lorcaserin [Ligand Id: 2941] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL360328 (Lorcaserin)
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • NET/Norepinephrine transporter in Human [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
There should be some charts here, you may need to enable JavaScript!
  • SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
There should be some charts here, you may need to enable JavaScript!
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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños 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]