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 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]
