ChEMBL ligand: CHEMBL654 (6-azamianserin, Avanza, Mirataz, Mirtazapin, Mirtazapina, Mirtazapine, Mirtazapine anhydrous, Norset, ORG 3770, ORG-3770, Promyrtil, Remeron, Remeron soltab, Rexer, Zispin)
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] 5-HT1A receptor/5-hydroxytryptamine receptor 1A in Rat [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327] There should be some charts here, you may need to enable JavaScript!
5-HT2A receptor/5-hydroxytryptamine receptor 2A in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] 5-HT2A receptor/5-hydroxytryptamine receptor 2A in Rat [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842] There should be some charts here, you may need to enable JavaScript!
5-HT2C receptor/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] There should be some charts here, you may need to enable JavaScript!
5-HT3A/5-hydroxytryptamine receptor 3A in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] There should be some charts here, you may need to enable JavaScript!
5-HT7 receptor/5-hydroxytryptamine receptor 7 in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] There should be some charts here, you may need to enable JavaScript!
α1A-adrenoceptor/Alpha-1A adrenergic receptor in Human [ChEMBL: CHEMBL229] [GtoPdb: 22] [UniProtKB: P35348] There should be some charts here, you may need to enable JavaScript!
α2A-adrenoceptor/Alpha-2A adrenergic receptor in Human [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913] There should be some charts here, you may need to enable JavaScript!
α2B-adrenoceptor/Alpha-2B adrenergic receptor in Human [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089] There should be some charts here, you may need to enable JavaScript!
α2C-adrenoceptor/Alpha-2C adrenergic receptor in Human [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825] There should be some charts here, you may need to enable JavaScript!
D1 receptor/D(1A) dopamine receptor in Rat [ChEMBL: CHEMBL265] [GtoPdb: 214] [UniProtKB: P18901] There should be some charts here, you may need to enable JavaScript!
D2 receptor/D(2) dopamine receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] D2 receptor/D(2) dopamine receptor in Rat [ChEMBL: CHEMBL339] [GtoPdb: 215] [UniProtKB: P61169] There should be some charts here, you may need to enable JavaScript!
D3 receptor/D(3) dopamine receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] There should be some charts here, you may need to enable JavaScript!
D4 receptor/D(4) dopamine receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] There should be some charts here, you may need to enable JavaScript!
H1 receptor/Histamine H1 receptor in Human [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367] There should be some charts here, you may need to enable JavaScript!
Norepinephrine transporter in Rat [ChEMBL: CHEMBL304] [UniProtKB: Q9WTR4] There should be some charts here, you may need to enable JavaScript!
DAT/Sodium-dependent dopamine transporter in Rat [ChEMBL: CHEMBL338] [GtoPdb: 927] [UniProtKB: P23977] There should be some charts here, you may need to enable JavaScript!
SERT/Sodium-dependent serotonin transporter in Rat [ChEMBL: CHEMBL313] [GtoPdb: 928] [UniProtKB: P31652] 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
5-HT1A receptor/5-hydroxytryptamine receptor 1A 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/5-hydroxytryptamine receptor 1A 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2C 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/5-hydroxytryptamine receptor 2C 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/5-hydroxytryptamine receptor 3A 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/5-hydroxytryptamine receptor 7 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]
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/D(1A) dopamine 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/D(2) dopamine 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/D(2) dopamine 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/D(3) dopamine 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/D(4) dopamine 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]
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]
DAT/Sodium-dependent 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]
SERT/Sodium-dependent 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 36:

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]