lorcaserin [Ligand Id: 2941] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL360328 (Lorcaserin, Lorcaserina, Lorcaserine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-hydroxytryptamine receptor 2C in Dog (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770041] [UniProtKB: Q60F97] | ||||||||
| ChEMBL | Agonist activity at dog 5HT2C receptor | F | 7.79 | pEC50 | 16.2 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 2715-2720 [PMID:21195614] |
| DAT/Dopamine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL238] [GtoPdb: 927] [UniProtKB: Q01959] | ||||||||
| ChEMBL | Displacement of [3H]WIN-35428 from DAT | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 1885-1902 [PMID:19284718] |
| NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
| ChEMBL | Displacement of [3H]nisoxetine from NET | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2009) 52: 1885-1902 [PMID:19284718] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Displacement of [3H]ketanserin from human 5HT2A receptor | B | 5.56 | pKi | 2782 | nM | Ki | J Med Chem (2009) 52: 1885-1902 [PMID:19284718] |
| GtoPdb | - | - | 6.8 | pKi | - | - | - | J Pharmacol Exp Ther (2008) 325: 577-87 [PMID:18252809] |
| ChEMBL | Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2A receptor (unknown origin) | B | 7.01 | pKi | 98.5 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 126929-126929 [PMID:31952960] |
| ChEMBL | Agonist activity at 5-HT2A receptor (unknown origin) | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 330-335 [PMID:23177783] |
| ChEMBL | Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | F | 6.21 | pEC50 | 616 | nM | EC50 | J Med Chem (2009) 52: 1885-1902 [PMID:19284718] |
| ChEMBL | Agonist activity at human 5-HT2A receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | F | 6.52 | pEC50 | 302 | nM | EC50 | J Med Chem (2015) 58: 1992-2002 [PMID:25633969] |
| ChEMBL | Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay | F | 6.59 | pEC50 | 258 | nM | EC50 | J Med Chem (2016) 59: 578-591 [PMID:26704965] |
| ChEMBL | Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | F | 6.61 | pEC50 | 248 | nM | EC50 | J Med Chem (2016) 59: 9866-9880 [PMID:27726356] |
| ChEMBL | Agonist activity at human 5-HT2A receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | F | 6.61 | pEC50 | 245.47 | nM | EC50 | J Med Chem (2016) 59: 9866-9880 [PMID:27726356] |
| ChEMBL | Effective concentration towards 5-hydroxytryptamine 2A receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release | F | 6.72 | pEC50 | 190 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 1467-1470 [PMID:15713408] |
| ChEMBL | Agonist activity at recombinant human 5HT2A receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay | F | 6.78 | pEC50 | 165.96 | nM | EC50 | J Med Chem (2016) 59: 578-591 [PMID:26704965] |
| ChEMBL | Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | F | 6.8 | pEC50 | 158.49 | nM | EC50 | J Med Chem (2008) 51: 305-313 [PMID:18095642] |
| GtoPdb | - | - | 6.8 | pEC50 | - | - | - | J Pharmacol Exp Ther (2008) 325: 577-87 [PMID:18252809] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from 5HT2B receptor (unknown origin) | B | 6.66 | pKi | 220 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 126929-126929 [PMID:31952960] |
| ChEMBL | Displacement of [3H]LSD from human 5HT2B receptor | B | 6.72 | pKi | 189 | nM | Ki | J Med Chem (2009) 52: 1885-1902 [PMID:19284718] |
| GtoPdb | - | - | 6.8 | pKi | - | - | - | J Pharmacol Exp Ther (2008) 325: 577-87 [PMID:18252809] |
| ChEMBL | Agonist activity at 5-HT2B receptor (unknown origin) | B | 8.89 | pKi | 1.3 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 330-335 [PMID:23177783] |
| GtoPdb | - | - | 6 | pEC50 | - | - | - | J Pharmacol Exp Ther (2008) 325: 577-87 [PMID:18252809] |
| ChEMBL | Effective concentration towards 5-hydroxytryptamine 2B receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release | F | 6 | pEC50 | 1000 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 1467-1470 [PMID:15713408] |
| ChEMBL | Agonist activity at human 5HT2B receptor expressed in HEK293 cells by inositol phosphate accumulation assay | F | 6.03 | pEC50 | 943 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 2715-2720 [PMID:21195614] |
| ChEMBL | Agonist activity at human recombinant 5HT2B receptor expressed in HEK293 cells assessed as [3H]inositol incorporation after 2 hrs by TopCount scintillation counting analysis | F | 6.03 | pEC50 | 943 | nM | EC50 | J Med Chem (2015) 58: 1992-2002 [PMID:25633969] |
| ChEMBL | Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | F | 6.1 | pEC50 | 794.33 | nM | EC50 | J Med Chem (2008) 51: 305-313 [PMID:18095642] |
| ChEMBL | Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay | F | 6.29 | pEC50 | 512.86 | nM | EC50 | J Med Chem (2016) 59: 578-591 [PMID:26704965] |
| ChEMBL | Agonist activity at human 5-HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | F | 6.32 | pEC50 | 478 | nM | EC50 | J Med Chem (2015) 58: 1992-2002 [PMID:25633969] |
| ChEMBL | Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | F | 6.36 | pEC50 | 436.52 | nM | EC50 | J Med Chem (2016) 59: 9866-9880 [PMID:27726356] |
| ChEMBL | Agonist activity at human 5-HT2B receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | F | 6.36 | pEC50 | 433 | nM | EC50 | J Med Chem (2016) 59: 9866-9880 [PMID:27726356] |
| ChEMBL | Agonist activity at recombinant human 5HT2B receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay | F | 6.48 | pEC50 | 328 | nM | EC50 | J Med Chem (2016) 59: 578-591 [PMID:26704965] |
| ChEMBL | Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | F | 6.66 | pEC50 | 219 | nM | EC50 | J Med Chem (2009) 52: 1885-1902 [PMID:19284718] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Displacement of [3H]mesulergine from 5HT2C receptor | B | 6.59 | pKi | 257 | nM | Ki | J Med Chem (2009) 52: 1885-1902 [PMID:19284718] |
| ChEMBL | Displacement of [3H]meselurgine from human 5HT2C receptor expressed in Swiss mouse 3T3 cells by scintillation proximity assay | B | 6.78 | pKi | 167 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 2715-2720 [PMID:21195614] |
| GtoPdb | - | - | 7.8 | pKi | - | - | - | J Pharmacol Exp Ther (2008) 325: 577-87 [PMID:18252809] |
| ChEMBL | Agonist activity at 5-HT2CR (unknown origin) | B | 7.82 | pKi | 15 | nM | Ki | J Med Chem (2018) 62: 288-305 [PMID:29620897] |
| ChEMBL | Displacement of [3H]DOI from recombinant human 5HT2C receptor expressed in HEK293T cell membranes after 1 hr by beta scintillation counting method | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 230-233 [PMID:30545651] |
| ChEMBL | Displacement of [125I]-1,4-Iodanyl-2,5-dimethoxyphenyl)propan-2amine from recombinant human 5HT2C receptor expressed in HEK293 cells measured after 2 hrs by scintillation counter method | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem Lett (2020) 30: 126929-126929 [PMID:31952960] |
| ChEMBL | Binding affinity to 5-HT2C receptor (unknown origin) | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem (2013) 21: 7083-7090 [PMID:24084296] |
| ChEMBL | Displacement of [125I]DOI from human recombinant 5HT2C receptor expressed in HEK293 cells by scintillation counting | B | 7.82 | pKi | 15 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 2715-2720 [PMID:21195614] |
| GtoPdb | IP accumulation assay. | - | 8.24 | pIC50 | 5.8 | nM | IC50 | US6953787 B2. 5HT2C receptor modulators. (2005) |
| ChEMBL | Agonist activity at human 5HT2C receptor expressed in CHO-K1 cells assessed as increase of fluorescence based calcium mobilization by FLIPR assay | F | 6.68 | pEC50 | 210 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 2715-2720 [PMID:21195614] |
| ChEMBL | Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay | B | 7.23 | pEC50 | 59 | nM | EC50 | J Med Chem (2016) 59: 9866-9880 [PMID:27726356] |
| ChEMBL | Agonist activity at human 5-HT2C INI receptor expressed in human HEK293 cells assessed as induction of beta-arrestin-2 recruitment incubated for 20 hrs by Tango assay | B | 7.23 | pEC50 | 58.88 | nM | EC50 | J Med Chem (2016) 59: 9866-9880 [PMID:27726356] |
| ChEMBL | Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay | B | 7.4 | pEC50 | 40 | nM | EC50 | J Med Chem (2017) 60: 6273-6288 [PMID:28657744] |
| ChEMBL | Agonist activity at tTA containing TEV cleavage site-fused 5-HT2C-INI receptor isoform (unknown origin) expressed in TEV-fused beta-arrestin2 expressing HEK cells assessed as induction of beta-arrestin2 recruitment after 20 hrs by Tango assay | B | 7.4 | pEC50 | 39.81 | nM | EC50 | J Med Chem (2017) 60: 6273-6288 [PMID:28657744] |
| ChEMBL | Effective concentration towards 5-hydroxytryptamine 2C receptors transfected in HEK293 cells was determined by measuring [3H]phosphoinositol release | F | 7.96 | pEC50 | 11 | nM | EC50 | Bioorg Med Chem Lett (2005) 15: 1467-1470 [PMID:15713408] |
| ChEMBL | Agonist activity at 5-HT2C receptor (unknown origin) | B | 8.05 | pEC50 | 9 | nM | EC50 | Bioorg Med Chem Lett (2013) 23: 330-335 [PMID:23177783] |
| ChEMBL | Agonist activity at human 5HT2C receptor expressed in HEK293 cells by inositol phosphate accumulation assay | F | 8.05 | pEC50 | 9 | nM | EC50 | Bioorg Med Chem Lett (2011) 21: 2715-2720 [PMID:21195614] |
| GtoPdb | - | - | 8.1 | pEC50 | - | - | - | J Pharmacol Exp Ther (2008) 325: 577-87 [PMID:18252809] |
| ChEMBL | Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | F | 8.1 | pEC50 | 7.94 | nM | EC50 | J Med Chem (2008) 51: 305-313 [PMID:18095642] |
| ChEMBL | Agonist activity at recombinant human 5HT2C receptor expressed in HEK293 cells assessed as accumulation of inositol phosphate measured after 2 hrs in presence of [3H]inositol by scintillation counter method | F | 8.12 | pEC50 | 7.6 | nM | EC50 | Bioorg Med Chem Lett (2020) 30: 126929-126929 [PMID:31952960] |
| ChEMBL | Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay | F | 8.32 | pEC50 | 4.79 | nM | EC50 | Eur J Med Chem (2019) 182: 111626-111626 [PMID:31445232] |
| ChEMBL | Agonist activity at recombinant human unedited 5HT2C receptor isoform INI expressed in Flp-In-293 cells assessed as increase in calcium influx measured for 300 secs by Fluo-4 dye based FLIPR assay | F | 8.32 | pEC50 | 4.77 | nM | EC50 | Eur J Med Chem (2019) 182: 111626-111626 [PMID:31445232] |
| ChEMBL | Agonist activity at human 5-HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | F | 8.44 | pEC50 | 3.6 | nM | EC50 | J Med Chem (2015) 58: 1992-2002 [PMID:25633969] |
| ChEMBL | Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | F | 8.46 | pEC50 | 3.47 | nM | EC50 | J Med Chem (2016) 59: 9866-9880 [PMID:27726356] |
| ChEMBL | Agonist activity at human 5-HT2C INI receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | F | 8.47 | pEC50 | 3.4 | nM | EC50 | J Med Chem (2016) 59: 9866-9880 [PMID:27726356] |
| ChEMBL | Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay | F | 8.57 | pEC50 | 2.7 | nM | EC50 | J Med Chem (2016) 59: 578-591 [PMID:26704965] |
| ChEMBL | Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as calcium flux by FLIPR assay | F | 8.57 | pEC50 | 2.7 | nM | EC50 | J Med Chem (2009) 52: 1885-1902 [PMID:19284718] |
| ChEMBL | Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | F | 8.58 | pEC50 | 2.64 | nM | EC50 | J Med Chem (2016) 59: 9866-9880 [PMID:27726356] |
| ChEMBL | Agonist activity at human 5-HT2C receptor expressed in human Flp-In-293 cells assessed as induction of calcium flux incubated for 1 hr by Fluo-4 direct dye based FLIPR assay | F | 8.58 | pEC50 | 2.63 | nM | EC50 | J Med Chem (2016) 59: 9866-9880 [PMID:27726356] |
| ChEMBL | Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay | F | 8.58 | pEC50 | 2.63 | nM | EC50 | J Med Chem (2017) 60: 6273-6288 [PMID:28657744] |
| ChEMBL | Agonist activity at human 5-HT2C-INI receptor isoform expressed in Flp-IN HEK293 cells assessed as induction of Gq-mediated calcium flux measured every second for 5 mins by Fluo-4 dye based FLIPR assay | F | 8.68 | pEC50 | 2.1 | nM | EC50 | J Med Chem (2017) 60: 6273-6288 [PMID:28657744] |
| ChEMBL | Agonist activity at recombinant human 5HT2C-INI receptor expressed in Flp-In-293 cells assessed as calcium flux by FLIPR assay | F | 8.74 | pEC50 | 1.82 | nM | EC50 | J Med Chem (2016) 59: 578-591 [PMID:26704965] |
| SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
| ChEMBL | Displacement of [3H]citalopram from SERT | B | 5.58 | pKi | 2606 | nM | Ki | J Med Chem (2009) 52: 1885-1902 [PMID:19284718] |
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]
