ML204 [Ligand Id: 4255] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1459962
  • acetylcholinesterase (Yt blood group)/Acetylcholinesterase in Human [ChEMBL: CHEMBL220] [GtoPdb: 2465] [UniProtKB: P22303]
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  • TRPC4 in Human [GtoPdb: 489] [UniProtKB: Q9UBN4]
  • TRPC4/Short transient receptor potential channel 4 in Mouse [ChEMBL: CHEMBL1741219] [GtoPdb: 489] [UniProtKB: Q9QUQ5]
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  • TRPC6/Short transient receptor potential channel 6 in Mouse [ChEMBL: CHEMBL1795081] [GtoPdb: 491] [UniProtKB: Q61143]
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  • TRPC5 in Human [GtoPdb: 490] [UniProtKB: Q9UL62]
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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 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]