112311-112311 [PMID:32339855] |
| 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 | 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 | 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 | Agonist activity at yeast Gal4-fused human PPARdelta transfected in human HepG2 cells assessed as transactivation by measuring beta-galactosidase activity incubated for 20 hrs by luminometry | B | 7.68 | pEC50 | 21 | nM | EC50 | Eur J Med Chem (2022) 235: 114240-114240 [PMID:35325635] |
| 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] |
| ChEMBL | Agonist activity at human PPAR-delta expressed in CHO-K1 cells by PathHunter assay | B | 8.22 | pEC50 | 6 | nM | EC50 | J Med Chem (2022) 65: 9974-10000 [PMID:35797110] |
| 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 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]
