piboserod [Ligand Id: 225] activity data from GtoPdb and ChEMBL

Click here for a description of the charts and data table

Please tell us if you are using this feature and what you think!

ChEMBL ligand: CHEMBL356359 (Piboserod, SB-207266)
  • D2 receptor/Dopamine D2 receptor in Human [ChEMBL: CHEMBL217] [GtoPdb: 215] [UniProtKB: P14416]
There should be some charts here, you may need to enable JavaScript!
  • D3 receptor/Dopamine D3 receptor in Human [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
There should be some charts here, you may need to enable JavaScript!
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
There should be some charts here, you may need to enable JavaScript!
  • 5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
There should be some charts here, you may need to enable JavaScript!
  • AT1 receptor/Type-1 angiotensin II receptor in Human [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
There should be some charts here, you may need to enable JavaScript!
  • 5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
There should be some charts here, you may need to enable JavaScript!
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 Binding affinity was determined by standard competitive displacement of [3H]-YM 09151 using Dopamine receptor D2 cloned from the african green monkey B 6 pKi <1000 nM Ki J Med Chem (1995) 38: 4760-4763 [PMID:7490724]
D3 receptor/Dopamine D3 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL234] [GtoPdb: 216] [UniProtKB: P35462]
ChEMBL Binding affinity was determined against Dopamine receptor D3 determined using cloned human receptors expressed in CHO cells radiolabeled with [125I]- iodosulpride B 6 pKi <1000 nM Ki J Med Chem (1995) 38: 4760-4763 [PMID:7490724]
Histamine H1 receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3943] [UniProtKB: P31389]
ChEMBL Binding affinity was determined against H1 receptor B 6 pKi <1000 nM Ki J Med Chem (1995) 38: 4760-4763 [PMID:7490724]
5-HT1A receptor/Serotonin 1a (5-HT1a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL214] [GtoPdb: 1] [UniProtKB: P08908]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1A receptor B 5 pKi <10000 nM Ki J Med Chem (1995) 38: 4760-4763 [PMID:7490724]
5-HT1D receptor/Serotonin 1d (5-HT1d) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1983] [GtoPdb: 3] [UniProtKB: P28221]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 4 receptor using [125I]SB 207710 as radioligand from piglet hippocampal membranes B 5 pKi <10000 nM Ki J Med Chem (1995) 38: 4760-4763 [PMID:7490724]
5-ht1e receptor/Serotonin 1e (5-HT1e) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2182] [GtoPdb: 4] [UniProtKB: P28566]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 1D receptor B 5 pKi <10000 nM Ki J Med Chem (1995) 38: 4760-4763 [PMID:7490724]
5-HT2A receptor/Serotonin 2a (5-HT2a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL224] [GtoPdb: 6] [UniProtKB: P28223]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 2A receptor B 6 pKi <1000 nM Ki J Med Chem (1995) 38: 4760-4763 [PMID:7490724]
5-HT2C receptor/Serotonin 2c (5-HT2c) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL324] [GtoPdb: 8] [UniProtKB: P08909]
ChEMBL Binding affinity was determined against cloned human 5-hydroxytryptamine 2C receptor using [3H]5-HT as radioligand B 6 pKi <1000 nM Ki J Med Chem (1995) 38: 4760-4763 [PMID:7490724]
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL Binding affinity at 5HT3 receptor B 6 pKi >1000 nM Ki Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL Displacement of [125I]SB207710 from human recombinant 5-HT4 receptor B 8.8 pKi 1.58 nM Ki Bioorg Med Chem (2013) 21: 7134-7145 [PMID:24113240]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 2C receptor using cloned rat receptors expressed in 293 cells radiolabeled with [3H]mesulergine B 9.3 pKi 0.5 nM Ki J Med Chem (1995) 38: 4760-4763 [PMID:7490724]
ChEMBL Binding affinity at 5HT4 receptor B 9.3 pKi 0.5 nM Ki Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477]
ChEMBL Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes B 9.4 pKi 0.4 nM Ki Bioorg Med Chem Lett (2014) 24: 4598-4602 [PMID:25149506]
ChEMBL Inhibitory constant for human cloned 5-HT4 receptor B 9.6 pKi 0.25 nM Ki Bioorg Med Chem Lett (2005) 15: 1697-1700 [PMID:15745824]
ChEMBL Displacement of [3H](1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate from human 5HT4R expressed in HEK293 cells B 9.8 pKi 0.16 nM Ki J Med Chem (2012) 55: 9446-9466 [PMID:23043420]
ChEMBL Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis B 10 pKi 0.1 nM Ki Eur J Med Chem (2013) 64: 629-637 [PMID:23711770]
ChEMBL Displacement of [3H]GR113808 from human 5HT4B receptor expressed in HEK293 cells B 10 pKi 0.1 nM Ki Bioorg Med Chem (2013) 21: 7134-7145 [PMID:24113240]
ChEMBL Displacement of [3H]GR113808 from human 5HT4 receptor expressed in HEK293 cells by liquid scintillation counting B 10.28 pKi 0.05 nM Ki Bioorg Med Chem (2010) 18: 8600-8613 [PMID:21075638]
GtoPdb - - 10.4 pKi - - - Br J Pharmacol (2004) 143: 549-60 [PMID:15466450];
Bioorg Med Chem (2001) 9: 2119-28 [PMID:11504648];
Neuroreport (1997) 8: 3189-96 [PMID:9351641]
ChEMBL Binding affinity was determined against 5-hydroxytryptamine 3 receptor B 9.2 pIC50 0.63 nM IC50 J Med Chem (1995) 38: 4760-4763 [PMID:7490724]
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL Displacement of [125I]SB207710 from 5-HT4 receptor in guinea pig brain membranes B 8.8 pKi 1.58 nM Ki Bioorg Med Chem (2013) 21: 7134-7145 [PMID:24113240]
AT1 receptor/Type-1 angiotensin II receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL227] [GtoPdb: 34] [UniProtKB: P30556]
ChEMBL Displacement of [tyrosyl-3,5-3H]angiotensin-2 from AT1 receptor (unknown origin) expressed in QBI-HEK293A cells after 2 hrs B 5 pKi >10000 nM Ki Bioorg Med Chem (2013) 21: 7134-7145 [PMID:24113240]
5-HT2B receptor in Human [GtoPdb: 7] [UniProtKB: P41595]
GtoPdb - - 6.3 pKi - - - Bioorg Med Chem (2001) 9: 2119-28 [PMID:11504648]
GtoPdb - - 6.6 pKi - - - Br J Pharmacol (2004) 143: 549-60 [PMID:15466450]

ChEMBL data shown on this page come from version 32:

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]