piboserod [Ligand Id: 225] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL356359 (Piboserod, SB-207266) |
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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 | 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 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]
