EMPA [Ligand Id: 4037] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL2385132 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| OX1 receptor/Orexin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5113] [GtoPdb: 321] [UniProtKB: O43613] | ||||||||
| GtoPdb | - | - | 5.34 | pKi | 4533 | nM | Ki | Mol Pharmacol (2009) 76: 618-31 [PMID:19542319] |
| ChEMBL | Displacement of [3H]-SB67404 from human orexin 1 receptor expressed in CHO cells incubated for 2 hrs by whole cell radioligand binding assay | B | 5.35 | pKi | 4466.84 | nM | Ki | J Med Chem (2020) 63: 11045-11053 [PMID:32977721] |
| GtoPdb | - | - | 6 | pKi | - | - | - | J Med Chem (2020) 63: 1528-1543 [PMID:31860301] |
| ChEMBL | Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX1 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liquid scintillation counting method | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (2020) 63: 1528-1543 [PMID:31860301] |
| ChEMBL | Binding affinity to orexin receptor 1 (unknown origin) | B | 6.05 | pKi | 900 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4761-4769 [PMID:23891187] |
| GtoPdb | [3H]SB 674042 displacement by EMPA from HEK293-hOX1 membrane preparations | - | 6.05 | pKi | 900 | nM | Ki | Br J Pharmacol (2009) 156: 1326-41 [PMID:19751316] |
| ChEMBL | Antagonist activity at OX1 receptor (unknown origin) | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3389-3392 [PMID:23601709] |
| OX2 receptor/Orexin receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4792] [GtoPdb: 322] [UniProtKB: O43614] | ||||||||
| ChEMBL | Displacement of [3H]4-(2,6-Difluoro-4-methoxybenzyl)-2-(5,6-dimethoxypyridin-3-yl)-2H-1,2,4-benzothiadiazin-3(4H)-one 1,1-dioxide from human wild-type OX2 receptor expressed in baculovirus infected Sf21 insect cell membranes measured after 90 mins by liquid scintillation counting method | B | 6 | pKi | 1000 | nM | Ki | J Med Chem (2020) 63: 1528-1543 [PMID:31860301] |
| ChEMBL | Antagonist activity at OX2 receptor (unknown origin) | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 3389-3392 [PMID:23601709] |
| ChEMBL | Binding affinity to orexin receptor 2 (unknown origin) | B | 8.96 | pKi | 1.1 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 4761-4769 [PMID:23891187] |
| GtoPdb | - | - | 9.2 | pKi | - | - | - |
Br J Pharmacol (2009) 156: 1326-41 [PMID:19751316]; Mol Pharmacol (2009) 76: 618-31 [PMID:19542319]; J Med Chem (2020) 63: 1528-1543 [PMID:31860301] |
| ChEMBL | Antagonist activity at OX2 receptor (unknown origin) | B | 8.7 | pIC50 | 2 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3389-3392 [PMID:23601709] |
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]
