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ChEMBL ligand: CHEMBL431298 (SB-271046) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
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]