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 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]
