brolamfetamine [Ligand Id: 163] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL6607 (Brolamfetamine, Bromo-dma, J275.083J) |
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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] | ||||||||
| 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] |
| GtoPdb | - | - | 9.2 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 1-6 [PMID:9933142] |
| 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] |
| GtoPdb | - | - | 7.8 | pKi | - | - | - | J Pharmacol Exp Ther (1998) 286: 85-90 [PMID:9655845] |
| 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 in Human [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
| GtoPdb | - | - | 7.6 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 1-6 [PMID:9933142] |
| 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 in Human [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| GtoPdb | - | - | 8.9 | pKi | - | - | - |
Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 1-6 [PMID:9933142]; Synapse (2000) 35: 144-150 [PMID:10611640] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| GtoPdb | - | - | 6.6 | pKi | - | - | - | J Neurochem (1997) 69: 1138-44 [PMID:9282936] |
| 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 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]
