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ChEMBL ligand: CHEMBL19393 (Amfetamine, (r)-, Amphetamine l-form, l-Amphetamine, Levamfetamine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]