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ChEMBL ligand: CHEMBL8739 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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coagulation factor VII/coagulation factor III, tissue factor/Coagulation factor VII/tissue factor in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2095194] [GtoPdb: 2363, 3192] [UniProtKB: P08709, P13726] | ||||||||
ChEMBL | Inhibition of amidolytic activity of human tissue factor/human factor 7a | B | 4.52 | pIC50 | 30000 | nM | IC50 | J Nat Prod (1998) 61: 1352-1355 [PMID:9834151] |
COX-1 /Cyclooxygenase-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL221] [GtoPdb: 1375] [UniProtKB: P23219] | ||||||||
ChEMBL | Inhibition of COX-1 (unknown origin) using arachidonic acid as substrate assessed as formation of prostanoid products preincubated for 10 mins prior to substrate addition measured after 2 mins by Ellman's method | B | 5.4 | pKi | 4000 | nM | Ki | J Med Chem (2013) 56: 8377-8388 [PMID:24088053] |
Cyclooxygenase-1 in Bovine (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2860] [UniProtKB: O62664] | ||||||||
ChEMBL | Inhibition of bovine COX1-mediated prostaglandin biosynthesis using [1-14C]arachidonic acid | B | 4.03 | pIC50 | 93000 | nM | IC50 | J Nat Prod (2001) 64: 745-749 [PMID:11421736] |
Cyclooxygenase-2 in Sheep (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4102] [UniProtKB: P79208] | ||||||||
ChEMBL | Inhibition of sheep COX2-mediated prostaglandin biosynthesis using [1-14C]arachidonic acid | B | 4.92 | pIC50 | 12000 | nM | IC50 | J Nat Prod (2001) 64: 745-749 [PMID:11421736] |
CYP19A1/Cytochrome P450 19A1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1978] [GtoPdb: 1362] [UniProtKB: P11511] | ||||||||
ChEMBL | Inhibition of aromatase in human placental microsomes by radiometric method | B | 4.35 | pIC50 | 44200 | nM | IC50 | J Nat Prod (2006) 69: 700-703 [PMID:16643058] |
FFA1 receptor/Free fatty acid receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4422] [GtoPdb: 225] [UniProtKB: O14842] | ||||||||
ChEMBL | Agonist activity at recombinant human GPR40 expressed in HEK293 cells assessed as increase in intracellular calcium flux measured for 120 secs by calcium-5 dye based assay | F | 4.96 | pEC50 | 11090 | nM | EC50 | Eur J Med Chem (2018) 158: 123-133 [PMID:30212763] |
ChEMBL | Agonist activity at human GPR40 expressed in T-REx HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay | F | 5.28 | pEC50 | 5200 | nM | EC50 | J Med Chem (2008) 51: 7640-7644 [PMID:19007110] |
ChEMBL | Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay | F | 5.5 | pEC50 | 3162.28 | nM | EC50 | J Med Chem (2016) 59: 2841-2846 [PMID:26928019] |
ChEMBL | Agonist activity at human FFA1 receptor expressed in human 1321N1 cells measured for 50 intervals of 0.4 secs by calcium mobilization assay | F | 5.52 | pEC50 | 3000 | nM | EC50 | J Med Chem (2016) 59: 2841-2846 [PMID:26928019] |
ChEMBL | Agonist activity at FFAR1 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 30 mins by BRET assay | F | 5.54 | pEC50 | 2884.03 | nM | EC50 | J Med Chem (2012) 55: 4511-4515 [PMID:22519963] |
GtoPdb | - | - | 5.7 | pEC50 | - | - | - |
J Biol Chem (2003) 278: 11303-11 [PMID:12496284]; Biochem Biophys Res Commun (2003) 301: 406-10 [PMID:12565875]; Nature (2003) 422: 173-6 [PMID:12629551] |
FFA4 receptor/G-protein coupled receptor 120 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5339] [GtoPdb: 127] [UniProtKB: Q5NUL3] | ||||||||
ChEMBL | Agonist activity at GPR120 expressed in HEK 293 cells assessed as beta-arrestin recruitment after 5 mins by BRET assay | F | 5.49 | pEC50 | 3235.94 | nM | EC50 | J Med Chem (2012) 55: 4511-4515 [PMID:22519963] |
GtoPdb | - | - | 5.5 | pEC50 | - | - | - | J Med Chem (2012) 55: 4511-5 [PMID:22519963] |
ChEMBL | Agonist activity at human GPR120-G-alpha-16 fusion protein expressed in Flp-in HEK293 cells assessed as effect on intracellular calcium concentration by FLIPR assay | F | 5.59 | pEC50 | 2600 | nM | EC50 | J Med Chem (2008) 51: 7640-7644 [PMID:19007110] |
FFA4 receptor in Rat [GtoPdb: 127] [UniProtKB: Q2AC31] | ||||||||
GtoPdb | - | - | 5.06 | pEC50 | - | - | - | Naunyn Schmiedebergs Arch Pharmacol (2008) 377: 515-22 [PMID:18320172] |
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 to PPAR-alpha (unknown origin) by fluorescence-based assay | B | 8.1 | pKd | 7.9 | nM | Kd | Med Chem Res (2009) 18: 8-19 |
ChEMBL | Inhibition of PPAR-alpha (unknown origin) by SPA assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | Med Chem Res (2009) 18: 8-19 |
ChEMBL | Displacement of [3H]GW2331 from Homo sapiens (human) PPARalpha receptor by scintillation proximity assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | Med Chem Res (2013) 22: 3126-3133 |
Peroxisome proliferator-activated receptor-β/δ/Peroxisome proliferator-activated receptor delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3979] [GtoPdb: 594] [UniProtKB: Q03181] | ||||||||
ChEMBL | Displacement of [3H]GW2433 from Homo sapiens (human) PPARdelta receptor by scintillation proximity assay | B | 4.8 | pIC50 | 16000 | nM | IC50 | Med Chem Res (2013) 22: 3126-3133 |
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 to PPARgamma | B | 5.7 | pKd | 2000 | nM | Kd | J Med Chem (2012) 55: 4027-4061 [PMID:22260081] |
ChEMBL | Displacement of [3H]BRL49653 from Homo sapiens (human) PPARgamma receptor by scintillation proximity assay | B | 5.22 | pIC50 | 6000 | nM | IC50 | Med Chem Res (2013) 22: 3126-3133 |
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]