lorcaserin [Ligand Id: 2941] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL360328 (Lorcaserin) |
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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 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]
