bezafibrate [Ligand Id: 2668] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL264374 (Bezafibrate, Bezafibrato, 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 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]
