R(-)amphetamine [Ligand Id: 2146] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL19393 (Amfetamine, (r)-, Amphetamine l-form, l-Amphetamine, Levamfetamine)
  • sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
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  • Trace amine-associated receptor 1 in Rhesus macaque [ChEMBL: CHEMBL1926495] [UniProtKB: Q8HZ64]
  • TA1 receptor/Trace amine-associated receptor 1 in Human [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0]
  • TA1 receptor/Trace amine-associated receptor 1 in Mouse [ChEMBL: CHEMBL4908] [GtoPdb: 364] [UniProtKB: Q923Y8]
  • TA1 receptor/Trace amine-associated receptor 1 in Rat [ChEMBL: CHEMBL3833] [GtoPdb: 364] [UniProtKB: Q923Y9]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL Binding affinity towards sigma opioid receptor in guinea pig cerebral homogenate using [3H]DTG as radioligand B 4.33 pKi 46400 nM Ki J Med Chem (1991) 34: 1094-1098 [PMID:1848295]
Trace amine-associated receptor 1 in Rhesus macaque (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1926495] [UniProtKB: Q8HZ64]
ChEMBL Activation of rhesus monkey TAAR1 expressed in RD-HGA16 cells co-expressing Gq protein assessed as cAMP accumulation by fluorescence plate reader F 5.73 pEC50 1860 nM EC50 Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049]
TA1 receptor/Trace amine-associated receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0]
ChEMBL Activation of human TAAR1 expressed in Syrian hamster AV12-664 cells co-expressing GalphaS protein assessed as accumulation of cAMP after 30 mins using cAMP XS EA/CL as substrate by luminescence method in presence of RX821002 and alprenolol F 5.77 pEC50 1700 nM EC50 Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049]
ChEMBL Activation of C-terminal HA epitope tagged human TAAR1 expressed in RD-HGA16 cells co-expressing Gq protein, Galpha16 by cAMP accumulation assay F 5.89 pEC50 1300 nM EC50 Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049]
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 6.04 pEC50 920 nM EC50 Bioorg Med Chem (2008) 16: 7415-7423 [PMID:18602830]
GtoPdb - - 6.2 pEC50 600 nM EC50 Bioorg Med Chem (2011) 19: 7044-8 [PMID:22037049]
GtoPdb - - 6.6 pEC50 - - - Mol Pharmacol (2008) 74: 585-594 [PMID:18524885]
ChEMBL Activation of human TAAR1 expressed in human HEK293T cells assessed as cAMP accumulation after 10 mins by BRET assay F 6.6 pEC50 250 nM EC50 Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049]
TA1 receptor/Trace amine-associated receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4908] [GtoPdb: 364] [UniProtKB: Q923Y8]
ChEMBL Activation of mouse TAAR1 expressed in human HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by liquid scintillation counting F 5.3 pEC50 4960 nM EC50 Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049]
ChEMBL Activation of mouse wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay F 6.1 pEC50 785.5 nM EC50 J Med Chem (2014) 57: 378-390 [PMID:24354319]
ChEMBL Activation of mouse TAAR1 transmembrane domain 6 Thr268(6.55)Met mutant expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay F 6.92 pEC50 121 nM EC50 J Med Chem (2014) 57: 378-390 [PMID:24354319]
ChEMBL Activation of mouse TAAR1 transmembrane domain 7 Tyr287(7.39)Asn mutant expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay F 6.98 pEC50 104.5 nM EC50 J Med Chem (2014) 57: 378-390 [PMID:24354319]
ChEMBL Activation of mouse TAAR1 expressed in human HEK293 cells assessed as accumulation of cAMP after 15 mins F 7.19 pEC50 65 nM EC50 Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049]
GtoPdb - - 7.2 pEC50 - - - J Pharmacol Exp Ther (2007) 321: 178-86 [PMID:17218486];
Genes Brain Behav (2007) 6: 628-39 [PMID:17212650]
TA1 receptor/Trace amine-associated receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3833] [GtoPdb: 364] [UniProtKB: Q923Y9]
ChEMBL Activation of rat TAAR1 expressed in Syrian hamster AV12-664 cells assessed as accumulation of cAMP after 30 mins using cAMP XS EA/CL as substrate by luminescence method F 5.85 pEC50 1400 nM EC50 Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049]
ChEMBL Activation of rat TAAR1 expressed in HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by liquid scintillation counting F 6.55 pEC50 280 nM EC50 Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049]
ChEMBL Activation of rat TAAR1 transmembrane domain 6 Met268(6.55)Thr mutant expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay F 6.67 pEC50 214.4 nM EC50 J Med Chem (2014) 57: 378-390 [PMID:24354319]
ChEMBL Activation of rat TAAR1 expressed in HEK293 cells assessed as accumulation of [3H]cAMP after 1 hr by competitive binding assay F 6.68 pEC50 210 nM EC50 Bioorg Med Chem (2011) 19: 7044-7048 [PMID:22037049]
GtoPdb - - 6.7 pEC50 - - - J Pharmacol Exp Ther (2007) 321: 178-86 [PMID:17218486];
Mol Pharmacol (2001) 60: 1181-8 [PMID:11723224]
ChEMBL Activation of rat TAAR1 transmembrane domain 7 Asn287(7.39)Tyr mutant expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay F 6.77 pEC50 169.9 nM EC50 J Med Chem (2014) 57: 378-390 [PMID:24354319]
ChEMBL Activation of rat wild type TAAR1 expressed in HEK293 cells assessed as stimulation of cAMP production after 1 hr by chemiluminescent assay F 7.47 pEC50 33.9 nM EC50 J Med Chem (2014) 57: 378-390 [PMID:24354319]

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]