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 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]
