ChEMBL ligand: CHEMBL33884 (GR-113808)
Plasmodium falciparum [ChEMBL: CHEMBL364] There should be some charts here, you may need to enable JavaScript!
5-HT3A/5-HT3B/Serotonin 3 (5-HT3) receptor in Rat [ChEMBL: CHEMBL2094116] [GtoPdb: 373, 374] [UniProtKB: P35563, Q9JJ16] There should be some charts here, you may need to enable JavaScript!
5-HT3A/Serotonin 3a (5-HT3a) receptor in Human [ChEMBL: CHEMBL1899] [GtoPdb: 373] [UniProtKB: P46098] There should be some charts here, you may need to enable JavaScript!
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639] 5-HT4 receptor in Mouse [GtoPdb: 9] [UniProtKB: P97288] 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] 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 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	Antagonist activity at 5-HT4 receptor in human HeLa cells assessed as inhibition of intracellular calcium mobilization incubated for 2 hrs by FLIPR assay	B	8.85	pKi	1.4	nM	Ki	Bioorg Med Chem (2023) 84: 117256-117256 [PMID:37003157]
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	J Neurochem (1997) 69: 1810-9 [PMID:9349523]; J Neurochem (1998) 70: 2252-61 [PMID:9603189]; Neuroreport (1997) 8: 3189-96 [PMID:9351641]; J Neurochem (2000) 74: 478-89 [PMID:10646498]; Naunyn Schmiedebergs Arch Pharmacol (2001) 363: 146-60 [PMID:11218067]; Br J Pharmacol (2000) 131: 827-35 [PMID:11030734]; Br J Pharmacol (2004) 143: 361-70 [PMID:15351779]
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 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]