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ChEMBL ligand: CHEMBL133455 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] | ||||||||
ChEMBL | Inhibitory constant against alpha-1A receptor using [3H]-7-MeO prazosin radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] | ||||||||
ChEMBL | Inhibitory constant against Alpha-1B adrenergic radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
ChEMBL | Inhibitory concentration required against Alpha-2A adrenergic receptor using [3H]clonidine radioligand | B | 4.72 | pIC50 | 19000 | nM | IC50 | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL266] [GtoPdb: 26] [UniProtKB: P19328] | ||||||||
ChEMBL | Inhibitory constant against Alpha-2B adrenergic receptor using [3H]MK-912 radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
ChEMBL | Inhibitory concentration required against Alpha-2A adrenergic receptor using [3H]clonidine radioligand | B | 4.85 | pIC50 | 14000 | nM | IC50 | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
NET/Norepinephrine transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL222] [GtoPdb: 926] [UniProtKB: P23975] | ||||||||
ChEMBL | Inhibitory constant against norepinephrine transporter receptor using [3H]radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | In vitro inhibitory concentration required against [3H]8-OH-DPAT binding to cloned human 5-hydroxytryptamine 1A receptor | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] | ||||||||
ChEMBL | Inhibitory constant against 5-hydroxytryptamine 1B receptor using with [125I]- cyanopindolol radioligand | B | 5.48 | pKi | 3300 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] | ||||||||
ChEMBL | Inhibitory constant against human 5-hydroxytryptamine 5A receptor using [3H]LSD radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | Inhibitory constant against cloned human 5-hydroxytryptamine 2A receptor using with [125I]- DOI radioligand | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
GtoPdb | - | - | 8.7 | pKi | - | - | - | J Med Chem (2003) 46: 4188-95 [PMID:12954071] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
ChEMBL | In vitro inhibitory constant against [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex | B | 9.7 | pKi | 0.2 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
ChEMBL | In vitro inhibition of [125I]DOI binding to 5-hydroxytryptamine 2A receptor in rat cerebral cortex | B | 9.3 | pIC50 | 0.5 | nM | IC50 | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
ChEMBL | In vitro relative agonist activity against 5-hydroxytryptamine 2A using PI assay in rat vascular smooth muscle cells | F | 7.1 | pEC50 | 80.1 | nM | EC50 | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
ChEMBL | Inhibitory constant against cloned human 5-hydroxytryptamine 2B receptor using with [125I]- DOI radioligand | B | 8.28 | pKi | 5.3 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
GtoPdb | - | - | 8.3 | pKi | - | - | - | J Med Chem (2003) 46: 4188-95 [PMID:12954071] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Inhibitory constant against cloned human 5-hydroxytryptamine 2C receptor using with [125I]- DOI radioligand | B | 8.47 | pKi | 3.4 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
GtoPdb | - | - | 8.5 | pKi | - | - | - | J Med Chem (2003) 46: 4188-95 [PMID:12954071] |
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
ChEMBL | Inhibitory constant against 5-hydroxytryptamine 3 receptor using [3H]GR-65630 radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
ChEMBL | Inhibitory constant against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 radioligand | B | 5.77 | pKi | 1700 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] | ||||||||
ChEMBL | Inhibitory constant against human 5-hydroxytryptamine 1D receptor using [3H]5-CT radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] | ||||||||
ChEMBL | Inhibitory constant against human 5-hydroxytryptamine 6 receptor using [3H]LSD radioligand | B | 5.66 | pKi | 2200 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] | ||||||||
ChEMBL | Inhibitory constant against human serotonin transporter using [3H]N-Me-citalopram radioligand | B | 5 | pKi | >10000 | nM | Ki | J Med Chem (2003) 46: 4188-4195 [PMID:12954071] |
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]