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 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]
