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]
  • This target only has 0 pki data point
1 CHEMBL14460_lig_chart_1 Dopamine D2 receptor Human
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  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
  • This target only has 0 pki data point
2 CHEMBL14460_lig_chart_2 Dopamine D3 receptor Human
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  • D4 receptor/Dopamine D4 receptor in Human [ChEMBL: CHEMBL219] [GtoPdb: 217] [UniProtKB: P21917]
  • This target only has 0 pki data point
3 CHEMBL14460_lig_chart_3 Dopamine D4 receptor Human
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  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
  • This target only has 0 pki data point
4 CHEMBL14460_lig_chart_4 Serotonin 1a (5-HT1a) receptor Human
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  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
5 CHEMBL14460_lig_chart_5 Serotonin 2a (5-HT2a) receptor Human
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  • 5-HT2B receptor/Serotonin 2b (5-HT2b) receptor in Human [ChEMBL: CHEMBL1833] [GtoPdb: 7] [UniProtKB: P41595]
6 CHEMBL14460_lig_chart_6 Serotonin 2b (5-HT2b) receptor Human
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  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Human [ChEMBL: CHEMBL225] [GtoPdb: 8] [UniProtKB: P28335]
7 CHEMBL14460_lig_chart_7 Serotonin 2c (5-HT2c) receptor Human
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  • 5-HT6 receptor/Serotonin 6 (5-HT6) receptor in Human [ChEMBL: CHEMBL3371] [GtoPdb: 11] [UniProtKB: P50406]
  • This target only has 0 pki data point
8 CHEMBL14460_lig_chart_8 Serotonin 6 (5-HT6) receptor Human
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  • 5-HT7 receptor/Serotonin 7 (5-HT7) receptor in Human [ChEMBL: CHEMBL3155] [GtoPdb: 12] [UniProtKB: P34969]
  • This target only has 0 pki data point
9 CHEMBL14460_lig_chart_9 Serotonin 7 (5-HT7) receptor Human
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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 27:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos 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]