ChEMBL ligand: CHEMBL3417009
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303] There should be some charts here, you may need to enable JavaScript!
Cholinesterase in Equus caballus [ChEMBL: CHEMBL5763] [UniProtKB: P81908] 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] Serotonin 4 (5-HT4) receptor in Guinea pig [ChEMBL: CHEMBL5017] [UniProtKB: O70528] There should be some charts here, you may need to enable JavaScript!
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720] 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
acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
ChEMBL	Inhibition of AChE (unknown origin)	B	7.8	pKi	16	nM	Ki	Eur J Med Chem (2019) 162: 234-248 [PMID:30447434]
ChEMBL	Inhibition of human erythrocyte AChE pre-incubated for 5 mins before acetylthiocholine iodide substrate by Ellman' method	B	7.8	pIC50	16	nM	IC50	J Med Chem (2015) 58: 3172-3187 [PMID:25793650]
ChEMBL	Mixed type competitive inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition measured every 1 min for 10 mins by Ellman's method	B	7.8	pIC50	16	nM	IC50	Eur J Med Chem (2018) 158: 463-477 [PMID:30243151]
ChEMBL	Inhibition of human erythrocyte AChE using acetylthiocholine iodide as substrate incubated for 5 mins followed by substrate addition by Ellman's method	B	7.8	pIC50	16	nM	IC50	Eur J Med Chem (2019) 169: 200-223 [PMID:30884327]
ChEMBL	Inhibition of human AChE using acetylthiocholine iodide as substrate preincubated for 5 mins followed by substrate addition and by DTNB reagent based Ellman's method	B	7.8	pIC50	16	nM	IC50	Bioorg Med Chem Lett (2022) 72: 128873-128873 [PMID:35779827]
GtoPdb	-	-	7.8	pIC50	16	nM	IC50	Proc Natl Acad Sci USA (2014) 111: E3825-30 [PMID:25157130]
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908]
ChEMBL	Inhibition of equine serum BuChE pre-incubated for 5 mins before butyrylthiocholine iodide substrate by Ellman' method	B	5.45	pIC50	3530	nM	IC50	J Med Chem (2015) 58: 3172-3187 [PMID:25793650]
5-HT4 receptor/Serotonin 4 (5-HT4) receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1875] [GtoPdb: 9] [UniProtKB: Q13639]
ChEMBL	Agonist activity at 5-HT4R (unknown origin)	B	7.98	pKi	10.4	nM	Ki	Eur J Med Chem (2019) 162: 234-248 [PMID:30447434]
ChEMBL	Displacement of [3H]GR113808 from human 5-HT4 receptor expressed in Chem-1 cell membrane incubated for 60 mins by radiometric scintillation counting analysis	B	7.98	pKi	10.4	nM	Ki	Bioorg Med Chem Lett (2022) 72: 128873-128873 [PMID:35779827]
ChEMBL	Displacement of [3H]-GR113808 from recombinant human 5-HT4BR expressed in membranes after 60 mins	B	8.02	pKi	9.5	nM	Ki	Eur J Med Chem (2019) 162: 234-248 [PMID:30447434]
ChEMBL	Displacement of [3H]GR113808 from human 5-HT4R membrane in Tris buffer assessed as inhibitory constant measured after 60 mins by filter binding method	B	8.18	pKi	6.6	nM	Ki	Eur J Med Chem (2019) 169: 200-223 [PMID:30884327]
ChEMBL	Activity at 5-HT4R (unknown origin) expressed in COS7 cells assessed as increase in sAPPalpha release	B	7.95	pEC50	11.3	nM	EC50	J Med Chem (2015) 58: 3172-3187 [PMID:25793650]
Serotonin 4 (5-HT4) receptor in Guinea pig (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5017] [UniProtKB: O70528]
ChEMBL	Displacement of [3H]GR113808 from 5-HT4R in guinea pig brain membranes incubated for 30 mins by radioligand binding assay	B	8.18	pKi	6.6	nM	Ki	J Med Chem (2015) 58: 3172-3187 [PMID:25793650]
sigma non-opioid intracellular receptor 1/Sigma opioid receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL287] [GtoPdb: 2552] [UniProtKB: Q99720]
ChEMBL	Displacement of [3H]-(+)-pentazocine from sigma-1 receptor in human Jurkat cell membranes after 2 hrs by liquid scintillation counting method	B	7.29	pKi	51	nM	Ki	Eur J Med Chem (2019) 162: 234-248 [PMID:30447434]

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]