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 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]
