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] |
| ChEMBL | Antagonist activity at human OX1R expressed in CHO/dhfr- cells assessed as inhibition of orexin A-induced intracellular Ca2+ mobilization preincubated for 25 mins followed by orexin A addition by FLIPR assay | F | 5 | pIC50 | >10000 | nM | IC50 | RSC Med Chem (2024) 15: 344-354 [PMID:38283232] |
| 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 human OX2R expressed in CHO/dhfr- cells assessed as inhibition of orexin B-induced intracellular Ca2+ mobilization preincubated for 25 mins followed by orexin B addition by FLIPR assay | F | 8.1 | pIC50 | 8 | nM | IC50 | RSC Med Chem (2024) 15: 344-354 [PMID:38283232] |
| 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 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]
