[3H](+)DOB [Ligand Id: 155] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL6607 (Brolamfetamine, Bromo-dma, J275.083J)
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 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-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396]
ChEMBL Inhibitory concentration against monoamine oxidase A in rat brain mitochondrial suspension B 4 pIC50 100000 nM IC50 J Med Chem (2005) 48: 2407-2419 [PMID:15801832]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL Binding affinity towards rat hippocampal 5-hydroxytryptamine 1A receptor using [3H]8-OH-DPAT as radioligand B 8.21 pKi 6.1 nM Ki J Med Chem (1996) 39: 2953-2961 [PMID:8709129]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb - - 9.1 pKd - - - Mol Pharmacol (2001) 60: 690-699 [PMID:11562430];
Biochem Pharmacol (1996) 51: 71-6 [PMID:8534270]
ChEMBL The compound evaluated for its affinity against 5-hydroxytryptamine 2A receptor B 7.39 pKi 41 nM Ki J Med Chem (1994) 37: 1929-1935 [PMID:8027974]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor expressed in NIH3T3 cells B 7.39 pKi 41 nM Ki J Med Chem (2008) 51: 6808-6828 [PMID:18847250]
ChEMBL Displacement of [125I]DOI from recombinant human 5HT2A expressed in Syrian hamster AV12 cell membranes B 9.22 pKi 0.6 nM Ki J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
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 5HT2A in Sprague-Dawley rat cortex membranes measured after 15 mins B 7.39 pKi 41 nM Ki J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
ChEMBL Binding affinity towards 5-hydroxytryptamine 2A receptor sites by using [3H]ketanserin as radioligand B 7.39 pKi 41 nM Ki Bioorg Med Chem Lett (2003) 13: 2565-2568 [PMID:12852967]
ChEMBL Binding affinity against rat 5-hydroxytryptamine 2A receptor using [3H]ketanserin as radioligand B 7.49 pKi 32 nM Ki J Med Chem (2001) 44: 3283-3291 [PMID:11563927]
ChEMBL Displacement of [3H]ketanserin from rat 5HT2A expressed in mouse NIH/3T3 cell membranes after 30 mins by scintillation counting method B 7.49 pKi 32 nM Ki J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
ChEMBL Displacement of [3H]ketanserin from NIH3T3 cells stably expressing rat 5-hydroxytryptamine 2A receptor B 7.49 pKi 32 nM Ki J Med Chem (2000) 43: 3074-3084 [PMID:10956215]
ChEMBL Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley rat brain by liquid scintillation spectroscopy B 7.66 pKi 22 nM Ki Bioorg Med Chem (2008) 16: 4661-4669 [PMID:18296055]
ChEMBL Binding affinity towards rat cortical 5-hydroxytryptamine 2A receptor using [3H]ketanserin as radioligand B 7.66 pKi 22 nM Ki J Med Chem (1996) 39: 2953-2961 [PMID:8709129]
ChEMBL Displacement of [3H]ketanserin from rat 5HT2A receptor expressed in mouse NIH3T3 cells B 7.89 pKi 13 nM Ki Bioorg Med Chem (2008) 16: 6242-6251 [PMID:18467103]
ChEMBL Binding affinity at cloned rat 5-hydroxytryptamine 2A receptor using [3H]DOB as radioligand B 8.66 pKi 2.2 nM Ki J Med Chem (2001) 44: 1003-1010 [PMID:11300881]
ChEMBL In vitro binding to 5-hydroxytryptamine 2A receptor using [125 I]-DOI B 8.66 pKi 2.2 nM Ki J Med Chem (2003) 46: 3526-3535 [PMID:12877591]
ChEMBL Displacement of [3H]DOB from 5HT2A in Sprague-Dawley rat cortex membranes measured after 15 mins by scintillation counting method B 9.1 pKi 0.8 nM Ki J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
ChEMBL Binding affinity for 5-HT2A serotonin receptor B 10 pKi 0.1 nM Ki J Med Chem (2004) 47: 6034-6041 [PMID:15537358]
ChEMBL Ability to stimulate phosphoinositide hydrolysis in NIH3T3 cells expressing the 5-hydroxytryptamine 2A receptor B 7.14 pEC50 72 nM EC50 J Med Chem (2001) 44: 1003-1010 [PMID:11300881]
ChEMBL Tested for its ability to activate phospholipase C by quantification of IP3 at cloned rat 5-hydroxytryptamine 2A receptor B 7.14 pEC50 72 nM EC50 J Med Chem (2003) 46: 3526-3535 [PMID:12877591]
ChEMBL Serotonin 5-HT2A receptor-mediated intracellular calcium [Ca2+] mobilization in rat A7r5 cells F 7.22 pEC50 60 nM EC50 J Med Chem (2004) 47: 6034-6041 [PMID:15537358]
ChEMBL Agonist activity at rat 5HT2A receptor expressed in mouse NIH3T3 cells assessed as stimulation of inositol phosphate accumulation F 7.66 pEC50 22 nM EC50 Bioorg Med Chem (2008) 16: 6242-6251 [PMID:18467103]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994]
ChEMBL Affinity against 5-hydroxytryptamine 2B receptor in the isolated rat stomach fundus B 7.35 pKd 44.67 nM Kd J Med Chem (1981) 24: 1414-1421 [PMID:7310818]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL The compound evaluated for its affinity against 5-hydroxytryptamine 2C receptor B 7.15 pKi 70 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 7.15 pKi 70 nM Ki J Med Chem (1992) 35: 734-740 [PMID:1542100]
ChEMBL Displacement of [3H]mesulergine from A9 cells stably expressing rat 5-hydroxytryptamine 2C receptor B 7.19 pKi 64 nM Ki J Med Chem (2000) 43: 3074-3084 [PMID:10956215]
ChEMBL Binding affinity at cloned rat 5-hydroxytryptamine 2C receptor using [3H]DOI as radioligand B 8.55 pKi 2.8 nM Ki J Med Chem (2001) 44: 1003-1010 [PMID:11300881]
ChEMBL In vitro binding to 5-hydroxytryptamine 2C receptor using [125 I]-DOI B 8.55 pKi 2.8 nM Ki J Med Chem (2003) 46: 3526-3535 [PMID:12877591]

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]