SDZ 205557 [Ligand Id: 258] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL287045 (SDZ-205557)
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  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
  • 5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288]
  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
  • Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16]
ChEMBL Binding affinity against 5-hydroxytryptamine 3 receptor using [3H]BRL-43694 in rat posterior cortex B 6.69 pKi 205 nM Ki Bioorg Med Chem Lett (1994) 4: 1433-1436
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 6.9 pKi 125.89 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 Binding affinity at 5HT4 receptor B 8.2 pKi 6.31 nM Ki Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477]
5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288]
GtoPdb - - 8.1 pKi - - - Hypertension (1995) 26: 1056-9 [PMID:7498967]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
GtoPdb - - 7.7 pKi - - - Neuropharmacology (1997) 36: 671-9 [PMID:9225293]
ChEMBL Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement. B 8.26 pKi 5.5 nM Ki J Med Chem (1997) 40: 1755-1761 [PMID:9171886]
ChEMBL Binding affinity towards 5-hydroxytryptamine 4 receptor was determined in rat striatal membranes using [3H]GR-113808 as radioligand B 8.26 pKi 5.5 nM Ki J Med Chem (1997) 40: 608-621 [PMID:9046352]
ChEMBL Binding affinity against 5-hydroxytryptamine 4 receptor using [3H]GR-113808 as radioligand in rat striatum B 8.28 pKi 5.3 nM Ki Bioorg Med Chem Lett (1994) 4: 1433-1436
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL Inhibition of 5-HT-evoked 5-HT4 receptor-mediated contractions in the guinea pig distal colon longitudinal muscle myenteric plexus (LMMP) F 6.6 pIC50 251.19 nM IC50 J Med Chem (1993) 36: 4121-4123 [PMID:8258837]
ChEMBL 5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum F 7.11 pIC50 77 nM IC50 J Med Chem (1997) 40: 608-621 [PMID:9046352]
ChEMBL 5-hydroxytryptamine 4 receptor antagonist activity expressed as the concentration which produced a 50% reduction of 5-HT induced contraction in guinea pig ileum; Not evaluable F 7.11 pIC50 77 nM IC50 Bioorg Med Chem Lett (1994) 4: 1433-1436
ChEMBL 5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum F 6 pEC50 >1000 nM EC50 Bioorg Med Chem Lett (1994) 4: 1433-1436

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]