bezafibrate [Ligand Id: 2668] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL264374 (Bezafibrate, Bezagen xl, Bezalip, Bezalip-mono, Bezatol sr, BM 15.075, BM-15.075, BM-15075, Fibrazate xl, Liparol xl, NSC-758174, Zimbacol xl) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| fatty acid binding protein 2/Fatty acid binding protein intestinal in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879] [GtoPdb: 2532] [UniProtKB: P12104] | ||||||||
| ChEMBL | Displacement of 1-anilinonaphthalene-8-sulphonic acid from I-FABP | B | 4.48 | pKi | 33000 | nM | Ki | J Med Chem (2008) 51: 3755-3764 [PMID:18533710] |
| fatty acid binding protein 1/Fatty acid-binding protein, liver in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5738] [GtoPdb: 2531] [UniProtKB: P02692] | ||||||||
| ChEMBL | Displacement of 1-anilinonaphthalene-8-sulphonic acid from rat recombinant L-FABP low binding affinity site expressed in Escherichia coli BL21 by competitive fluorescence displacement assay | B | 4.35 | pKi | 44400 | nM | Ki | J Med Chem (2008) 51: 3755-3764 [PMID:18533710] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
| ChEMBL | Transactivation of human Peroxisome proliferator activated receptor alpha expressed in CHO-K1 cells | B | 4.11 | pEC50 | >78000 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 77-80 [PMID:11738577] |
| ChEMBL | In vitro effective concentration for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected KRP-297 cells | F | 4.11 | pEC50 | >78000 | nM | EC50 | J Med Chem (2003) 46: 3581-3599 [PMID:12904063] |
| GtoPdb | - | - | 4.3 | pEC50 | - | - | - |
J Med Chem (2004) 47: 4118-27 [PMID:15293980]; Biochem Biophys Res Commun (2002) 290: 131-9 [PMID:11779144] |
| ChEMBL | Activity at PPARalpha | B | 4.3 | pEC50 | 50000 | nM | EC50 | J Med Chem (2009) 52: 6931-6935 [PMID:19817384] |
| ChEMBL | Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay | B | 4.3 | pEC50 | 50000 | nM | EC50 | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
| ChEMBL | Agonist activity for Human PPAR alpha receptor in transcriptional activation assay | F | 4.3 | pEC50 | 50000 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | Compound was tested for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected CV-1 cells | F | 4.3 | pEC50 | 50000 | nM | EC50 | J Med Chem (1999) 42: 3785-3788 [PMID:10508427] |
| ChEMBL | Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay | B | 4.33 | pEC50 | 46580 | nM | EC50 | Bioorg Med Chem (2013) 21: 766-778 [PMID:23265844] |
| ChEMBL | Agonist activity at human PPARalpha expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay | F | 4.37 | pEC50 | 42500 | nM | EC50 | Bioorg Med Chem (2011) 19: 771-782 [PMID:21215640] |
| ChEMBL | In vitro transactivation using receptor transactivation assay against hPPAR alpha | F | 4.45 | pEC50 | 35700 | nM | EC50 | J Med Chem (2002) 45: 789-804 [PMID:11831892] |
| ChEMBL | Agonist activity at GAL4-tagged PPARalpha-LBD (unknown origin) expressed in HEK293 cells assessed as induction of receptor transactivation incubated for 16 hrs by luciferase reporter gene assay | B | 4.5 | pEC50 | 31700 | nM | EC50 | J Med Chem (2020) 63: 13124-13139 [PMID:33142057] |
| ChEMBL | Agonist activity at human PPARalpha expressed in monkey CV1 cells by transactivation assay | F | 4.52 | pEC50 | 30000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 2128-2132 [PMID:18280733] |
| ChEMBL | Agonist activity at human PPARalpha expressed in CV1 cells by transactivation assay | F | 4.52 | pEC50 | 30000 | nM | EC50 | Bioorg Med Chem (2008) 16: 981-994 [PMID:17964792] |
| ChEMBL | Agonist activity at Gal4-tagged human PPARalpha ligand binding domain expressed in COS-7 cells measured after overnight incubation by dual-glo luciferase reporter gene assay | B | 5.15 | pEC50 | 7100 | nM | EC50 | Medchemcomm (2016) 7: 1209-1216 |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204] | ||||||||
| ChEMBL | Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor transfected CV-1 cells | F | 4.05 | pEC50 | 90000 | nM | EC50 | J Med Chem (1999) 42: 3785-3788 [PMID:10508427] |
| ChEMBL | Agonist activity for murine PPAR alpha receptor in transcriptional activation assay | F | 4.05 | pEC50 | 90000 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| 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 HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay | B | 4.45 | pEC50 | 35740 | nM | EC50 | Bioorg Med Chem (2013) 21: 766-778 [PMID:23265844] |
| ChEMBL | Agonist activity at human PPARdelta expressed in CV1 cells by transactivation assay | F | 4.52 | pEC50 | 30000 | nM | EC50 | Bioorg Med Chem (2008) 16: 981-994 [PMID:17964792] |
| ChEMBL | Agonist activity at human PPARdelta expressed in monkey CV1 cells by transactivation assay | F | 4.52 | pEC50 | 30000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 2128-2132 [PMID:18280733] |
| ChEMBL | Agonist activity at Gal4-tagged human PPARdelta ligand binding domain expressed in COS-7 cells measured after overnight incubation by dual-glo luciferase reporter gene assay | B | 4.65 | pEC50 | 22600 | nM | EC50 | Medchemcomm (2016) 7: 1209-1216 |
| ChEMBL | Compound was tested for agonist activity on human Peroxisome proliferator activated receptor delta-GAL4 chimeric receptor in transfected CV-1 cells | F | 4.7 | pEC50 | 20000 | nM | EC50 | J Med Chem (1999) 42: 3785-3788 [PMID:10508427] |
| ChEMBL | Agonist activity for Human PPAR delta receptor in transcriptional activation assay | F | 4.7 | pEC50 | 20000 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | Agonist activity at human PPARdelta expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay | F | 4.72 | pEC50 | 18900 | nM | EC50 | Bioorg Med Chem (2011) 19: 771-782 [PMID:21215640] |
| 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 monkey CV1 cells by transactivation assay | F | 4 | pEC50 | 100000 | nM | EC50 | Bioorg Med Chem Lett (2008) 18: 2128-2132 [PMID:18280733] |
| ChEMBL | In vitro transactivation using receptor transactivation assay against hPPAR gamma | F | 4.13 | pEC50 | 73500 | nM | EC50 | J Med Chem (2002) 45: 789-804 [PMID:11831892] |
| ChEMBL | Agonist activity at human PPARgamma expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay | B | 4.15 | pEC50 | 70360 | nM | EC50 | Bioorg Med Chem (2013) 21: 766-778 [PMID:23265844] |
| ChEMBL | Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assay | B | 4.22 | pEC50 | 60000 | nM | EC50 | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
| ChEMBL | Agonist activity for Human PPAR gamma receptor in transcriptional activation assay | F | 4.22 | pEC50 | 60000 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | Compound was tested for agonist activity on human Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells | F | 4.22 | pEC50 | 60000 | nM | EC50 | J Med Chem (1999) 42: 3785-3788 [PMID:10508427] |
| ChEMBL | Agonist activity at human PPARgamma expressed in HepG2 cells co-transfected with PPRE3-TK-luc assessed as beta-galactosidase activity after 20 to 22 hrs by luciferase based transactivation assay | F | 4.24 | pEC50 | 57200 | nM | EC50 | Bioorg Med Chem (2011) 19: 771-782 [PMID:21215640] |
| ChEMBL | Agonist activity at Gal4-tagged human PPARgamma ligand binding domain expressed in COS-7 cells measured after overnight incubation by dual-glo luciferase reporter gene assay | B | 4.81 | pEC50 | 15400 | nM | EC50 | Medchemcomm (2016) 7: 1209-1216 |
| ChEMBL | Agonist activity at human PPARgamma expressed in CV1 cells by transactivation assay | F | 5.52 | pEC50 | 3000 | nM | EC50 | Bioorg Med Chem (2008) 16: 981-994 [PMID:17964792] |
| Peroxisome proliferator-activated receptor-γ/Peroxisome proliferator-activated receptor gamma in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2459] [GtoPdb: 595] [UniProtKB: P37238] | ||||||||
| ChEMBL | Compound was tested for its agonist activity against murine Peroxisome proliferator activated receptor gamma-Gal4 chimeric receptor in transfected CV-1 cells | F | 4.26 | pEC50 | 55000 | nM | EC50 | J Med Chem (1999) 42: 3785-3788 [PMID:10508427] |
| ChEMBL | Agonist activity for murine PPAR gamma receptor in transcriptional activation assay | F | 4.26 | pEC50 | 55000 | 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]
