MK-0767 [Ligand Id: 2677] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL24458 (KRP-297) |
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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 | Binding affinity towards peroxisome proliferator activated receptor alpha | B | 6.64 | pKd | 230 | nM | Kd | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| ChEMBL | Binding affinity for Peroxisome proliferator activated receptor alpha (PPAR alpha) | B | 6.64 | pKd | 228 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 533-538 [PMID:10098657] |
| GtoPdb | - | - | 7.64 | pKd | - | - | - |
Biochem Biophys Res Commun (2004) 318: 323-8 [PMID:15120604]; Diabetes (1998) 47: 1841-7 [PMID:9836514]; Biochem Biophys Res Commun (1999) 260: 609-13 [PMID:10403814] |
| ChEMBL | Binding affinity for human peroxisome proliferator activated receptor alpha | B | 6.64 | pKi | 230 | nM | Ki | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
| ChEMBL | Binding affinity towards human peroxidase proliferator activated receptor alpha (hPPARalpha) | B | 6.04 | pIC50 | 914 | nM | IC50 | J Med Chem (2001) 44: 2061-2064 [PMID:11405642] |
| ChEMBL | In vitro effective concentration for agonist activity on human Peroxisome proliferator activated receptor alpha-Gal4 chimeric receptor in transfected KRP-297 cells | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2003) 46: 3581-3599 [PMID:12904063] |
| ChEMBL | Transactivation of human Peroxisome proliferator activated receptor alpha expressed in CHO-K1 cells | B | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 77-80 [PMID:11738577] |
| ChEMBL | Effective concentration against human peroxisome proliferator activated receptor alpha in Gal4 transactivation assay | B | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
| ChEMBL | Agonistic activity for Peroxisome proliferator activated receptor alpha | F | 6 | pEC50 | 1000 | nM | EC50 | J Med Chem (2003) 46: 1306-1317 [PMID:12672231] |
| ChEMBL | Binding affinity at human PPAR alpha | B | 6.04 | pEC50 | 922 | nM | EC50 | J Med Chem (2001) 44: 2061-2064 [PMID:11405642] |
| ChEMBL | Agonist activity for Human PPAR alpha receptor in transcriptional activation assay | F | 6.07 | pEC50 | 850 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| ChEMBL | Agonist activity at GAL4-fused PPARalpha assessed as transcriptional activity by cell based assay | F | 6.1 | pEC50 | 800 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 7075-7079 [PMID:23084275] |
| ChEMBL | Agonist activity at human PPARalpha-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay | F | 6.4 | pEC50 | 400 | nM | EC50 | Bioorg Med Chem (2011) 19: 3255-3264 [PMID:21515063] |
| Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2128] [GtoPdb: 593] [UniProtKB: P23204] | ||||||||
| ChEMBL | Agonist activity for murine PPAR alpha receptor in transcriptional activation assay | F | 5 | pEC50 | 10000 | 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-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay | F | 5 | pEC50 | >10000 | nM | EC50 | Bioorg Med Chem (2011) 19: 3255-3264 [PMID:21515063] |
| ChEMBL | Agonist activity for Human PPAR delta receptor in transcriptional activation assay | F | 5.04 | pEC50 | 9100 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| 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 | 5.14 | pEC50 | 7200 | 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 | Binding affinity towards peroxisome proliferator activated receptor gamma | B | 6.48 | pKd | 330 | nM | Kd | J Med Chem (2005) 48: 6523-6543 [PMID:16220969] |
| ChEMBL | Binding affinity for Peroxisome proliferator activated receptor gamma (PPAR gamma) | B | 6.49 | pKd | 326 | nM | Kd | Bioorg Med Chem Lett (1999) 9: 533-538 [PMID:10098657] |
| GtoPdb | - | - | 6.49 | pKd | - | - | - |
Diabetes (1998) 47: 1841-7 [PMID:9836514]; Biochem Biophys Res Commun (1999) 260: 609-13 [PMID:10403814] |
| ChEMBL | Binding affinity for human peroxisome proliferator activated receptor gamma | B | 6.48 | pKi | 330 | nM | Ki | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
| ChEMBL | Binding affinity at human peroxidase proliferator activated receptor gamma (hPPARgamma) | B | 6.33 | pIC50 | 463 | nM | IC50 | J Med Chem (2001) 44: 2061-2064 [PMID:11405642] |
| ChEMBL | Binding affinity at human PPAR gamma | B | 5.96 | pEC50 | 1090 | nM | EC50 | J Med Chem (2001) 44: 2061-2064 [PMID:11405642] |
| ChEMBL | Agonist activity at GAL4-fused PPARgamma assessed as transcriptional activity by cell based assay | F | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2012) 22: 7075-7079 [PMID:23084275] |
| ChEMBL | Agonist activity at human PPARgamma-LBD expressed in CV1 cells co-transfected with Gal4 after 40 hrs by luciferase based transactivation assay | F | 6.05 | pEC50 | 900 | nM | EC50 | Bioorg Med Chem (2011) 19: 3255-3264 [PMID:21515063] |
| ChEMBL | Transactivation activity at Homo sapiens (human) PPARgamma | B | 6.07 | pEC50 | 850 | nM | EC50 | Med Chem Res (2011) 20: 1005-1014 |
| ChEMBL | Agonistic activity for human Peroxisome proliferator activated receptor gamma | F | 6.1 | pEC50 | 800 | nM | EC50 | J Med Chem (2003) 46: 1306-1317 [PMID:12672231] |
| ChEMBL | Effective concentration against human peroxisome proliferator activated receptor gamma in Gal4 transactivation assay | B | 6.1 | pEC50 | 800 | nM | EC50 | J Med Chem (2004) 47: 4118-4127 [PMID:15293980] |
| ChEMBL | Concentration of compound that affords half-maximum transactivation of human Peroxisome proliferator activated receptor gamma in CHO-K1 cells was determined in vitro | B | 6.1 | pEC50 | 800 | nM | EC50 | Bioorg Med Chem Lett (2002) 12: 77-80 [PMID:11738577] |
| ChEMBL | Agonist activity on Gal4 chimeric human Peroxisome proliferator activated receptor gamma expressed in KRP-297 cells | F | 6.1 | pEC50 | 800 | nM | EC50 | J Med Chem (2003) 46: 3581-3599 [PMID:12904063] |
| GtoPdb | - | - | 7 | pEC50 | - | - | - | Biochem Biophys Res Commun (2004) 318: 323-8 [PMID:15120604] |
| ChEMBL | Agonist activity for Human PPAR gamma receptor in transcriptional activation assay | F | 7.08 | pEC50 | 83 | nM | EC50 | J Med Chem (2000) 43: 527-550 [PMID:10691680] |
| 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 | 6.85 | pEC50 | 140 | 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]
