ML 10302 [Ligand Id: 235] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL286136 (ML-10302) |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 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 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]
