ChEMBL ligand: CHEMBL621 (Desyrel, J10.767K, Trazodona, Trazodone, Trialodine, Trittico)
α1A-adrenoceptor/Alpha-1a adrenergic receptor in Rat [ChEMBL: CHEMBL319] [GtoPdb: 22] [UniProtKB: P43140] There should be some charts here, you may need to enable JavaScript!
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823] There should be some charts here, you may need to enable JavaScript!
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100] 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!
D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] There should be some charts here, you may need to enable JavaScript!
D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462] 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!
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] There should be some charts here, you may need to enable JavaScript!
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] There should be some charts here, you may need to enable JavaScript!
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] 5-HT2C receptor in Rat [GtoPdb: 8] [UniProtKB: P08909] There should be some charts here, you may need to enable JavaScript!
SERT/Serotonin transporter in Human [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645] There should be some charts here, you may need to enable JavaScript!
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] 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	DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)	B	7.33	pKi	47	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1A adrenergic receptor radioligand binding (ligand: prazosin)	B	6.93	pIC50	117	nM	IC50	DrugMatrix in vitro pharmacology data
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL315] [GtoPdb: 23] [UniProtKB: P15823]
ChEMBL	DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)	B	7.21	pKi	61	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1B adrenergic receptor radioligand binding (ligand: prazosin)	B	6.95	pIC50	111	nM	IC50	DrugMatrix in vitro pharmacology data
α1D-adrenoceptor/Alpha-1d adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL223] [GtoPdb: 24] [UniProtKB: P25100]
ChEMBL	DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)	B	6.89	pKi	130	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-1D adrenergic receptor radioligand binding (ligand: prazosin)	B	6.58	pIC50	265	nM	IC50	DrugMatrix in vitro pharmacology data
α2A-adrenoceptor/Alpha-2a adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1867] [GtoPdb: 25] [UniProtKB: P08913]
ChEMBL	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	B	6.47	pKi	341	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-2A adrenergic receptor radioligand binding (ligand: MK-912)	B	6.04	pIC50	909	nM	IC50	DrugMatrix in vitro pharmacology data
α2B-adrenoceptor/Alpha-2b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1942] [GtoPdb: 26] [UniProtKB: P18089]
ChEMBL	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	B	6.75	pKi	178	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Alpha-2B adrenergic receptor radioligand binding (ligand: Rauwolscine)	B	6.41	pIC50	389	nM	IC50	DrugMatrix in vitro pharmacology data
α2C-adrenoceptor/Alpha-2c adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1916] [GtoPdb: 27] [UniProtKB: P18825]
ChEMBL	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	B	6.55	pKi	282	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Adrenergic Alpha-2C radioligand binding (ligand: [3H] MK-912)	B	5.71	pIC50	1942	nM	IC50	DrugMatrix in vitro pharmacology data
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	Antagonist activity at D2 receptor (unknown origin) by HTRF cAMP assay	F	5.35	pIC50	4485	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127027-127027 [PMID:32122737]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)	B	5.9	pKi	1271	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Dopamine D3 radioligand binding (ligand: [3H] Spiperone)	B	5.43	pIC50	3743	nM	IC50	DrugMatrix in vitro pharmacology data
H1 receptor/Histamine H1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL231] [GtoPdb: 262] [UniProtKB: P35367]
ChEMBL	DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)	B	7.38	pKi	42	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Histamine H1, Central radioligand binding (ligand: [3H] Pyrilamine)	B	6.44	pIC50	361	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	Displacement of 8-OH-DPAT from human 5-HT1AR in human brain frontal cortex incubated for 30 mins by liquid scintillation counter analysis	B	6.93	pKi	118	nM	Ki	Eur J Med Chem (2022) 235: 114319-114319 [PMID:35367707]
ChEMBL	Agonist activity at 5HT1A receptor (unknown origin) by calcium-dye based FLIPR assay	F	6.11	pEC50	785	nM	EC50	Bioorg Med Chem Lett (2020) 30: 127027-127027 [PMID:32122737]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL273] [GtoPdb: 1] [UniProtKB: P19327]
ChEMBL	Binding affinity of a compound to rat brain 5-hydroxytryptamine 1A (serotonin) receptor assayed by radiolabeled [3H]-8-OH-DPAT ligand displacement	B	6.65	pKi	223.87	nM	Ki	J Med Chem (1996) 39: 126-134 [PMID:8568799]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)	B	6.75	pKi	178	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1A radioligand binding (ligand: [3H] 8-OH-DPAT)	B	6.51	pIC50	311	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3459] [GtoPdb: 2] [UniProtKB: P28564]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)	B	6.08	pKi	830	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT1B radioligand binding (ligand: [125I] Cyanopindolol)	B	5.87	pIC50	1356	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
GtoPdb	-	-	7.4	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)	B	8.25	pKi	5.6	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	Antagonist activity at 5HT2A receptor (unknown origin) by HTRF cAMP assay	F	6.61	pIC50	243	nM	IC50	Bioorg Med Chem Lett (2020) 30: 127027-127027 [PMID:32122737]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2A radioligand binding (ligand: [3H] Ketanserin)	B	7.7	pIC50	20	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
GtoPdb	-	-	8.2	pKi	-	-	-	Circulation (2000) 102: 2836-41 [PMID:11104741]; Psychopharmacology (Berl) (1996) 126: 234-40 [PMID:8876023]
ChEMBL	Compound was tested for the inhibition of [3H]ketanserin binding to 5-hydroxytryptamine 2A receptor	B	7.77	pIC50	17	nM	IC50	J Med Chem (1999) 42: 336-345 [PMID:9986703]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb	-	-	7.1	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]; Circulation (2000) 102: 2836-41 [PMID:11104741]
ChEMBL	Displacement of [3H]-5HT from human 5-HT2B receptor expressed in african green monkey COS7 cells assessed as inhibition constant	B	7.13	pKi	74	nM	Ki	J Med Chem (2023) 66: 11027-11039 [PMID:37584406]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)	B	7.17	pKi	68	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2B radioligand binding (ligand: [3H] Lysergic acid diethylamide)	B	6.97	pIC50	107	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb	-	-	6.6	pKi	-	-	-	Naunyn Schmiedebergs Arch Pharmacol (2004) 370: 114-23 [PMID:15322733]
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)	B	7.33	pKi	47	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Serotonin (5-Hydroxytryptamine) 5-HT2C radioligand binding (ligand: [3H] Mesulergine)	B	7.04	pIC50	91	nM	IC50	DrugMatrix in vitro pharmacology data
5-HT2C receptor in Rat [GtoPdb: 8] [UniProtKB: P08909]
GtoPdb	-	-	6.7	pKi	-	-	-	Circulation (2000) 102: 2836-41 [PMID:11104741]; Psychopharmacology (Berl) (1996) 126: 234-40 [PMID:8876023]
SERT/Serotonin transporter in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL228] [GtoPdb: 928] [UniProtKB: P31645]
ChEMBL	DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)	B	6.99	pKi	102	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Transporter, Serotonin (5-Hydroxytryptamine) (SERT) radioligand binding (ligand: [3H] Paroxetine)	B	6.72	pIC50	192	nM	IC50	DrugMatrix in vitro pharmacology data
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL	DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)	B	6.03	pKi	926	nM	Ki	DrugMatrix in vitro pharmacology data
ChEMBL	DRUGMATRIX: Sigma1 radioligand binding (ligand: [3H] Haloperidol)	B	5.66	pIC50	2203	nM	IC50	DrugMatrix in vitro pharmacology data

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]