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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 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]