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, Levanfetamina)
  • 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 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]