2C-B [Ligand Id: 13549] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL292821
  • 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 Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • TA1 receptor/Trace amine-associated receptor 1 in Human [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0]
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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 Affinity against 5-hydroxytryptamine 2A receptor (K) labeled with [3H]ketanserin. B 7.47 pKi 34 nM Ki J Med Chem (1994) 37: 1929-1935 [PMID:8027974]
ChEMBL Affinity against 5-hydroxytryptamine 2A receptor (D) labeled with [125I]DOI. B 9 pKi 1 nM Ki J Med Chem (1994) 37: 1929-1935 [PMID:8027974]
GtoPdb - - 9.18 pKi 0.66 nM Ki J Med Chem (2006) 49: 5794-803 [PMID:16970404]
ChEMBL Displacement of (+/-)-[125I]DOI from human cloned 5HT2A receptor B 9.18 pKi 0.66 nM Ki J Med Chem (2006) 49: 5794-5803 [PMID:16970404]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
ChEMBL Displacement of [3H]ketanserin from NIH3T3 cells stably expressing rat 5-hydroxytryptamine 2A receptor B 7.8 pKi 16 nM Ki J Med Chem (2000) 43: 3074-3084 [PMID:10956215]
ChEMBL Displacement of (+/-)-[125I]DOI from rat cloned 5HT2A receptor B 9.06 pKi 0.88 nM Ki J Med Chem (2006) 49: 5794-5803 [PMID:16970404]
ChEMBL Activity at rat 5HT2A receptor expressed in NIH3T3 cells assessed as stimulation of phospholipase C-mediated IP production F 7.57 pEC50 27 nM EC50 J Med Chem (2006) 49: 5794-5803 [PMID:16970404]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL Displacement of [3H]mesulergine from A9 cells stably expressing rat 5-hydroxytryptamine 2C receptor B 6.72 pKi 190 nM Ki J Med Chem (2000) 43: 3074-3084 [PMID:10956215]
ChEMBL Affinity against 5-hydroxytryptamine 2C receptor in J1 cells transfected with the rat 5-HT2C gene labeled with [3H]mesulergine. B 7.44 pKi 36 nM Ki J Med Chem (1994) 37: 1929-1935 [PMID:8027974]
ChEMBL Binding affinity towards 5-hydroxytryptamine 1C receptor from frontal cortical regions of male Sprague-Dawley rat homogenates, using [3H]mesulergine as radioligand B 7.44 pKi 36 nM Ki J Med Chem (1992) 35: 734-740 [PMID:1542100]
TA1 receptor/Trace amine-associated receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0]
ChEMBL Agonist activity at human trace amine associated receptor 1 expressed in RD-HGA16 CHO-K1 cells coexpressed with Galpha16 protein assessed as internal calcium mobilization by calcium 3 assay F 5.14 pEC50 7190 nM EC50 Bioorg Med Chem (2008) 16: 7415-7423 [PMID:18602830]

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]