ChEMBL ligand: CHEMBL6616
5-HT1A receptor/5-hydroxytryptamine receptor 1A in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] 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 Mouse [ChEMBL: CHEMBL5377] [GtoPdb: 6] [UniProtKB: P35363] 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-HT2B receptor/5-hydroxytryptamine receptor 2B 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/5-hydroxytryptamine receptor 2C in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] 5-HT2C receptor/5-hydroxytryptamine receptor 2C in Mouse [ChEMBL: CHEMBL3006] [GtoPdb: 8] [UniProtKB: P34968] 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-HT5A receptor/5-hydroxytryptamine receptor 5A in Human [ChEMBL: CHEMBL3426] [GtoPdb: 10] [UniProtKB: P47898] There should be some charts here, you may need to enable JavaScript!
Amine oxidase [flavin-containing] A in Rat [ChEMBL: CHEMBL3358] [UniProtKB: P21396] 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
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]
5-HT2A receptor/5-hydroxytryptamine receptor 2A 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	Binding affinity to human [125I]DOI-labeled 5-HT2A receptor expressed in HEK293 cell membrane incubated for 60 mins	B	9.55	pKi	0.28	nM	Ki	J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2A 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/5-hydroxytryptamine receptor 2B 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	Binding affinity to 5HT2B (unknown origin) assessed as inhibition constant	B	8.54	pKi	2.9	nM	Ki	ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908]
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 5HT2B receptor	B	8.7	pKi	2	nM	Ki	J Med Chem (2011) 54: 5320-5334 [PMID:21726069]
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 [125I]DOI-labeled 5-HT2B receptor expressed in CHO cell membrane incubated for 60 mins	B	8.82	pKi	1.5	nM	Ki	J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
ChEMBL	Binding affinity to 5HT2B receptor (unknown origin) assessed as inhibition constant	B	9.12	pKi	0.75	nM	Ki	ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908]
ChEMBL	Inhibition of 5HT2B receptor (unknown origin)	B	8.24	pIC50	5.8	nM	IC50	ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908]
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	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	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 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]
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	Inhibition of 5HT2B (unknown origin)	B	8.82	pIC50	1.5	nM	IC50	ACS Chem Biol (2017) 12: 2619-2630 [PMID:28849908]
ChEMBL	Agonist activity at human 5-HT2B receptor expressed in CHO cells assessed as IP2 production measured after 30 mins incubation by HTRF assay	F	7.79	pEC50	16.22	nM	EC50	J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
ChEMBL	Agonist activity at human 5-HT2B receptor expressed in CHO cells assessed as IP2 production measured after 30 mins incubation by HTRF assay	F	7.8	pEC50	16	nM	EC50	J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
ChEMBL	Agonist activity at human 5-HT2B receptor expressed in CHO cells assessed as maximal IP2 production measured after 30 mins incubation by HTRF assay relative to control	F	8.1	pEC50	7.94	nM	EC50	J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
ChEMBL	Agonist activity at human 5-HT2B receptor expressed in CHO cells assessed as maximal IP2 production measured after 30 mins incubation by HTRF assay relative to control	F	8.15	pEC50	7	nM	EC50	J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
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/5-hydroxytryptamine receptor 2C 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: 144-50 [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	Binding affinity to human [125I]DOI-labeled 5-HT2C receptor expressed in HEK293 cell membrane incubated for 60 mins	B	9.32	pKi	0.48	nM	Ki	J Med Chem (2024) 67: 6144-6188 [PMID:38593423]
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/5-hydroxytryptamine receptor 2C 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/5-hydroxytryptamine receptor 2C 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/5-hydroxytryptamine receptor 5A 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]
Amine oxidase [flavin-containing] 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-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 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]