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 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]
