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ChEMBL ligand: CHEMBL286136 (ML-10302) |
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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 W2 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | 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 | Binding affinity against 5-hydroxytryptamine 3 receptor using [3H]BRL-43694 in rat posterior cortex | B | 6.11 | pKi | 782 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 1433-1436 |
ChEMBL | Binding affinity was measured on 5-hydroxytryptamine 3 receptor using [3H]-BRL 43694 as radioligand in rat posterior cortex. | B | 6.14 | pKi | 730 | nM | Ki | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] | ||||||||
ChEMBL | Binding affinity was determined against cloned 5-hydroxytryptamine 4B receptor isoform expressed in COS-7 cells | B | 7.97 | pKi | 10.7 | 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 | 8.08 | pKi | 8.4 | nM | Ki | J Med Chem (2000) 43: 3761-3769 [PMID:11020291] |
ChEMBL | Binding affinity was determined against cloned 5-hydroxytryptamine 4C receptor isoform expressed in COS-7 cells | B | 8.1 | pKi | 7.98 | nM | Ki | J Med Chem (2000) 43: 3761-3769 [PMID:11020291] |
ChEMBL | Binding affinity to Rluc fused 5HT4 receptor expressed in CHO cells | B | 8.24 | pKi | 5.7 | nM | Ki | J Med Chem (2007) 50: 4482-4492 [PMID:17676726] |
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 | 8.25 | pKi | 5.6 | nM | Ki | J Med Chem (2000) 43: 3761-3769 [PMID:11020291] |
ChEMBL | Displacement of [3H]GR-113808 from human 5HT4 isoform E receptor expressed in rat C6 cells by liquid scintillation counting | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2009) 52: 2214-2225 [PMID:19334715] |
ChEMBL | Binding affinity for 5-HT4 receptor using [3H]GR-113808 | B | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2005) 48: 6220-6228 [PMID:16190749] |
ChEMBL | Displacement of [3H]GR-113808 from human 5HT4e receptor expressed in C6 cells | F | 8.3 | pKi | 5 | nM | Ki | J Med Chem (2007) 50: 4482-4492 [PMID:17676726] |
ChEMBL | Binding affinity was determined against cloned 5-hydroxytryptamine 4D receptor isoform expressed in COS-7 cells | B | 8.43 | pKi | 3.69 | nM | Ki | J Med Chem (2000) 43: 3761-3769 [PMID:11020291] |
ChEMBL | Binding affinity to YFP fused 5HT4 receptor expressed in CHO cells | B | 8.46 | pKi | 3.5 | nM | Ki | J Med Chem (2007) 50: 4482-4492 [PMID:17676726] |
GtoPdb | - | - | 9 | pKi | 1 | nM | Ki |
J Neurochem (1998) 70: 2252-61 [PMID:9603189]; Br J Pharmacol (2000) 129: 771-81 [PMID:10683202]; Br J Pharmacol (2000) 131: 827-35 [PMID:11030734]; Br J Pharmacol (2000) 130: 527-38 [PMID:10821780]; J Med Chem (2003) 46: 2606-20 [PMID:12801225] |
ChEMBL | Binding affinity towards cloned human 5-hydroxytryptamine 4E receptor expressed in C6 glial cells using [3H]GR-113808 as radioligand | B | 9 | pKi | 1 | nM | Ki | J Med Chem (2003) 46: 2606-2620 [PMID:12801225] |
ChEMBL | Agonist activity at human 5HT4 isoform E receptor expressed in rat C6 cells assessed as cAMP accumulation by radio-immunoassay relative to 5HT | F | 7.29 | pEC50 | 51 | nM | EC50 | J Med Chem (2009) 52: 2214-2225 [PMID:19334715] |
ChEMBL | Agonist activity against 5-HT4 receptor in rat esophageal muscularis mucosae | F | 7.7 | pEC50 | 19.95 | nM | EC50 | Bioorg Med Chem Lett (1994) 4: 2477-2480 |
ChEMBL | Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay | F | 8.6 | pEC50 | 2.5 | nM | EC50 | Eur J Med Chem (2015) 103: 289-301 [PMID:26363507] |
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] | ||||||||
ChEMBL | Binding affinity at 5-hydroxytryptamine 4 receptor in rat striatal membranes by [3H]GR-113808 displacement. | B | 8.97 | pKi | 1.07 | 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 | 8.97 | pKi | 1.07 | 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 | 8.97 | pKi | 1.07 | nM | Ki | Bioorg Med Chem Lett (1994) 4: 1433-1436 |
ChEMBL | 5-hydroxytryptamine 4 receptor agonist activity was determined by the relaxation of the carbachol-contracted rat esophageal tunica muscularis mucosae | F | 8.62 | pIC50 | 2.4 | nM | IC50 | 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 | Displacement of [3H]GR113808 from serotonin 5-HT4 receptor in Dunkin-Hartley guinea pigs striatal nuclei membranes incubated for 2 hrs by liquid scintillation counting | B | 8.22 | pKi | 6 | nM | Ki | Medchemcomm (2017) 8: 647-651 [PMID:30108781] |
ChEMBL | Displacement of [3H]-GR113808 from 5-HT4R in Dunkin-Hartley guinea pig straitum nuclear membranes after 2 hrs by filter binding method | B | 8.22 | pKi | 6 | nM | Ki | Medchemcomm (2018) 9: 1466-1471 [PMID:30288221] |
ChEMBL | 5-hydroxytryptamine 4 receptor agonist activity, concentration which gave 50% increase in the response to electrically-stimulated myenteric plexus and longitudinal muscle of the guinea pig ileum | F | 8.4 | pEC50 | 4 | nM | EC50 | J Med Chem (1997) 40: 608-621 [PMID:9046352] |
ChEMBL | 5-hydroxytryptamine 4 receptor agonist activity as increased response to electrical stimulation in guinea pig ileum | F | 8.4 | pEC50 | 4 | nM | EC50 | Bioorg Med Chem Lett (1994) 4: 1433-1436 |
ChEMBL | Agonist activity at 5-HT4 receptor in guinea pig ileum assessed as increase in response to electrical stimulation | B | 8.4 | pEC50 | 4 | nM | EC50 | Eur J Med Chem (2015) 103: 289-301 [PMID:26363507] |
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]