(+)-norfenfluramine [Ligand Id: 216] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL253811 ((S)-Norfenfluramine) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| ChEMBL | Agonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | F | 6.7 | pEC50 | 199.53 | nM | EC50 | J Med Chem (2008) 51: 305-313 [PMID:18095642] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| ChEMBL | Binding affinity to human 5-HT2B receptor expressed in african green monkey COS7 cells assessed as inhibition constant | B | 7.95 | pKi | 11.2 | nM | Ki | J Med Chem (2023) 66: 11027-11039 [PMID:37584406] |
| GtoPdb | - | - | 8 | pKi | - | - | - | Circulation (2000) 102: 2836-41 [PMID:11104741] |
| ChEMBL | Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of phospho-inositide hydrolysis by IP hydrolysis assay | F | 7.64 | pEC50 | 23 | nM | EC50 | J Med Chem (2023) 66: 11027-11039 [PMID:37584406] |
| ChEMBL | Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of intracellular calcium level by calcium mobilization assay | F | 7.64 | pEC50 | 23 | nM | EC50 | J Med Chem (2023) 66: 11027-11039 [PMID:37584406] |
| ChEMBL | Agonist activity at 5-HT2B receptor (unknown origin) assessed as stimulation of MAPK cascade by calcium mobilization assay | F | 7.64 | pEC50 | 23 | nM | EC50 | J Med Chem (2023) 66: 11027-11039 [PMID:37584406] |
| ChEMBL | Agonist activity at human 5HT2B receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | F | 7.8 | pEC50 | 15.85 | nM | EC50 | J Med Chem (2008) 51: 305-313 [PMID:18095642] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Agonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as intracellular IP3 accumulation | F | 7.6 | pEC50 | 25.12 | nM | EC50 | J Med Chem (2008) 51: 305-313 [PMID:18095642] |
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]
