EPPTB [Ligand Id: 5457] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1669669 (Ro-5212773) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| TA1 receptor/Trace amine-associated receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5857] [GtoPdb: 364] [UniProtKB: Q96RJ0] | ||||||||
| ChEMBL | Inhibition of human TAAR1 | B | 5.3 | pKi | >5000 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1227-1231 [PMID:21237643] |
| GtoPdb | - | - | 5.1 | pIC50 | 7487 | nM | IC50 | Proc Natl Acad Sci USA (2009) 106: 20081-6 [PMID:19892733] |
| ChEMBL | Antagonist activity at human TAAR1 assessed as reversal of endogenous beta-PEA effect | F | 5.13 | pIC50 | 7490 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1227-1231 [PMID:21237643] |
| TA1 receptor/Trace amine-associated receptor 1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4908] [GtoPdb: 364] [UniProtKB: Q923Y8] | ||||||||
| GtoPdb | - | - | 9 | pKi | 0.9 | nM | Ki |
Bioorg Med Chem Lett (2011) 21: 1227-31 [PMID:21237643]; Proc Natl Acad Sci USA (2009) 106: 20081-6 [PMID:19892733] |
| ChEMBL | Inhibition of mouse TAAR1 | B | 9.05 | pKi | 0.9 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1227-1231 [PMID:21237643] |
| ChEMBL | Antagonist activity at mouse TAAR1 assessed as reversal of endogenous beta-PEA effect | F | 7.55 | pIC50 | 28 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1227-1231 [PMID:21237643] |
| GtoPdb | - | - | 7.7 | pIC50 | 19 | nM | IC50 | Proc Natl Acad Sci USA (2009) 106: 20081-6 [PMID:19892733] |
| TA1 receptor/Trace amine-associated receptor 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3833] [GtoPdb: 364] [UniProtKB: Q923Y9] | ||||||||
| GtoPdb | - | - | 6 | pKi | 942 | nM | Ki | Proc Natl Acad Sci USA (2009) 106: 20081-6 [PMID:19892733] |
| ChEMBL | Inhibition of rat TAAR1 | B | 6.03 | pKi | 942 | nM | Ki | Bioorg Med Chem Lett (2011) 21: 1227-1231 [PMID:21237643] |
| ChEMBL | Antagonist activity at rat TAAR1 assessed as reversal of endogenous beta-PEA effect | F | 5.34 | pIC50 | 4540 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 1227-1231 [PMID:21237643] |
| GtoPdb | - | - | 5.4 | pIC50 | 4500 | nM | IC50 | Proc Natl Acad Sci USA (2009) 106: 20081-6 [PMID:19892733] |
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]
