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ChEMBL ligand: CHEMBL14460 (SB-243213) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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D2 receptor/Dopamine D2 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416] | ||||||||
ChEMBL | Displacement of [3H]spiperone from human cloned dopamine D2 receptor | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3844-3847 [PMID:18602261] |
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 | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3844-3847 [PMID:18602261] |
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 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3844-3847 [PMID:18602261] |
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908] | ||||||||
ChEMBL | Displacement of [3H]8-OH-DPAT from human cloned 5HT1A receptor | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3844-3847 [PMID:18602261] |
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223] | ||||||||
ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine receptor 2A in HEK293 cells, using [3H]ketanserin as radioligand. | B | 6.8 | pKi | 158.49 | nM | Ki | J Med Chem (2000) 43: 1123-1134 [PMID:10737744] |
ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine 2A receptor of HEK293 cells by displacement of [3H]ketanserin | B | 6.8 | pKi | 158.49 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1863-1866 [PMID:10969986] |
ChEMBL | Binding affinity for human 5-hydroxytryptamine 2A receptor expressed in HEK 293 cells using [3H]ketanserin | B | 6.8 | pKi | 158.49 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4989-4993 [PMID:16168649] |
GtoPdb | - | - | 6.8 | pKi | - | - | - | J Med Chem (2000) 43: 1123-34 [PMID:10737744] |
ChEMBL | Displacement of [3H]ketanserin from human cloned 5HT2A receptor | B | 7.49 | pIC50 | 32.4 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3844-3847 [PMID:18602261] |
5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595] | ||||||||
GtoPdb | - | - | 7 | pKi | - | - | - | J Med Chem (2000) 43: 1123-34 [PMID:10737744] |
ChEMBL | Binding affinities towards human cloned 5-hydroxytryptamine 2B receptor in HEK293 cells using [3H]5-HT as radioligand. | B | 7 | pKi | 100 | nM | Ki | J Med Chem (2000) 43: 1123-1134 [PMID:10737744] |
ChEMBL | Binding affinity towards human cloned 5-HT2B receptor of HEK293 cells by displacement of [3H]5-HT | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1863-1866 [PMID:10969986] |
ChEMBL | Binding affinity for human 5-hydroxytryptamine 2B receptor expressed in HEK 293 cells using [3H]5-HT | B | 7 | pKi | 100 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4989-4993 [PMID:16168649] |
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335] | ||||||||
ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine receptor 2C in HEK293 cells, using [3H]mesulergine as radioligand. | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2000) 43: 1123-1134 [PMID:10737744] |
ChEMBL | Binding affinity towards human cloned 5-hydroxytryptamine 2C receptor of HEK293 cells by displacement of [3H]mesulergine | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2000) 10: 1863-1866 [PMID:10969986] |
ChEMBL | Binding affinity for human 5-hydroxytryptamine 2C receptor expressed in HEK 293 cells using [3H]mesulergine | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2005) 15: 4989-4993 [PMID:16168649] |
ChEMBL | Binding affinity at 5HT2C receptor | B | 9 | pKi | 1 | nM | Ki | Bioorg Med Chem Lett (2008) 18: 3844-3847 [PMID:18602261] |
ChEMBL | Displacement of [3H]mesulergine at human cloned 5HT2C receptor expressed in CHOK1 cell | B | 9.15 | pIC50 | 0.7 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3844-3847 [PMID:18602261] |
GtoPdb | - | - | 9 | pEC50 | - | - | - | J Med Chem (2000) 43: 1123-34 [PMID:10737744] |
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 cloned 5HT6 receptor | B | 6.18 | pIC50 | 667 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3844-3847 [PMID:18602261] |
5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969] | ||||||||
ChEMBL | Displacement of [3H]LSD from human cloned 5HT7 receptor | B | 6 | pIC50 | >1000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 3844-3847 [PMID:18602261] |
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]