JWH015 [Ligand Id: 5558] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL306764 (JWH-015) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Farnesoid X receptor/Bile acid receptor FXR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2047] [GtoPdb: 603] [UniProtKB: Q96RI1] | ||||||||
| ChEMBL | Antagonist activity at human GTS-tagged FXR after 20 mins by TR-FRET assay | B | 5.49 | pIC50 | 3220 | nM | IC50 | Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559] |
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Binding affinity towards cloned human Cannabinoid receptor 1 | B | 2.58 | pKi | 2.58 | nM | Log Ki | J Med Chem (2000) 43: 2300-2309 [PMID:10882356] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | B | 5.92 | pKi | 1204 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 5.92 | pKi | 1204 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in CHO cells | B | 5.92 | pKi | 1202.26 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB1 receptor expressed in HEK cells | B | 5.92 | pKi | 1202.26 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB1 receptor in cell free system | B | 6.42 | pKi | 383 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| ChEMBL | Binding affinity to CB1 receptor (unknown origin) | B | 6.42 | pKi | 383 | nM | Ki | J Med Chem (2013) 56: 7161-7176 [PMID:23672690] |
| ChEMBL | Binding affinity to CB1 receptor (unknown origin) | B | 6.42 | pKi | 383 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| CB1 receptor/Cannabinoid CB1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3571] [GtoPdb: 56] [UniProtKB: P20272] | ||||||||
| ChEMBL | Displacement of [3H]CP-55940 from CB1 receptor in rat brain by filtration assay | B | 6.78 | pKi | 164.06 | nM | Ki | Eur J Med Chem (2009) 44: 2482-2496 [PMID:19249138] |
| CB2 receptor/Cannabinoid CB2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL253] [GtoPdb: 57] [UniProtKB: P34972] | ||||||||
| ChEMBL | Binding affinity towards cloned human cannabinoid receptor 2 | B | 1.14 | pKi | 1.14 | nM | Log Ki | J Med Chem (2000) 43: 2300-2309 [PMID:10882356] |
| ChEMBL | In vitro inhibitory activity towards human cannabinoid receptors 2 using fluorescence assay | B | 7.44 | pKi | 36 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 3758-3762 [PMID:15993070] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells | B | 7.45 | pKi | 35.48 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | B | 7.45 | pKi | 35.48 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK cells | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Displacement of [3H]CP-55940 from human recombinant CB2 receptor expressed in HEK293 cells | B | 7.46 | pKi | 35 | nM | Ki | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| ChEMBL | Binding affinity to CB2 receptor (unknown origin) | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2013) 56: 7161-7176 [PMID:23672690] |
| ChEMBL | Binding affinity to CB2 receptor (unknown origin) | B | 7.85 | pKi | 14 | nM | Ki | J Med Chem (2013) 56: 8224-8256 [PMID:23865723] |
| ChEMBL | Displacement of [3H]CP-55940 from human cloned CB2 receptor by filtration assay | B | 7.86 | pKi | 13.8 | nM | Ki | Eur J Med Chem (2009) 44: 2482-2496 [PMID:19249138] |
| ChEMBL | Displacement of [3H]CP 55940 from human CB2 receptor in cell free system | B | 7.88 | pKi | 13.3 | nM | Ki | Eur J Med Chem (2011) 46: 547-555 [PMID:21183257] |
| ChEMBL | Agonist activity at human recombinant CB2 receptor expressed in HEK cells assessed as calcium mobilization by FLIPR | F | 6.2 | pEC50 | 634 | nM | EC50 | J Med Chem (2008) 51: 1904-1912 [PMID:18311894] |
| ChEMBL | Agonist activity at human recombinant CB2 receptor expressed in HEK293 cells coexpressing Galphaq/o5 assessed as calcium mobilization by FLIPR assay | F | 6.2 | pEC50 | 634 | nM | EC50 | J Med Chem (2010) 53: 295-315 [PMID:19921781] |
| CB2 receptor/Cannabinoid CB2 receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5373] [GtoPdb: 57] [UniProtKB: P47936] | ||||||||
| ChEMBL | Inverse agonist activity at C-terminally prolink-tagged mouse CB2 receptor expressed in CHOK1 cells harboring beta-galactosidase enzyme fused beta-arrestin assessed as increase in beta-arrestin recruitment after 90 mins by chemiluminescent assay | B | 6.8 | pEC50 | 160 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| ChEMBL | Inverse agonist activity at mouse CB2 receptor expressed in HEK293 cells assessed as inhibition of forskolin-mediated cAMP accumulation after 5 mins by fluorescence assay | F | 7.52 | pEC50 | 30 | nM | EC50 | J Med Chem (2018) 61: 9841-9878 [PMID:29939744] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| Pregnane X receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3401] [GtoPdb: 606] [UniProtKB: O75469] | ||||||||
| ChEMBL | Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay | B | 5.58 | pEC50 | 2640 | nM | EC50 | Bioorg Med Chem (2013) 21: 4266-4278 [PMID:23688559] |
| GPR55 in Human [GtoPdb: 109] [UniProtKB: Q9Y2T6] | ||||||||
| GtoPdb | - | - | 8.4 | pEC50 | 4 | nM | EC50 | Br J Pharmacol (2007) 152: 1092-101 [PMID:17876302] |
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]
