SB 271046 [Ligand Id: 276] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL431298 (SB-271046)
  • α1B-adrenoceptor/Alpha-1b adrenergic receptor in Human [ChEMBL: CHEMBL232] [GtoPdb: 23] [UniProtKB: P35368]
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  • D1 receptor/Dopamine D1 receptor in Human [ChEMBL: CHEMBL2056] [GtoPdb: 214] [UniProtKB: P21728]
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  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
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  • 5-HT1B receptor/Serotonin 1b (5-HT1b) receptor in Human [ChEMBL: CHEMBL1898] [GtoPdb: 2] [UniProtKB: P28222]
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  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
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  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
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  • 5-HT1F receptor/Serotonin 1f (5-HT1f) receptor in Human [ChEMBL: CHEMBL1805] [GtoPdb: 5] [UniProtKB: P30939]
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
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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 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 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 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 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 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 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 against 5 Hydroxy tryptamine 6 receptor B 9 pKi 1 nM Ki Bioorg. Med. Chem. Lett. (2005) 15: 1707-1711 [PMID:15745826]
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 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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]