ChEMBL ligand: CHEMBL431298 (SB-271046)
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368] There should be some charts here, you may need to enable JavaScript!
D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728] 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!
D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917] 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-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222] There should be some charts here, you may need to enable JavaScript!
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221] There should be some charts here, you may need to enable JavaScript!
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566] There should be some charts here, you may need to enable JavaScript!
5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939] 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] 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] There should be some charts here, you may need to enable JavaScript!
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] There should be some charts here, you may need to enable JavaScript!
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406] There should be some charts here, you may need to enable JavaScript!
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] 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
α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
ChEMBL	The compound was tested for the binding affinity towards Alpha-1B adrenergic receptor	B	5.7	pKi	1995.26	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
D1 receptor/Dopamine D1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
ChEMBL	Displacement of [3H]SCH-23390 from human cloned dopamine D1 receptor	B	6.92	pKi	120	nM	Ki	Bioorg Med Chem Lett (2008) 18: 738-743 [PMID:18053713]
D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
ChEMBL	The compound was tested for the binding affinity towards human cloned Dopamine receptor D2 in CHO cells, using [125I]iodosulpride as radioligand	B	5.6	pKi	2511.89	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
ChEMBL	Displacement of [3H]spiperone from human cloned dopamine D2 receptor	B	6.34	pKi	460	nM	Ki	Bioorg Med Chem Lett (2008) 18: 738-743 [PMID:18053713]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL	Displacement of [3H]spiperone from human cloned dopamine D3 receptor	B	5.88	pKi	1330	nM	Ki	Bioorg Med Chem Lett (2008) 18: 738-743 [PMID:18053713]
ChEMBL	The compound was tested for the binding affinity towards human cloned Dopamine receptor D3 in CHO cells, using [125I]iodosulpride as radioligand	B	6.3	pKi	501.19	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
D4 receptor/Dopamine D4 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
ChEMBL	Displacement of [3H]spiperone from human cloned dopamine D4 receptor	B	6.89	pKi	130	nM	Ki	Bioorg Med Chem Lett (2008) 18: 738-743 [PMID:18053713]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL	The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1A receptor in HEK293 cells, using [3H]8-OH-DPAT as radioligand	B	6.4	pKi	398.11	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
ChEMBL	Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor	B	6.47	pKi	340	nM	Ki	Bioorg Med Chem Lett (2008) 18: 738-743 [PMID:18053713]
5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
ChEMBL	The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1B receptor in CHO cells, using [3H]5-HT as radioligand	B	6.1	pKi	794.33	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL	The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1D receptor in CHO cells, using [3H]5-HT as radioligand	B	6.6	pKi	251.19	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL	The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1E receptor in CHO cells, using [3H]5-HT as radioligand	B	5	pKi	<10000	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
ChEMBL	The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 1F receptor in CHO cells, using [3H]5-HT as radioligand	B	6	pKi	<1000	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL	The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2A receptor in HEK293 cells, using [3H]ketanserin as radioligand	B	5.6	pKi	<2511.89	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
ChEMBL	Displacement of [3H]ketanserin from human cloned 5HT2A receptor	B	5.76	pKi	1740	nM	Ki	Bioorg Med Chem Lett (2008) 18: 738-743 [PMID:18053713]
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
ChEMBL	The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells, using [3H]5-HT as radioligand	B	5.4	pKi	<3981.07	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
ChEMBL	The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 2C receptor in HEK293 cells, using [3H]5-mesulergine as radioligand	B	5.7	pKi	1995.26	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
ChEMBL	Displacement of [3H]5-HT from 5-HT2C receptor (unknown origin) expressed in hamster AV12 cells	B	6.11	pKi	776.25	nM	Ki	J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL	Displacement of [3H]5-HT from 5-HT2C receptor (unknown origin) expressed in hamster AV12 cells	B	6.11	pKi	770	nM	Ki	J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL	Displacement of [3H]mesulergine from human cloned 5HT2C receptor	B	6.28	pKi	530	nM	Ki	Bioorg Med Chem Lett (2008) 18: 738-743 [PMID:18053713]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL	The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 4 receptor in HeLa cells, using [3H]LSD as radioligand	B	5.4	pKi	3981.07	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
ChEMBL	Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells by liquid scintillation counting	B	7.89	pKi	13	nM	Ki	J Med Chem (2009) 52: 675-687 [PMID:19159187]
ChEMBL	Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis	B	8.52	pKi	3.02	nM	Ki	J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL	Displacement of [3H]LSD from human 5-HT6 receptor expressed in hamster BHK cells after 60 mins by scintillation counting analysis	B	8.52	pKi	3	nM	Ki	J Med Chem (2014) 57: 5823-5828 [PMID:24878269]
ChEMBL	Displacement of [3H]LSD from human 5-HT6 receptor expressed in HEK293 cell membranes incubated for 60 mins by radioligand binding assay	B	8.77	pKi	1.7	nM	Ki	Eur J Med Chem (2015) 92: 807-817 [PMID:25637882]
ChEMBL	Antagonist activity at human recombinant 5HT6 receptor expressed in CHO cells	B	8.89	pKi	1.3	nM	Ki	J Med Chem (2014) 57: 7160-7181 [PMID:24850589]
ChEMBL	Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HEK 293 cells	B	8.89	pKi	1.3	nM	Ki	Bioorg Med Chem Lett (2000) 10: 1719-1721 [PMID:10937732]
ChEMBL	Displacement of [3H]LSD from human 5HT6 receptor expressed in HeLa cells	B	8.89	pKi	1.3	nM	Ki	Bioorg Med Chem Lett (2009) 19: 3214-3216 [PMID:19433358]
ChEMBL	Binding affinity to 5-HT6 receptor (unknown origin)	B	8.9	pKi	1.26	nM	Ki	J Med Chem (2024) 67: 1580-1610 [PMID:38190615]
ChEMBL	Displacement of [3H]LSD from human 5-hydroxytryptamine 6 receptor expressed in HeLa cells	B	8.9	pKi	1.26	nM	Ki	Bioorg Med Chem Lett (2005) 15: 4867-4871 [PMID:16143522]
ChEMBL	The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 6 receptor in HeLa cells, using [3H]LSD as radioligand; n=3	B	8.9	pKi	1.26	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
ChEMBL	Binding affinity against human 5-hydroxytryptamine 6 receptor	B	8.9	pKi	1.26	nM	Ki	Bioorg Med Chem Lett (2001) 11: 2843-2846 [PMID:11597412]
ChEMBL	Binding affinity to 5HT6 receptor	B	8.9	pKi	1.26	nM	Ki	Bioorg Med Chem Lett (2011) 21: 698-703 [PMID:21190848]
GtoPdb	-	-	8.9	pKi	1.26	nM	Ki	J Med Chem (1999) 42: 202-5 [PMID:9925723]
ChEMBL	Binding affinity towards human 5-hydroxytryptamine 6 receptor	B	9	pKi	1	nM	Ki	J Med Chem (2003) 46: 2795-2812 [PMID:12825922]
ChEMBL	Binding affinity for human 5-hydroxytryptamine 6 receptor	B	9	pKi	1	nM	Ki	J Med Chem (2005) 48: 4216-4219 [PMID:15974573]
ChEMBL	Binding affinity against 5 Hydroxy tryptamine 6 receptor	B	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (2005) 15: 1707-1711 [PMID:15745826]
ChEMBL	Displacement of [3H]LSD from human cloned 5HT6 receptor expressed in HEK293 cells	B	9	pKi	1	nM	Ki	Bioorg Med Chem Lett (2008) 18: 738-743 [PMID:18053713]
ChEMBL	Inhibition of [3H]LSD binding to human 5-hydroxytryptamine 6 receptor expressed in HEK293 cells	B	9.1	pKi	0.8	nM	Ki	J Med Chem (2005) 48: 1781-1795 [PMID:15771424]
ChEMBL	Displacement of [3H]LSD from human recombinant 5HT6 receptor	B	9.18	pKi	0.66	nM	Ki	Bioorg Med Chem Lett (2009) 19: 2409-2412 [PMID:19346128]
ChEMBL	Displacement of [3H]-LSD from human 5-HT6R expressed in human HeLa cells after 1 hr by liquid scintillation counting method	B	9.2	pKi	0.63	nM	Ki	Eur J Med Chem (2017) 135: 117-124 [PMID:28441580]
ChEMBL	Inhibition of human recombinant 5HT6 receptor expressed in CHO cells	B	8.7	pIC50	2	nM	IC50	J Med Chem (2014) 57: 7160-7181 [PMID:24850589]
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
ChEMBL	The compound was tested for the binding affinity towards human cloned 5-hydroxytryptamine 7 receptor in HEK293 cells, using [3H]5-CT as radioligand	B	5.4	pKi	3981.07	nM	Ki	Bioorg Med Chem Lett (2002) 12: 1357-1360 [PMID:11992776]
ChEMBL	Displacement of [3H]LSD from human cloned 5HT7 receptor	B	6.59	pKi	260	nM	Ki	Bioorg Med Chem Lett (2008) 18: 738-743 [PMID:18053713]
ChEMBL	Displacement of [3H]-LSD from human 5HT6 receptor expressed in BHK cell membrane measured after 60 mins by scintillation counter method	B	8.52	pKi	3	nM	Ki	Eur J Med Chem (2021) 210: 113059-113059 [PMID:33310288]

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]