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ChEMBL ligand: CHEMBL15594 (Arachidonate, Arachidonic acid, Cis-5,8,11,14-Eicosatetraenoic Acid) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519] | ||||||||
ChEMBL | Inhibition of FAAH | B | 4 | pIC50 | >100000 | nM | IC50 | J. Med. Chem. (2008) 51: 7327-7343 [PMID:18983142] |
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 | 4.55 | pIC50 | 28200 | nM | IC50 | J. Nat. Prod. (2006) 69: 700-703 [PMID:16643058] |
cPLA2-4C/Cytosolic phospholipase A2 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4834] [GtoPdb: 1426] [UniProtKB: Q9UP65] | ||||||||
ChEMBL | Concentration required to inhibit human Cytosolic phospholipase A2 | B | 4 | pIC50 | >100000 | nM | IC50 | Bioorg. Med. Chem. Lett. (2001) 11: 587-590 [PMID:11229777] |
fatty acid binding protein 4/Fatty acid binding protein adipocyte in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2083] [GtoPdb: 2534] [UniProtKB: P15090] | ||||||||
ChEMBL | Binding affinity against Adipocyte lipid binding protein | B | 6.74 | pKd | 180 | nM | Kd | J. Med. Chem. (2002) 45: 2469-2483 [PMID:12036355] |
GroEL/GroES in Escherichia coli (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106139] [UniProtKB: Q548M1, Q7BGE6] | ||||||||
ChEMBL | Inhibition of Escherichia coli GroEL expressed in Escherichia coli DH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured rhodanese refolding by measuring rhodanese enzyme activity after 45 mins by Fe(SCN)3 dye based spectrometric analysis | B | 4.74 | pIC50 | 18000 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084] |
ChEMBL | Inhibition of Escherichia coli GroEL expressed in Escherichia coliDH5alpha/Escherichia coli GroES expressed in Escherichia coli BL21 (DE3) assessed as reduction in GroEL/GroES-mediated denatured soluble pig heart MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 20 to 40 mins by malachite green dye based spectrometric analysis | B | 5.14 | pIC50 | 7300 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084] |
HSP60/HSP10 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL4106131] [UniProtKB: P10809, P61604] | ||||||||
ChEMBL | Inhibition of human N-terminal octa-His-tagged HSP60 expressed in Escherichia coli Rosetta(DE3) pLysS/human HSP10 expressed in Escherichia coli Rosetta(DE3) assessed as reduction in HSP60/HSP10-mediated denatured MDH refolding by measuring MDH enzyme activity using sodium mesoxalate as substrate after 40 to 60 mins by malachite green dye based spectrometric analysis | B | 5.35 | pIC50 | 4500 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 1106-1112 [PMID:30852084] |
Peroxisome proliferator-activated receptor-α/Peroxisome proliferator-activated receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL239] [GtoPdb: 593] [UniProtKB: Q07869] | ||||||||
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 | 5.51 | pIC50 | 3100 | 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 | Displacement of [3H]BRL49653 from Homo sapiens (human) PPARgamma receptor by scintillation proximity assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | Med Chem Res (2013) 22: 3126-3133 |
TRPV2/Transient receptor potential cation channel subfamily V member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2863] [GtoPdb: 508] [UniProtKB: Q9WUD2] | ||||||||
ChEMBL | Antagonist activity at recombinant rat TRPV2 expressed in HEK293 cells assessed as inhibition of LPC-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 8255-8281 [PMID:30176215] |
ChEMBL | Antagonist activity at recombinant rat TRPV2 expressed in HEK293 cells assessed as inhibition of CBD-induced Ca2+ levels preincubated for 5 mins followed by agonist addition by Fuo-4-AM based spectrofluorimetry | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2018) 61: 8255-8281 [PMID:30176215] |
Cav1.2/Voltage-gated L-type calcium channel alpha-1C subunit in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3762] [GtoPdb: 529] [UniProtKB: P22002] | ||||||||
ChEMBL | Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes | F | 5.07 | pIC50 | 8500 | nM | IC50 | Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000] |
ChEMBL | Inhibition of L-type calcium channel measured using whole-cell patch clamp in rat ventricular myocytes | F | 5.24 | pIC50 | 5800 | nM | IC50 | Journal of Applied Toxicology (2012) 32: 858-866 [PMID:22761000] |
Kir2.3 in Human [GtoPdb: 432] [UniProtKB: P48050] | ||||||||
GtoPdb | - | - | 6.35 | pEC50 | - | - | - | Mol Pharmacol (2001) 59: 1061-8 [PMID:11306688] |
TRPV4 in Mouse [GtoPdb: 510] [UniProtKB: Q9EPK8] | ||||||||
GtoPdb | - | - | 5 | pEC50 | - | - | - | Nature (2003) 424: 434-8 [PMID:12879072] |
K2P2.1 in Human [GtoPdb: 514] [UniProtKB: O95069] | ||||||||
GtoPdb | - | - | 5 | pEC50 | 10000 | nM | EC50 | EMBO J (1998) 17: 4283-90 [PMID:9687497] |
K2P3.1 in Human [GtoPdb: 515] [UniProtKB: O14649] | ||||||||
GtoPdb | - | - | 1 | pIC50 | - | - | - | EMBO J (2001) 20: 47-54 [PMID:11226154] |
Kv4.2 in Rat [GtoPdb: 553] [UniProtKB: Q63881] | ||||||||
GtoPdb | - | - | 5.7 | pIC50 | - | - | - |
Life Sci (1999) 65: PL143-9 [PMID:10503950]; J Neurosci (1996) 16: 2522-32 [PMID:8786428] |
ChEMBL data shown on this page come from version 31:
Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]