SB 243213 [Ligand Id: 194] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL14460 (SB-243213)
  • 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-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-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
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]