Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL133455 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
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 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]