mirtazapine [Ligand Id: 7241] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL654 (6-azamianserin, Avanza, Mirataz, Mirtazapin, Mirtazapine, Mirtazapine anhydrous, Norset, ORG 3770, ORG-3770, Promyrtil, Remeron, Remeron soltab, Rexer, Zispin) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] | ||||||||
| ChEMBL | Binding affinity at human Alpha-1A adrenergic receptor in CHO cells uby [3H]prazosin (0.25 nM) displacement. | B | 5.5 | pIC50 | 3162.28 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 71-74 [PMID:10636247] |
| α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] | ||||||||
| GtoPdb | Inhibition of [3H]rauwolscine binding. | - | 7.1 | pKi | - | - | - |
J Med Chem (2005) 48: 1709-12 [PMID:15771415]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | Inhibition of [3H]rauwolscine binding to Alpha-2A adrenergic receptor | B | 7.7 | pKi | 20 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
| ChEMBL | Binding affinity at human Alpha-2A adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement. | B | 7.07 | pIC50 | 85.11 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 71-74 [PMID:10636247] |
| GtoPdb | - | - | 7.1 | pIC50 | 85.11 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 71-4 [PMID:10636247] |
| α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] | ||||||||
| GtoPdb | - | - | 6.7 | pKi | - | - | - |
Bioorg Med Chem Lett (2000) 10: 71-4 [PMID:10636247]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | Binding affinity at human Alpha-2B adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement. | B | 6.65 | pIC50 | 223.87 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 71-74 [PMID:10636247] |
| α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] | ||||||||
| GtoPdb | Inhibition of [3H]rauwolscine binding. | - | 7.7 | pKi | - | - | - |
J Med Chem (2005) 48: 1709-12 [PMID:15771415]; Pharmacol Res Perspect (2022) 10: e00936 [PMID:35224877] |
| ChEMBL | Inhibition of [3H]rauwolscine binding to Alpha-2C adrenergic receptor | B | 7.74 | pKi | 18 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
| ChEMBL | Binding affinity at human Alpha-2C adrenergic receptor in CHO cells by [3H]rauwolscine (1 nM) displacement. | B | 6.7 | pIC50 | 199.53 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 71-74 [PMID:10636247] |
| GtoPdb | - | - | 6.7 | pIC50 | 199.53 | nM | IC50 | Bioorg Med Chem Lett (2000) 10: 71-4 [PMID:10636247] |
| D1 receptor/Dopamine D1 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] | ||||||||
| ChEMBL | Inhibition of [3H]SCH-23390 binding to rat Dopamine receptor D1 | B | 5.38 | pKi | 4167 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
| D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
| ChEMBL | Inhibition of [3H]-spiperone binding to human Dopamine receptor D2 | B | 5.26 | pKi | >5454 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
| D2 receptor/Dopamine D2 receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] | ||||||||
| ChEMBL | The binding affinity at the Dopamine receptor D2 determined using [3H]spiperone | B | 5.84 | pKi | 1460 | nM | Ki | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
| D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] | ||||||||
| ChEMBL | Inhibition of [125I]iodosulpiride binding to human Dopamine receptor D3 | B | 5.24 | pKi | 5723 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
| ChEMBL | The binding affinity at the Dopamine receptor D3 determined using [3H]spiperone | B | 7.7 | pKi | >20 | nM | Ki | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
| D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] | ||||||||
| ChEMBL | The binding affinity at the Dopamine receptor D4 determined using [3H]YM-09151-2 | B | 7.6 | pKi | >25 | nM | Ki | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
| DAT/Dopamine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] | ||||||||
| ChEMBL | Binding affinity against dopamine transporter (DAT) by displacement of [3H]WIN-35428 in male wistar rats | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] | ||||||||
| ChEMBL | Inhibition of [3H]pyrilamine binding to human Histamine H1 receptor | B | 8.8 | pKi | 1.6 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
| Norepinephrine transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] | ||||||||
| ChEMBL | Inhibition of [3H]nisoxetine binding to rat Norepinephrine transporter | B | 5.79 | pKi | 1640 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
| ChEMBL | Binding affinity against norepinephrine transporter (NET) by displacement of [3H]nisoxetine in male wistar rats | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| ChEMBL | The binding affinity at the Norepinephrine transporter reuptake sites determined using competition binding assay | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
| ChEMBL | Binding affinity to 5HT1A receptor | B | 5.3 | pKd | 5011.87 | nM | Kd | J Med Chem (2009) 52: 6107-6125 [PMID:19754201] |
| ChEMBL | The binding affinity at the 5-hydroxytryptamine 1A receptor determined using [3H]5-CT | B | 7.74 | pKi | >18 | nM | Ki | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
| ChEMBL | Binding affinity to human 5HT1A receptor | B | 7.74 | pKi | 18 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 126679-126679 [PMID:31537425] |
| 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 1A receptor (5-HT1A) by displacement of [3H]8-OH-DPAT from rat hippocampus membranes | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
| GtoPdb | - | - | 7.16 | pKi | 69 | nM | Ki | J Med Chem (2005) 48: 1709-12 [PMID:15771415] |
| ChEMBL | Inhibition of [125I]R91150 binding to human 5-hydroxytryptamine 2A receptor | B | 7.16 | pKi | 69 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
| ChEMBL | Binding affinity to human 5HT2A receptor | B | 8.09 | pKi | 8.2 | nM | Ki | Bioorg Med Chem Lett (2019) 29: 126679-126679 [PMID:31537425] |
| 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] | ||||||||
| ChEMBL | Binding affinity against 5-hydroxytryptamine 2A receptor by displacement of [3H]ketanserin from rat prefrontal cerebral cortex mambranes | B | 7.83 | pKi | 14.8 | nM | Ki | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| ChEMBL | The binding affinity at 5-hydroxytryptamine 2A receptor was determined using [3H]ketanserin | B | 8.7 | pKi | 2 | nM | Ki | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
| ChEMBL | Inhibition of [3H]mesulergine binding to human 5-hydroxytryptamine 2C receptor | B | 7.41 | pKi | 39 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
| GtoPdb | - | - | 7.41 | pKi | 39 | nM | Ki | J Med Chem (2005) 48: 1709-12 [PMID:15771415] |
| 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] | ||||||||
| ChEMBL | The binding affinity at 5-hydroxytryptamine 2C receptor was determined using [3H]mesulergine | B | 8.26 | pKi | 5.5 | nM | Ki | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
| 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] | ||||||||
| ChEMBL | Displacement of [3H]GR65630 from human 5-HT3A receptor expressed in HEK293 cells by liquid scintillation counting analysis | B | 5.54 | pKi | 2900 | nM | Ki | Bioorg Med Chem Lett (2013) 23: 5945-5948 [PMID:24035337] |
| 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
| ChEMBL | Inhibition of [3H]5-HT binding to human 5-hydroxytryptamine 7 receptor | B | 6.58 | pKi | 265 | nM | Ki | J Med Chem (2005) 48: 1709-1712 [PMID:15771415] |
| SERT/Serotonin transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] | ||||||||
| ChEMBL | Binding affinity against serotonin transporter (SERT) by displacement of [3H]paroxetine in male wistar rats | B | 6 | pIC50 | >1000 | nM | IC50 | J Med Chem (2003) 46: 5512-5532 [PMID:14640559] |
| ChEMBL | The binding affinity at the 5-HT reuptake sites determined using competition binding assay | B | 7 | pIC50 | >100 | nM | IC50 | J Med Chem (2002) 45: 3280-3285 [PMID:12109911] |
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]
