bromoenol lactone [Ligand Id: 5149] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL6206
  • iPLA2-G6/85/88 kDa calcium-independent phospholipase A2 in Human [ChEMBL: CHEMBL3213] [GtoPdb: 1431] [UniProtKB: O60733]
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  • Fatty acid amide hydrolase/Fatty-acid amide hydrolase 1 in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
  • Fatty acid amide hydrolase/Fatty-acid amide hydrolase 1 in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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  • TRPC5/Short transient receptor potential channel 5 in Human [ChEMBL: CHEMBL1250411] [GtoPdb: 490] [UniProtKB: Q9UL62]
  • TRPC5 in Mouse [GtoPdb: 490] [UniProtKB: Q9QX29]
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  • TRPC6/Short transient receptor potential channel 6 in Human [ChEMBL: CHEMBL2417347] [GtoPdb: 491] [UniProtKB: Q9Y210]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
iPLA2-G6/85/88 kDa calcium-independent phospholipase A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3213] [GtoPdb: 1431] [UniProtKB: O60733]
ChEMBL Compounds were evaluated for the inhibitory activity against canine myocardial cytosolic calcium dependent phospholipase A2. B 6.85 pIC50 140 nM IC50 J Med Chem (1993) 36: 95-100 [PMID:8421294]
ChEMBL Compounds were evaluated for the inhibitory activity against canine myocardial cytosolic calcium dependent phospholipase A2. B 7 pIC50 >100 nM IC50 J Med Chem (1993) 36: 95-100 [PMID:8421294]
Fatty acid amide hydrolase/Fatty-acid amide hydrolase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
ChEMBL Irreversible inhibition of fatty acid amide hydrolase B 6.1 pIC50 800 nM IC50 J Med Chem (2005) 48: 5059-5087 [PMID:16078824]
Fatty acid amide hydrolase/Fatty-acid amide hydrolase 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
ChEMBL Inhibition of FAAH in rat brain assessed as hydrolysis of anandamide B 6.1 pIC50 800 nM IC50 J Med Chem (2008) 51: 7327-7343 [PMID:18983142]
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364]
ChEMBL Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR green assay F 4.8 pIC50 15848.93 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
ChEMBL Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay F 5 pIC50 10000 nM IC50 Nat Chem Biol (2009) 5: 765-771 [PMID:19734910]
TRPC5/Short transient receptor potential channel 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1250411] [GtoPdb: 490] [UniProtKB: Q9UL62]
ChEMBL Antagonist activity at TRPC5 (unknown origin) assessed as inhibition of channel activity B 4.97 pIC50 10600 nM IC50 Eur J Med Chem (2024) 265: 116066-116066 [PMID:38185057]
TRPC5 in Mouse [GtoPdb: 490] [UniProtKB: Q9QX29]
GtoPdb - - 4.97 pIC50 - - - J Pharmacol Exp Ther (2011) 339: 329-40 [PMID:21795434]
TRPC6/Short transient receptor potential channel 6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2417347] [GtoPdb: 491] [UniProtKB: Q9Y210]
ChEMBL Antagonist activity at TRPC6 (unknown origin) assessed as inhibition of channel activity B 5.14 pIC50 7200 nM IC50 Eur J Med Chem (2024) 265: 116066-116066 [PMID:38185057]

ChEMBL data shown on this page come from version 36:

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]