mirtazapine [Ligand Id: 7241] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL654 (Mirtazapine, Remeron, ORG 3770, ORG-3770, Remeron soltab, Zispin)
  • α1A-adrenoceptor/Alpha-1a adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348]
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  • α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
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  • α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
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  • α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
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  • D1 receptor/Dopamine D1 receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
  • D2 receptor/Dopamine D2 receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
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  • Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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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]
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]
GtoPdb Inhibition of [3H]rauwolscine binding. - 7.7 pKi 20 nM Ki J Med Chem (2005) 48: 1709-12 [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]
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]
GtoPdb - - 6.7 pIC50 223.87 nM IC50 Bioorg Med Chem Lett (2000) 10: 71-4 [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. - 7.74 pKi 18 nM Ki J Med Chem (2005) 48: 1709-12 [PMID:15771415]
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 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]