PD-146176 [Ligand Id: 11390] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL180917 (PD-146176) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| 15-LOX-1/Arachidonate 15-lipoxygenase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2903] [GtoPdb: 1388] [UniProtKB: P16050] | ||||||||
| ChEMBL | Competitive inhibition of human 15-LOX1 using linoleic acid as substrate after 10 mins by Lineweaver-Burk plot analysis | B | 5.42 | pKi | 3810 | nM | Ki | J Med Chem (2015) 58: 7850-7862 [PMID:26331552] |
| ChEMBL | Competitive inhibition of human 15-LOX-1 assessed as reduction in conversion of linoleic acid to 13(S)-HpODE incubated for 10 mins followed by linoleic acid addition by Lineweaver-Burk plot analysis | B | 5.42 | pKi | 3810 | nM | Ki | Eur J Med Chem (2016) 122: 786-801 [PMID:27477687] |
| GtoPdb | - | - | 6.7 | pKi | - | - | - | Br J Pharmacol (1997) 120: 1199-206 [PMID:9105693] |
| ChEMBL | Inhibition of human 12/15-LOX expressed in HEK293 cells after 30 mins by microplate reader analysis | B | 6.09 | pIC50 | 810 | nM | IC50 | Bioorg Med Chem (2016) 24: 1183-1190 [PMID:26899595] |
| Arachidonate 15-lipoxygenase in Rabbit (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4358] [UniProtKB: P12530] | ||||||||
| ChEMBL | Inhibitory concentration against isolated rabbit reticulocyte 15-lipoxygenase measured in the presence of linoleic acid | B | 5.42 | pIC50 | 3810 | nM | IC50 | Bioorg Med Chem Lett (2005) 15: 1435-1440 [PMID:15713402] |
| ChEMBL | Inhibition of rabbit reticulocyte 15-LOX using [14C]-linoleic acid as substrate preincubated for 15 mins followed by substrate addition by RP-HPLC analysis | B | 5.42 | pIC50 | 3810 | nM | IC50 | J Med Chem (2019) 62: 4624-4637 [PMID:30964295] |
| ChEMBL | Inhibition of 15LOX in rabbit reticulocytes by EIA assay | B | 5.95 | pIC50 | 1120 | nM | IC50 | J Nat Prod (2007) 70: 859-862 [PMID:17378609] |
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]
