ChEMBL ligand: CHEMBL1376358
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!
butyrylcholinesterase/Butyrylcholinesterase in Human [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276] There should be some charts here, you may need to enable JavaScript!
TRPC3/Short transient receptor potential channel 3 in Human [ChEMBL: CHEMBL2417348] [GtoPdb: 488] [UniProtKB: Q13507] There should be some charts here, you may need to enable JavaScript!
TRPC4 in Human [GtoPdb: 489] [UniProtKB: Q9UBN4] TRPC4/Short transient receptor potential channel 4 in Mouse [ChEMBL: CHEMBL1741219] [GtoPdb: 489] [UniProtKB: Q9QUQ5] There should be some charts here, you may need to enable JavaScript!
TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62] TRPC5/Short transient receptor potential channel 5 in Mouse [ChEMBL: CHEMBL4523481] [GtoPdb: 490] [UniProtKB: Q9QX29] There should be some charts here, you may need to enable JavaScript!
TRPC6/Short transient receptor potential channel 6 in Mouse [ChEMBL: CHEMBL1795081] [GtoPdb: 491] [UniProtKB: Q61143] 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 human AchE using acetylthiocholine iodide as substrate incubated for 20 mins prior to substrate addition measured for 1 hr by Ellman's method	B	4	pIC50	>100000	nM	IC50	Bioorg Med Chem (2013) 21: 4218-4224 [PMID:23719283]
butyrylcholinesterase/Butyrylcholinesterase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914] [GtoPdb: 2471] [UniProtKB: P06276]
ChEMBL	Inhibition of human BuChE using butyrylthiocholine iodide as substrate incubated for 20 mins prior to substrate addition measured for 1 hr by Ellman's method	B	4.21	pIC50	61010	nM	IC50	Bioorg Med Chem (2013) 21: 4218-4224 [PMID:23719283]
TRPC3/Short transient receptor potential channel 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417348] [GtoPdb: 488] [UniProtKB: Q13507]
ChEMBL	Inhibition of human TRPC3 expressed in HEK293 cells assessed as reduction in carbachol-induced membrane potential by FMP-2 dye based assay	B	4.31	pIC50	48600	nM	IC50	J Med Chem (2019) 62: 7589-7602 [PMID:30943030]
TRPC4 in Human [GtoPdb: 489] [UniProtKB: Q9UBN4]
GtoPdb	As determined by the FMP assay using DAMGO to stimulate Gi/o via the coexpressed μ receptor.	-	4.99	pKi	10300	nM	Ki	J Med Chem (2019) 62: 7589-7602 [PMID:30943030]
GtoPdb	-	-	5.27	pIC50	5430	nM	IC50	Br J Pharmacol (2015) 172: 3495-509 [PMID:25816897]
TRPC4/Short transient receptor potential channel 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741219] [GtoPdb: 489] [UniProtKB: Q9QUQ5]
ChEMBL	Inhibition of mouse TRPC4 beta expressed in HEK293 cells co-expressing mu-opioid receptor assessed as reduction in DAMGO-induced membrane potential by FMP-2 dye based assay	B	4.99	pIC50	10300	nM	IC50	J Med Chem (2019) 62: 7589-7602 [PMID:30943030]
ChEMBL	Inhibition of mouse TRPC4 beta expressed in HEK293 cells co-expressing mu-opioid receptor assessed as reduction in DAMGO-induced intracellular calcium level in presence of mu-opioid receptor agonist DAMGO by Fluo-4AM dye based fluorescence assay	B	5.43	pIC50	3700	nM	IC50	J Med Chem (2019) 62: 7589-7602 [PMID:30943030]
TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62]
GtoPdb	As determined by the FMP assay using DAMGO to stimulate Gi/o via the coexpressed μ receptor.	-	5.09	pIC50	8200	nM	IC50	J Med Chem (2019) 62: 7589-7602 [PMID:30943030]
GtoPdb	-	-	5.09	pIC50	-	-	-	Br J Pharmacol (2015) 172: 3495-509 [PMID:25816897]
TRPC5/Short transient receptor potential channel 5 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523481] [GtoPdb: 490] [UniProtKB: Q9QX29]
ChEMBL	Inhibition of mouse TRPC5 expressed in HEK293 cells co-expressing mu-opioid receptor assessed as reduction in DAMGO-induced membrane potential by FMP-2 dye based assay	B	5.09	pIC50	8200	nM	IC50	J Med Chem (2019) 62: 7589-7602 [PMID:30943030]
TRPC6/Short transient receptor potential channel 6 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795081] [GtoPdb: 491] [UniProtKB: Q61143]
ChEMBL	Inhibition of mouse TRPC6 expressed in HEK293 cells co-expressing M5 receptor assessed as reduction in carbachol-induced membrane potential by FMP-2 dye based assay	B	4.22	pIC50	59600	nM	IC50	J Med Chem (2019) 62: 7589-7602 [PMID:30943030]

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]