glemanserin [Ligand Id: 186] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL18972 (Glemanserin, MDL 11,939, MDL-11939, MDL-11,939)
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
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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]
GtoPdb - - 7.6 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL Binding affinity for human 5-hydroxytryptamine 2A receptor B 8.6 pKi 2.5 nM Ki J. Med. Chem. (2001) 44: 477-501 [PMID:11170639]
ChEMBL Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay F 8.6 pKi 2.5 nM Ki J. Med. Chem. (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Antagonist activity at human 5HT2A receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay F 8.61 pKi 2.46 nM Ki J. Med. Chem. (2013) 56: 1211-1227 [PMID:23301527]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Binding affinity against 5-hydroxytryptamine 2A receptor B 8.6 pKi 2.5 nM Ki J. Med. Chem. (1995) 38: 1196-1202 [PMID:7707322]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay F 5 pKi 10000 nM Ki J. Med. Chem. (2013) 56: 1211-1227 [PMID:23301527]
ChEMBL Antagonist activity at human 5HT2C receptor expressed in HEK293 cells assessed as inhibition of 5HT-induced intracellular calcium release measured for 90 secs by fluorescence assay F 5 pKi 10000 nM Ki J. Med. Chem. (2013) 56: 1211-1227 [PMID:23301527]
GtoPdb - - 6.6 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL Binding affinity against 5-hydroxytryptamine 2C receptor B 6.08 pKi 830 nM Ki J. Med. Chem. (1995) 38: 1196-1202 [PMID:7707322]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 5.5 pKi - - - Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]

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, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]