ML 10302 [Ligand Id: 235] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL286136 (ML-10302)
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  • 5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
  • 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]
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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 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 31:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, Cibrián-Uhalte E, Davies M, Dedman N, Karlsson A, Magariños MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]