GR 113808 [Ligand Id: 247] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL33884 (GR-113808) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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| 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: 373, 374] [UniProtKB: P35563, Q9JJ16] | ||||||||
| 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]
