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 |
|---|---|---|---|---|---|---|---|---|
| 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 | 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 |
Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 146-60 [PMID:11218067]; J Neurochem (2000) 74: 478-89 [PMID:10646498]; J Neurochem (1998) 70: 2252-61 [PMID:9603189]; Neuroreport (1997) 8: 3189-96 [PMID:9351641]; Br J Pharmacol (2000) 131: 827-35 [PMID:11030734]; Br J Pharmacol (2004) 143: 361-70 [PMID:15351779]; J Neurochem (1997) 69: 1810-9 [PMID:9349523] |
| 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 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]
