HTL6641 [Ligand Id: 11695] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3740099 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Inhibition of human ERG | B | 5 | pIC50 | >10000 | nM | IC50 | Medchemcomm (2015) 6: 947-955 |
| OX1 receptor/Orexin receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5113] [GtoPdb: 321] [UniProtKB: O43613] | ||||||||
| GtoPdb | - | - | 7.5 | 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 | 7.5 | pKi | 31.62 | nM | Ki | J Med Chem (2020) 63: 1528-1543 [PMID:31860301] |
| GtoPdb | - | - | 7.7 | pKi | 20 | nM | Ki | Medicinal Chemistry Communications (2015) 6: 947-955 |
| 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 orexin receptor-1 (unknown origin) after 90 mins | B | 7.7 | pKi | 19.95 | nM | Ki | Medchemcomm (2015) 6: 947-955 |
| 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 | 8.3 | pKi | 5.01 | nM | Ki | J Med Chem (2020) 63: 1528-1543 [PMID:31860301] |
| GtoPdb | - | - | 8.3 | pKi | - | - | - | J Med Chem (2020) 63: 1528-1543 [PMID:31860301] |
| ChEMBL | Displacement of [3H]EMPA from human orexin receptor-2 expressed in HEK293 cells after 90 mins by scintillation counting | B | 8.6 | pKi | 2.51 | nM | Ki | Medchemcomm (2015) 6: 947-955 |
| GtoPdb | - | - | 8.6 | pKi | 2.5 | nM | Ki | Medicinal Chemistry Communications (2015) 6: 947-955 |
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]
