GW0742X [Ligand Id: 2686] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL38508 (GW0742) |
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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 transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay | B | 5.6 | pEC50 | 2500 | nM | EC50 | J Med Chem (2021) 64: 6996-7032 [PMID:33988379] |
| ChEMBL | Maximum transcriptional activation of human PPAR alpha receptor | B | 5.96 | pEC50 | 1100 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| ChEMBL | Displacement of pan-PPAR fluormone from PPARalpha LBD by TR-FRET based LanthaScreen assay | B | 6.04 | pEC50 | 920 | nM | EC50 | J Med Chem (2012) 55: 4978-4989 [PMID:22582973] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204] | ||||||||
| ChEMBL | Activity against murine PPAR alpha receptor | B | 5.06 | pEC50 | 8800 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| 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 human PPARdelta (unknown origin) by competitive TR-FRET assay | B | 9.4 | pKd | 0.4 | nM | Kd | J Med Chem (2013) 56: 1535-1543 [PMID:23286787] |
| GtoPdb | - | - | 9 | pIC50 | - | - | - |
Atherosclerosis (2005) 181: 29-37 [PMID:15939051]; Bioorg Med Chem Lett (2003) 13: 1517-21 [PMID:12699745] |
| ChEMBL | Binding affinity for human PPAR delta receptor | B | 9 | pIC50 | 1 | nM | IC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| ChEMBL | Agonist activity at human PPARdelta LBD by cell based luciferase reporter gene assay | F | 6.52 | pEC50 | 300 | nM | EC50 | J Med Chem (2011) 54: 788-808 [PMID:21218783] |
| ChEMBL | Activation of PPARbeta-LBD (unknown origin) assessed as fluorescein-labeled coactivator C33 recruitment by TR-FRET assay | B | 7.17 | pEC50 | 67.11 | nM | EC50 | Bioorg Med Chem Lett (2016) 26: 3978-3983 [PMID:27450788] |
| ChEMBL | Agonist activity at human PPARdelta transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay | B | 7.57 | pEC50 | 26.9 | nM | EC50 | J Med Chem (2021) 64: 6996-7032 [PMID:33988379] |
| ChEMBL | Agonist activity at human PPARdelta transfected in human HEK293 cells incubated for 18 hrs by Renilla/Firefly dual-luciferase reporter assay | B | 7.74 | pEC50 | 18 | nM | EC50 | Eur J Med Chem (2021) 225: 113807-113807 [PMID:34455359] |
| ChEMBL | Agonist activity at human GAL4 fused PPARdelta-LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay | B | 7.89 | pEC50 | 13 | nM | EC50 | Eur J Med Chem (2018) 159: 267-276 [PMID:30296685] |
| ChEMBL | Transactivation of GAL4-fused human PPARdelta LBD expressed in HEK293 cells after 18 hrs by luciferase reporter gene assay | B | 7.89 | pEC50 | 13 | nM | EC50 | Eur J Med Chem (2019) 164: 352-365 [PMID:30605833] |
| ChEMBL | Agonist activity at PPARdelta (unknown origin) by Alpha Screen assay | B | 8.4 | pEC50 | 4 | nM | EC50 | Medchemcomm (2019) 10: 1412-1419 [PMID:31673308] |
| ChEMBL | Agonist activity at human PPAR-delta | B | 8.4 | pEC50 | 4 | nM | EC50 | J Med Chem (2016) 59: 9201-9214 [PMID:27652492] |
| ChEMBL | Displacement of pan-PPAR fluormone from PPARdelta LBD by TR-FRET based LanthaScreen assay | B | 8.54 | pEC50 | 2.9 | nM | EC50 | J Med Chem (2012) 55: 4978-4989 [PMID:22582973] |
| ChEMBL | Agonist activity at human PPARdelta after 22 to 24 hrs by luciferase reporter gene assay | B | 8.7 | pEC50 | 2 | nM | EC50 | Bioorg Med Chem Lett (2018) 28: 2717-2722 [PMID:29628329] |
| ChEMBL | Agonist activity at human PPARdelta expressed in nonhuman mammalian cells assessed as increase in receptor transcriptional activity incubated for 22 to 24 hrs by luciferase reporter gene assay | B | 8.72 | pEC50 | 1.9 | nM | EC50 | J Med Chem (2020) 63: 2854-2876 [PMID:32096640] |
| ChEMBL | Maximum transcriptional activation of human PPAR delta receptor | B | 9 | pEC50 | 1 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| ChEMBL | Agonist activity at PPARdelta (unknown origin) | B | 9 | pEC50 | 1 | nM | EC50 | Eur J Med Chem (2018) 159: 267-276 [PMID:30296685] |
| Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2458] [GtoPdb: 594] [UniProtKB: P35396] | ||||||||
| ChEMBL | Activity against murine PPAR delta receptor | B | 7.52 | pEC50 | 30 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| ChEMBL | Agonist activity at mouse PPAR-delta expressed in african green monkey CV-1 cells after 24 hrs by luciferase reporter gene assay | F | 8.24 | pEC50 | <=5.8 | nM | EC50 | Bioorg Med Chem Lett (2010) 20: 7239-7242 [PMID:21074432] |
| 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 transfected in COS-7 cells assessed luciferase activity measured after 24 hrs by cell based luciferase transactivation assay | B | 5.02 | pEC50 | 9530 | nM | EC50 | J Med Chem (2021) 64: 6996-7032 [PMID:33988379] |
| ChEMBL | Maximum transcriptional activation of human PPAR gamma receptor | B | 5.7 | pEC50 | 2000 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238] | ||||||||
| ChEMBL | Activity against murine PPAR gamma receptor | B | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem Lett (2003) 13: 1517-1521 [PMID:12699745] |
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]
