ChEMBL ligand: CHEMBL6616 (Racemic DOI)
Monoamine oxidase A in Rat [ChEMBL: CHEMBL3358] [UniProtKB: P21396] 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] 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 Mouse [ChEMBL: CHEMBL5377] [GtoPdb: 6] [UniProtKB: P35363] 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] 5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994] 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/Serotonin 2c (5-HT2c) receptor in Mouse [ChEMBL: CHEMBL3006] [GtoPdb: 8] [UniProtKB: P34968] 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909] There should be some charts here, you may need to enable JavaScript!
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] There should be some charts here, you may need to enable JavaScript!
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566] There should be some charts here, you may need to enable JavaScript!
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939] 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
Monoamine oxidase A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3358] [UniProtKB: P21396]
ChEMBL	Inhibitory concentration against monoamine oxidase A in rat brain mitochondrial suspension	B	4.36	pIC50	44000	nM	IC50	J Med Chem (2005) 48: 2407-2419 [PMID:15801832]
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]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL	Displacement of [3H]ketanserein from 5HT2A receptor F340L mutant expressed in NIH3T3 cells	B	4.86	pKi	13700	nM	Ki	J Med Chem (2008) 51: 6808-6828 [PMID:18847250]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in human A549 cells	B	7.54	pKi	29	nM	Ki	Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904]
ChEMBL	Displacement of [3H]INBMeO from human 5HT2A receptor expressed in human A549 cells	B	7.55	pKi	28	nM	Ki	Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904]
ChEMBL	Displacement of [3H]INBMeO from human 5HT2A receptor expressed in human HEK293 cells	B	7.85	pKi	14	nM	Ki	Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904]
ChEMBL	Displacement of [3H]ketanserin from human 5HT2A receptor expressed in human HEK293 cells	B	7.89	pKi	13	nM	Ki	Bioorg Med Chem (2008) 16: 6116-6123 [PMID:18468904]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor expressed in NIH3T3 cells	B	9.04	pKi	0.92	nM	Ki	J Med Chem (2008) 51: 6808-6828 [PMID:18847250]
ChEMBL	Displacement of [125I]DOI from recombinant human 5HT2A expressed in Syrian hamster AV12 cell membranes	B	9.15	pKi	0.7	nM	Ki	J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
GtoPdb	-	-	9.2	pKi	0.63	nM	Ki	Biochem Pharmacol (1996) 51: 71-6 [PMID:8534270]; Mol Pharmacol (1990) 38: 604-9 [PMID:2233697]; Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 1-6 [PMID:9933142]
ChEMBL	Binding activity against cloned human 5-hydroxytryptamine 2A receptor using [125I]DOI as the radioligand.	B	9.34	pKi	0.46	nM	Ki	J Med Chem (1998) 41: 5148-5149 [PMID:9857084]
ChEMBL	Partial agonist activity at human 5-HT2A receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay	B	8.2	pEC50	6.31	nM	EC50	Bioorg Med Chem (2015) 23: 3933-3937 [PMID:25583099]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5377] [GtoPdb: 6] [UniProtKB: P35363]
ChEMBL	Percent of maximum stimulation of phosphatidylinositol turnover at cloned 5-hydroxytryptamine 2A receptor in 3T3 cells	F	6.92	pKd	119	nM	K aff	J Med Chem (1994) 37: 4346-4351 [PMID:7996545]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL322] [GtoPdb: 6] [UniProtKB: P14842]
GtoPdb	-	-	7.1	pKi	-	-	-	Mol Pharmacol (2000) 58: 877-86 [PMID:11040033]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A receptor in Sprague-Dawley rat brain by liquid scintillation spectroscopy	B	7.72	pKi	19	nM	Ki	Bioorg Med Chem (2008) 16: 4661-4669 [PMID:18296055]
ChEMBL	Displacement of [3H]ketanserin from 5HT2A in Sprague-Dawley rat cortex membranes measured after 15 mins	B	7.72	pKi	19	nM	Ki	J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
ChEMBL	Displacement of [3H]DOB from 5HT2A in Sprague-Dawley rat cortex membranes measured after 15 mins by scintillation counting method	B	9.15	pKi	0.7	nM	Ki	J Med Chem (2017) 60: 2605-2628 [PMID:28244748]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL	Binding activity against cloned human 5-hydroxytryptamine 2B receptor using [3H]5-HT as the radioligand.	B	7.37	pKi	42.7	nM	Ki	J Med Chem (1998) 41: 5148-5149 [PMID:9857084]
GtoPdb	-	-	7.7	pKi	19.9	nM	Ki	Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 1-6 [PMID:9933142]; Mol Pharmacol (1994) 46: 227-34 [PMID:8078486]; Br J Pharmacol (2003) 140: 277-84 [PMID:12970106]
ChEMBL	Displacement of radiolabeled DOI from human 5HT2B receptor agonist site	F	8.46	pKi	3.5	nM	Ki	J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL	Displacement of [125I](+/-)-DOI from human 5HT2B receptor	B	8.7	pKi	2	nM	Ki	J Med Chem (2011) 54: 5320-5334 [PMID:21726069]
ChEMBL	Binding affinity to human 5-HT2B receptor by radioligand displacement assay	B	8.7	pKi	2	nM	Ki	Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL	Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting	B	8.8	pKi	1.6	nM	Ki	J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL	Binding affinity to human 5-HT2B receptor by radioligand displacement assay	B	8.4	pIC50	4	nM	IC50	Eur J Med Chem (2013) 63: 85-94 [PMID:23466604]
ChEMBL	Displacement of radiolabeled DOI from human 5HT2B receptor agonist site	F	8.46	pIC50	3.5	nM	IC50	J Med Chem (2008) 51: 7094-7098 [PMID:18983139]
ChEMBL	Binding affinity to human 5-HT2B receptor by radioligand displacement assay	B	8.49	pIC50	3.2	nM	IC50	Bioorg Med Chem (2013) 21: 2764-2771 [PMID:23582449]
ChEMBL	Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells after 60 mins by scintillation counting	B	8.49	pIC50	3.2	nM	IC50	J Med Chem (2017) 60: 349-361 [PMID:27997171]
ChEMBL	Displacement of [125I](+/-)DOI from human recombinant 5-HT2B receptor expressed in CHO cells	B	8.6	pIC50	2.5	nM	IC50	Bioorg Med Chem (2016) 24: 1793-1810 [PMID:26988801]
ChEMBL	Displacement of [125I]DOI from human recombinant 5HT2B receptor expressed in CHO cells measured after 60 mins by scintillation counting method	B	8.6	pIC50	2.5	nM	IC50	Bioorg Med Chem (2017) 25: 471-482 [PMID:27876250]
5-HT2B receptor in Rat [GtoPdb: 7] [UniProtKB: P30994]
GtoPdb	-	-	7.6	pKi	-	-	-	Mol Pharmacol (1994) 46: 227-34 [PMID:8078486]; Mol Pharmacol (1993) 43: 419-26 [PMID:8450835]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
GtoPdb	-	-	8.6	pKi	2.51	nM	Ki	Naunyn Schmiedebergs Arch Pharmacol (1999) 359: 1-6 [PMID:9933142]; Br J Pharmacol (2003) 140: 277-84 [PMID:12970106]; Synapse (2000) 35: 144-150 [PMID:10611640]
ChEMBL	Binding activity against cloned human 5-hydroxytryptamine 2C receptor using [125I]DOI as the radioligand.	B	8.74	pKi	1.82	nM	Ki	J Med Chem (1998) 41: 5148-5149 [PMID:9857084]
ChEMBL	Partial agonist activity at human 5-HT2C receptor expressed in HEK293 cells preincubated for 1 hr at 37 degC followed by incubated for 15 mins at room temperature by IP-One assay	B	7.34	pEC50	45.71	nM	EC50	Bioorg Med Chem (2015) 23: 3933-3937 [PMID:25583099]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3006] [GtoPdb: 8] [UniProtKB: P34968]
ChEMBL	Percent of maximum stimulation of phosphatidylinositol turnover at cloned 5-hydroxytryptamine 2C receptor in A9 cells	F	7.37	pKd	43	nM	K aff	J Med Chem (1994) 37: 4346-4351 [PMID:7996545]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL	Binding affinity towards 5-hydroxytryptamine 1C receptor from frontal cortical regions of male Sprague-Dawley rat homogenates, using [3H]mesulergine as radioligand	B	7.52	pKi	30	nM	Ki	J Med Chem (1992) 35: 734-740 [PMID:1542100]
ChEMBL	Agonist activity at rat 5-HT2C receptor expressed in African clawed frog oocytes assessed as increase in current amplitude	B	6.75	pEC50	178	nM	EC50	J Med Chem (2017) 60: 6273-6288 [PMID:28657744]
5-HT5A receptor/Serotonin 5a (5-HT5a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 5A receptor	B	6	pKi	>1000	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
5-ht1e receptor in Human [GtoPdb: 4] [UniProtKB: P28566]
GtoPdb	-	-	5.8	pKi	-	-	-	Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]; Eur J Pharmacol (2004) 484: 127-39 [PMID:14744596]
5-HT1F receptor in Human [GtoPdb: 5] [UniProtKB: P30939]
GtoPdb	-	-	5.8	pKi	-	-	-	Proc Natl Acad Sci USA (1993) 90: 408-12 [PMID:8380639]

ChEMBL data shown on this page come from version 32:

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]