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ChEMBL ligand: CHEMBL1376358 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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]