ChEMBL ligand: CHEMBL117287 (Prucaloprida, Prucalopride, R-093877, R093877, Resolor)
5-HT3A/5-hydroxytryptamine receptor 3A in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] There should be some charts here, you may need to enable JavaScript!
5-HT4 receptor/5-hydroxytryptamine receptor 4 in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] 5-HT4 receptor/5-hydroxytryptamine receptor 4 in Rat [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758] 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
5-HT3A/5-hydroxytryptamine receptor 3A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098]
ChEMBL	Binding affinity at 5HT3 receptor	B	5.4	pKi	3981.07	nM	Ki	Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477]
5-HT4 receptor/5-hydroxytryptamine receptor 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL	Tested for selectivity for 5-hydroxytryptamine 4 receptor	B	6	pKi	>1000	nM	Ki	J Med Chem (2003) 46: 319-344 [PMID:12540230]
ChEMBL	Tested for selectivity for 5-hydroxytryptamine 4 receptor	B	6	pKi	>1000	nM	Ki	J Med Chem (2003) 46: 319-344 [PMID:12540230]
ChEMBL	Tested for selectivity for 5-hydroxytryptamine 4 receptor	B	6.96	pKi	110	nM	Ki	J Med Chem (2003) 46: 319-344 [PMID:12540230]
ChEMBL	Competition Assay: Prior to these competition studies, a series of saturation curves were performed in order to check whether the pharmacological parameters Kd, Bmax and the Hill Coefficient of [3H]-GR113808, obtained in our experimental conditions, are consistent with those published in the literature. For that purpose, 7.5 μg/μL membrane preparation samples are incubated in duplicate (50 mM HEPES buffer, pH 7.4, +37° C.) at +37° C. for 30 minutes, in the presence of 7 increasing concentrations (0.05-1.5 nM, 200 μl of final volume) of [3H]-GR113808 (Grossman et al., 1993). Using a Brandel Cell Harvester, the binding of the radioligand with the proteins is interrupted by rapid filtration of the incubation medium through a filter strip (WHATMAN GF/B FP-100) pre-incubated in polyethylenimine (PEI 0.5% in water); filtration is followed by 3 rinses with 4 ml of 50 mM HEPES buffer, pH 7.4, at +4° C. The non-specific binding of [3H]-GR113808 is quantified in the presence of 30 μM of serotonin, specific binding thus being estimated as the difference: (binding in the absence of serotonin)−(binding in the presence of serotonin).	B	7.36	pKi	44.1	nM	Ki	US-9663465-B2. Acetylcholinesterase inhibitors and promnesiant serotonin 5-HT4 receptor agonists, their methods of preparation and the pharmaceutical compositions containing the same (2017)
ChEMBL	Tested for agonist activity against 5-hydroxytryptamine 4 receptor	F	8.12	pKi	7.5	nM	Ki	J Med Chem (2003) 46: 319-344 [PMID:12540230]
ChEMBL	Binding affinity at 5HT4 receptor	B	8.6	pKi	2.51	nM	Ki	Bioorg Med Chem (2009) 17: 2607-2622 [PMID:19261477]
GtoPdb	-	-	8.6	pKi	-	-	-	J Neurochem (2000) 74: 478-89 [PMID:10646498]; Eur J Pharmacol (2001) 423: 71-83 [PMID:11438309]
ChEMBL	Agonist activity at 5-HT4E receptor (unknown origin)	B	7.59	pEC50	26	nM	EC50	J Med Chem (2018) 61: 4993-5008 [PMID:29763304]
ChEMBL	Agonist activity at human 5HT4e receptor expressed in CHO cells assessed as cAMP level after 4 hrs by luciferase reporter gene assay	F	8.28	pEC50	5.2	nM	EC50	Eur J Med Chem (2015) 103: 289-301 [PMID:26363507]
ChEMBL	Agonist activity at recombinant human 5-HT4E receptor expressed in CHO cells assessed as induction of c-AMP accumulation after 4 hrs by luciferase reporter assay	B	8.28	pEC50	5.2	nM	EC50	J Med Chem (2018) 61: 4993-5008 [PMID:29763304]
5-HT4 receptor/5-hydroxytryptamine receptor 4 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4317] [GtoPdb: 9] [UniProtKB: Q62758]
ChEMBL	Agonist activity at rat 5HT4e receptor expressed in HEK293 cells assessed as cAMP level after 30 mins by HTRF assay	F	7.59	pEC50	26	nM	EC50	Eur J Med Chem (2015) 103: 289-301 [PMID:26363507]
ChEMBL	Partial agonist activity at rat 5HT4E receptor expressed in HEK293 cells assessed as cAMP accumulation incubated for 30 mins by HTRF assay	B	7.59	pEC50	26	nM	EC50	J Med Chem (2021) 64: 10641-10665 [PMID:34251799]

ChEMBL data shown on this page come from version 36:

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]