RHC80267 [Ligand Id: 5255] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL158897
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Human [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
  • Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
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  • PLA2-G7/LDL-associated phospholipase A2 in Human [ChEMBL: CHEMBL3514] [GtoPdb: 1432] [UniProtKB: Q13093]
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  • LIP1, secretory lipase (Family 3) in Malassezia globosa (strain ATCC MYA-4612 / CBS 7966)(Dandruff-associated fungus) [ChEMBL: CHEMBL3608197] [UniProtKB: A8PUY1]
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  • αβ-Hydrolase 12/Monoacylglycerol lipase ABHD12 in Human [ChEMBL: CHEMBL5516] [GtoPdb: 3070] [UniProtKB: Q8N2K0]
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  • Neutral cholesterol ester hydrolase 1 in Human [ChEMBL: CHEMBL5048] [UniProtKB: Q6PIU2]
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  • Diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Human [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
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  • Diacylglycerol lipase β/Sn1-specific diacylglycerol lipase beta in Human [ChEMBL: CHEMBL5521] [GtoPdb: 1397] [UniProtKB: Q8NCG7]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
Fatty acid amide hydrolase/Anandamide amidohydrolase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2243] [GtoPdb: 1400] [UniProtKB: O00519]
ChEMBL Inhibition of recombinant FAAH transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe B 4.15 pIC50 70000 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5838-5841 [PMID:18657971]
Fatty acid amide hydrolase/Anandamide amidohydrolase in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3229] [GtoPdb: 1400] [UniProtKB: P97612]
ChEMBL Inhibition of rat histidine tagged FAAH expressed in Escherichia coli by coumarin ester substrate fluorescence assay B 5.65 pIC50 2240 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 4585-4592 [PMID:22738638]
PLA2-G7/LDL-associated phospholipase A2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3514] [GtoPdb: 1432] [UniProtKB: Q13093]
ChEMBL Inhibition of recombinant PLA2g7 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe B 4.96 pIC50 11000 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5838-5841 [PMID:18657971]
LIP1, secretory lipase (Family 3) in Malassezia globosa (strain ATCC MYA-4612 / CBS 7966)(Dandruff-associated fungus) (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3608197] [UniProtKB: A8PUY1]
ChEMBL Inhibition of Malassezia globosa CBS 7966 LIP1 using pNPA substrate B 4.12 pIC50 75250 nM IC50 Bioorg. Med. Chem. Lett. (2015) 25: 3464-3467 [PMID:26199121]
αβ-Hydrolase 12/Monoacylglycerol lipase ABHD12 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5516] [GtoPdb: 3070] [UniProtKB: Q8N2K0]
ChEMBL Inhibition of recombinant ABHD12 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe B 4 pIC50 >100000 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5838-5841 [PMID:18657971]
Neutral cholesterol ester hydrolase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5048] [UniProtKB: Q6PIU2]
ChEMBL Inhibition of recombinant KIAA1363 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe B 5 pIC50 10000 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5838-5841 [PMID:18657971]
Protein BAT5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6168] [UniProtKB: O95870]
ChEMBL Inhibition of recombinant BAT5 transfected in HEK293T cells by SDS-PAGE using rhodamine-tagged FP probe B 4.64 pIC50 23000 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5838-5841 [PMID:18657971]
Diacylglycerol lipase α/Sn1-specific diacylglycerol lipase alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5545] [GtoPdb: 1396] [UniProtKB: Q9Y4D2]
ChEMBL Inhibition of human DAGLalpha B 4.19 pIC50 65000 nM IC50 Bioorg. Med. Chem. Lett. (2012) 22: 4585-4592 [PMID:22738638]
GtoPdb - - 4.19 pIC50 65000 nM IC50 Bioorg Med Chem Lett (2012) 22: 4585-92 [PMID:22738638]
ChEMBL Inhibition of human C-terminal HA-tagged DAGLalpha expressed in HEK293F cell membrane fractions using DiFMU-octanoate as substrate by fluorogenic surrogate substrate assay B 4.6 pIC50 25118.86 nM IC50 Bioorg Med Chem Lett (2016) 26: 3831-3837 [PMID:27394666]
ChEMBL Inhibition of human C-terminal HA-tagged DAGLalpha expressed in HEK293F cell membrane fractions using DiFMU-octanoate as substrate by fluorogenic surrogate substrate assay B 4.6 pIC50 25118.86 nM IC50 Bioorg Med Chem Lett (2016) 26: 3831-3837 [PMID:27394666]
ChEMBL Inhibition of human C-terminal HA-tagged DAGLalpha expressed in HEK293F cell membrane fractions using PNP butyrate as substrate by colorimetric surrogate substrate assay B 5.3 pIC50 5011.87 nM IC50 Bioorg Med Chem Lett (2016) 26: 3831-3837 [PMID:27394666]
ChEMBL Inhibition of human C-terminal HA-tagged DAGLalpha expressed in HEK293F cell membrane fractions using PNP butyrate as substrate by colorimetric surrogate substrate assay B 5.3 pIC50 5011.87 nM IC50 Bioorg Med Chem Lett (2016) 26: 3831-3837 [PMID:27394666]
ChEMBL Inhibition of human recombinant DAGLalpha overexpressed in african green monkey COS7 cells B 7.22 pIC50 60 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5838-5841 [PMID:18657971]
Diacylglycerol lipase β/Sn1-specific diacylglycerol lipase beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5521] [GtoPdb: 1397] [UniProtKB: Q8NCG7]
ChEMBL Inhibition of human recombinant DAGLbeta overexpressed in african green monkey COS7 cells B 7.22 pIC50 60 nM IC50 Bioorg. Med. Chem. Lett. (2008) 18: 5838-5841 [PMID:18657971]

ChEMBL data shown on this page come from version 28:

Gaulton A, Hersey A, Nowotka M, Bento AP, Chambers J, Mendez D, Mutowo P, Atkinson F, Bellis LJ, CibriƔn-Uhalte E, Davies M, Dedman N, Karlsson A, MagariƱos MP, Overington JP, Papadatos G, Smit I, Leach AR. (2017) 'The ChEMBL database in 2017.' Nucleic Acids Res., 45(D1). DOI: 10.1093/nar/gkw1074. [PMCID:5210557]