amphetamine [Ligand Id: 4804] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL405 (Adzenys er, Adzenys xr-odt, Amfetamin, Amfetamine, Amphetamine, Amphetamine, dl-, Amphetamine resin complex, Dyanavel, Dyanavel xr, Norephedrane, NSC-27159) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Inhibition of [3H]dopamine uptake at dopamine transporter expressed in rat striatal homogenate after 5 mins by scintillation counting analysis | B | 6.02 | pIC50 | 960 | nM | IC50 | J Med Chem (1976) 19: 725-727 [PMID:1271416] |
| NET/Norepinephrine transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2370] [GtoPdb: 926] [UniProtKB: O55192] | ||||||||
| ChEMBL | Inhibition of noradrenaline transporter in NMRI albino mouse brain assessed as [3H]NA accumulation in hypothalamus after 5 mins | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (1978) 21: 78-82 [PMID:22757] |
| 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 | 5 | pKi | >10000 | nM | Ki | J Med Chem (2000) 43: 3074-3084 [PMID:10956215] |
| ChEMBL | Displacement of [3H]ketanserin from rat 5HT2A expressed in mouse NIH/3T3 cell membranes after 30 mins by scintillation counting method | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2017) 60: 2605-2628 [PMID:28244748] |
| 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL323] [GtoPdb: 7] [UniProtKB: P30994] | ||||||||
| ChEMBL | Affinity against serotonergic receptor in the isolated rat stomach fundus | B | 5.27 | pKd | 5370.32 | 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 | Displacement of [3H]mesulergine from A9 cells stably expressing rat 5-hydroxytryptamine 2C receptor | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2000) 43: 3074-3084 [PMID:10956215] |
| ChEMBL | Compound was tested for binding affinity towards 5-hydroxytryptamine 1C receptor from frontal cortical regions of male Sprague-Dawley rat homogenates, using [3H]mesulergine as radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (1992) 35: 734-740 [PMID:1542100] |
| SERT/Serotonin transporter in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4642] [GtoPdb: 928] [UniProtKB: Q60857] | ||||||||
| ChEMBL | Inhibition of 5-HT transporter in NMRI albino mouse brain assessed as [3H]5-HT accumulation in hypothalamus after 5 mins | B | 4.35 | pIC50 | 45000 | nM | IC50 | J Med Chem (1978) 21: 78-82 [PMID:22757] |
| sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3602] [GtoPdb: 2552] [UniProtKB: Q9R0C9] | ||||||||
| ChEMBL | Binding affinity towards sigma opioid receptor was determined in rat cerebral homogenate using [3H]haloperidol as radioligand | B | 4.3 | pKi | >50000 | nM | Ki | J Med Chem (1991) 34: 1094-1098 [PMID:1848295] |
| Organic cation transporter 3/Solute carrier family 22 member 3 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770033] [GtoPdb: 1021] [UniProtKB: O88446] | ||||||||
| ChEMBL | TP_TRANSPORTER: inhibition of MPP+ uptake (MPP+: 1 uM) in OCT3-expressing HRPE cells | F | 4.38 | pIC50 | 42000 | nM | IC50 | J Biol Chem (1998) 273: 32776-32786 [PMID:9830022] |
| Transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6184] [UniProtKB: Q63380] | ||||||||
| ChEMBL | Inhibition of [3H]norepinephrine uptake at NET expressed in rat hypothalamic homogenate containing synaptosomes after 5 mins by scintillation counting analysis | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (1976) 19: 725-727 [PMID:1271416] |
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]
