ML204 [Ligand Id: 4255] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1459962 |
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| 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 recombinant acetylcholinesterase expressed in HEK-293 cells using AMTch as substrate after 30 mins by spectrophotometric method | B | 6.08 | pIC50 | 840 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| TRPC4 in Human [GtoPdb: 489] [UniProtKB: Q9UBN4] | ||||||||
| GtoPdb | - | - | 5.5 | pIC50 | 2900 | nM | IC50 | J Biol Chem (2011) 286: 33436-46 [PMID:21795696] |
| TRPC4/Short transient receptor potential channel 4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1741219] [GtoPdb: 489] [UniProtKB: Q9QUQ5] | ||||||||
| GtoPdb | - | - | 5.54 | pIC50 | 2910 | nM | IC50 | J Biol Chem (2011) 286: 33436-46 [PMID:21795696] |
| ChEMBL | Inhibition of mouse TRPC4 beta expressed in HEK293 cells co-expressing mu-opioid receptor assessed as reduction in DAMGO-induced current by QPatch clamp assay | B | 5.59 | pIC50 | 2600 | 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 | 6.02 | pIC50 | 960 | 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 HA-tagged mouse TRPC6 expressed in HEK293 cells assessed as reduction in acetylcholine-induced membrane potential by FLIPR membrane potential dye based assay | B | 4.75 | pIC50 | 17900 | nM | IC50 | J Med Chem (2019) 62: 7589-7602 [PMID:30943030] |
| TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62] | ||||||||
| GtoPdb | - | - | 5 | pIC50 | ~10000 | nM | IC50 | J Biol Chem (2011) 286: 33436-46 [PMID:21795696] |
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]
