GR 113808 [Ligand Id: 247] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL33884 (GR-113808)
Created with Highcharts 10.3.3ValuesChart context menuPlasmodium falciparumpKd Plasmodium falciparumpKi Plasmodium falciparumpIC50 Plasmodium falciparumpEC50 Plasmodium falciparum0123456Highcharts.com
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 3 (5-HT3) receptorpKd RatpKi RatpIC50 RatpEC50 Rat01234567Highcharts.com
  • 5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 3a (5-HT3a) receptorpKd HumanpKi HumanpIC50 HumanpEC50 Human0123456Highcharts.com
  • 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]
Created with Highcharts 10.3.3ValuesChart context menuSerotonin 4 (5-HT4) receptorpKd HumanpKi HumanpIC50 HumanpEC50 HumanpKd MousepKi MousepIC50 MousepEC50 MousepKd RatpKi RatpIC50 RatpEC50 RatpKd Guinea pigpKi Guinea pigpIC50 Guinea pigpEC50 Guinea pig024681012Highcharts.com
DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay F 4.9 pIC50 12589.25 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5.1 pIC50 7943.28 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094116] [GtoPdb: 373374] [UniProtKB: P35563Q9JJ16]
ChEMBL Inhibitory concentration against 5-hydroxytryptamine 3 receptor in rat entorhinal cortex using [3H]-LY 278584 as radioligand B 6 pIC50 >1000 nM IC50 J Med Chem (1999) 42: 2870-2880 [PMID:10425096]
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 5 pKi >10000 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 Antagonist activity at 5-HT4 receptor in human HeLa cells assessed as inhibition of intracellular calcium mobilization incubated for 2 hrs by FLIPR assay B 8.85 pKi 1.4 nM Ki Bioorg Med Chem (2023) 84: 117256-117256 [PMID:37003157]
ChEMBL Binding affinity to YFP fused 5HT4 receptor expressed in CHO cells B 9.15 pKi 0.7 nM Ki J Med Chem (2007) 50: 4482-4492 [PMID:17676726]
ChEMBL Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells B 9.28 pKi 0.53 nM Ki J Med Chem (2000) 43: 3761-3769 [PMID:11020291]
ChEMBL Binding affinity to Rluc fused 5HT4 receptor expressed in CHO cells B 9.3 pKi 0.5 nM Ki J Med Chem (2007) 50: 4482-4492 [PMID:17676726]
ChEMBL Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells F 9.3 pKi 0.5 nM Ki J Med Chem (2007) 50: 4482-4492 [PMID:17676726]
ChEMBL Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells B 9.39 pKi 0.41 nM Ki J Med Chem (2000) 43: 3761-3769 [PMID:11020291]
ChEMBL Binding affinity was determined against cloned 5-hydroxytryptamine 4A receptor isoform expressed in COS-7 cells B 9.48 pKi 0.33 nM Ki J Med Chem (2000) 43: 3761-3769 [PMID:11020291]
ChEMBL Displacement of [3H]GR113808 from human 5HT4b receptor expressed in HEK293 cell membranes B 9.6 pKi 0.25 nM Ki Bioorg Med Chem Lett (2014) 24: 4598-4602 [PMID:25149506]
ChEMBL Binding affinity at 5HT4 receptor B 9.8 pKi 0.16 nM Ki Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477]
ChEMBL Binding affinity was determined against cloned 5-hydroxytryptamine 4E receptor isoform expressed in C6 glial cells incubated with 0.2 nM [3H]GR-113808 B 10 pKi 0.1 nM Ki J Med Chem (2000) 43: 3761-3769 [PMID:11020291]
ChEMBL Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells B 10.11 pKi 0.08 nM Ki J Med Chem (2000) 43: 3761-3769 [PMID:11020291]
ChEMBL Antagonistic activity at human 5HT4 receptor expressed in HEK293 cells F 10.13 pKi 0.07 nM Ki Bioorg Med Chem (2010) 18: 8600-8613 [PMID:21075638]
GtoPdb - - 10.3 pKi 0.05 nM Ki J Neurochem (1997) 69: 1810-9 [PMID:9349523];
J Neurochem (1998) 70: 2252-61 [PMID:9603189];
Neuroreport (1997) 8: 3189-96 [PMID:9351641];
J Neurochem (2000) 74: 478-89 [PMID:10646498];
Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 146-60 [PMID:11218067];
Br J Pharmacol (2000) 131: 827-35 [PMID:11030734];
Br J Pharmacol (2004) 143: 361-70 [PMID:15351779]
ChEMBL Displacement of [3H]GR113808 from human 5-HT4B receptor expressed in HEK293 cells after 1 hr by liquid scintillation counting analysis B 10.4 pKi 0.04 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 10.4 pKi 0.04 nM Ki Bioorg Med Chem (2013) 21: 7134-7145 [PMID:24113240]
ChEMBL Antagonist activity at human 5HT4ER expressed in CHO cells assessed as reduction in cAMP levels F 9.68 pIC50 0.21 nM IC50 J Med Chem (2012) 55: 9446-9466 [PMID:23043420]
5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288]
GtoPdb - - 9.7 pKi - - - FEBS Lett (1996) 398: 19-25 [PMID:8946946]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
GtoPdb - - 8.7 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 9.82 pKi 0.15 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 9.82 pKi 0.15 nM Ki J Med Chem (1997) 40: 608-621 [PMID:9046352]
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL Binding affinity against 5-hydroxytryptamine 4 receptor in guinea pig striatum using [3H]GR-113808 as radioligand B 9.96 pKi 0.11 nM Ki J Med Chem (1999) 42: 2870-2880 [PMID:10425096]
ChEMBL 5-hydroxytryptamine 4 receptor antagonist activity, concentration which gave 50% reduction of the 5-HT-induced contractions in the guinea pig ileum F 7.89 pIC50 13 nM IC50 J Med Chem (1997) 40: 608-621 [PMID:9046352]

ChEMBL data shown on this page come from version 35:

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]