PF-8380 [Ligand Id: 9142] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3186509 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| autotaxin/Autotaxin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3691] [GtoPdb: 2901] [UniProtKB: Q13822] | ||||||||
| ChEMBL | Inhibition of ATX in human plasma assessed as decrease in hydrolysis of lysophosphatidylcholine by measuring choline release after 24 hrs by horseradish peroxidase/choline oxidase-coupled assay | B | 6.54 | pIC50 | 289 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5403-5410 [PMID:27780639] |
| ChEMBL | Inhibition of ATX in human whole blood assessed as decrease in LPA levels after 2 hrs by LC-MS/MS method | B | 7 | pIC50 | 101 | nM | IC50 | J Med Chem (2018) 61: 3697-3711 [PMID:29620892] |
| ChEMBL | Inhibition of autotaxin in healthy human whole blood assessed as reduction in LPA level after 2 hrs by LC-MS/MS analysis | B | 7 | pIC50 | 100 | nM | IC50 | ACS Med Chem Lett (2016) 7: 857-861 [PMID:27660691] |
| ChEMBL | Inhibition of autotaxin in healthy human plasma assessed as reduction in LPA level after 3 hrs by mass spectrometric analysis | B | 7.36 | pIC50 | 44 | nM | IC50 | ACS Med Chem Lett (2016) 7: 857-861 [PMID:27660691] |
| ChEMBL | Inhibition of recombinant full length human C-terminal His-tagged autotaxin expressed in human 293E cells assessed as choline release using lysophosphatidylcholine as substrate after 1 hr by Amplex red fluorescence assay | B | 8.08 | pIC50 | 8.4 | nM | IC50 | ACS Med Chem Lett (2016) 7: 857-861 [PMID:27660691] |
| ChEMBL | Inhibition of human C-terminal His6-tagged ATX beta expressed in Sf9 insect cells using FS-3 as substrate preincubated for 45 mins followed by substrate addition and measured at 1 min interval for 30 mins by fluorescence assay | B | 8.37 | pIC50 | 4.3 | nM | IC50 | Eur J Med Chem (2020) 201: 112456-112456 [PMID:32535330] |
| ChEMBL | Inhibition of human ATX expressed in HEK293 cells using FS-3 as substrate after 15 mins | B | 8.52 | pIC50 | 3 | nM | IC50 | J Med Chem (2017) 60: 2006-2017 [PMID:28165241] |
| ChEMBL | Inhibition of human recombinant ATX using Rac-1-Palmitoyl-glycero-3-phosphocholine as substrate incubated for 2 hrs using ADHP fluorogenic peroxidase substrate by horseradish peroxidase/choline oxidase-coupled assay | B | 8.52 | pIC50 | 3 | nM | IC50 | Bioorg Med Chem Lett (2016) 26: 5403-5410 [PMID:27780639] |
| ChEMBL | Inhibition of human full length ATX expressed in HEK cells using FS-3 as substrate incubated for 15 mins followed by substrate addition measured after 30 mins | B | 8.52 | pIC50 | 3 | nM | IC50 | ACS Med Chem Lett (2017) 8: 1252-1257 [PMID:29259743] |
| ChEMBL | Inhibition of recombinant human ATX expressed in HEK293 cells using FS3 as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins | B | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2016) 59: 5604-5621 [PMID:26745766] |
| ChEMBL | Inhibition of human ATX expressed in HEK293 cells using FS-3 as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins | B | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2017) 60: 722-748 [PMID:27982588] |
| ChEMBL | Inhibition of recombinant human ATX beta expressed in HEK293 cells using FS-3 as substrate pretreated for 15 mins followed by substrate addition measured after 30 mins | B | 8.55 | pIC50 | 2.8 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4156-4164 [PMID:28743508] |
| ChEMBL | Inhibition of recombinant ATX (unknown origin) expressed in HEK293 cells using FS-3 as substrate after 15 mins | B | 8.55 | pIC50 | 2.8 | nM | IC50 | Bioorg Med Chem (2016) 24: 4660-4674 [PMID:27544588] |
| ChEMBL | Inhibition of human ATX by fluorogenic substrate-3 assay | B | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2020) 63: 7326-7346 [PMID:32479084] |
| ChEMBL | Inhibition of human ATX pre-incubated for 45 mins before fluorogenic substrate-3 addition and measured every minute for 30 mins by fluorescence based assay | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2020) 63: 7326-7346 [PMID:32479084] |
| ChEMBL | Inhibition of recombinant human ATX beta expressed in HEK293 cells using LPC as substrate measured after 30 mins by LC-MS/MS analysis | B | 8.77 | pIC50 | 1.7 | nM | IC50 | Bioorg Med Chem Lett (2017) 27: 4156-4164 [PMID:28743508] |
| GtoPdb | - | - | 8.77 | pIC50 | 1.7 | nM | IC50 |
J Pharmacol Exp Ther (2010) 334: 310-7 [PMID:20392816]; Arch Pharm (Weinheim) (2013) 346: 91-7 [PMID:23300119] |
| ChEMBL | Inhibition of ATX (unknown origin) assessed as decrease in choline release | B | 8.96 | pIC50 | 1.1 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2279-2284 [PMID:29798825] |
| autotaxin in Human [GtoPdb: 2901] [UniProtKB: Q13822] | ||||||||
| GtoPdb | - | - | 8.77 | pIC50 | 1.7 | nM | IC50 |
J Pharmacol Exp Ther (2010) 334: 310-7 [PMID:20392816]; Arch Pharm (Weinheim) (2013) 346: 91-7 [PMID:23300119] |
| autotaxin/Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3826871] [GtoPdb: 2901] [UniProtKB: Q9R1E6] | ||||||||
| ChEMBL | Inhibition of recombinant mouse ATX expressed in HEK293 cells using FS3 as substrate preincubated for 15 mins followed by substrate addition measured after 30 mins | B | 8.55 | pIC50 | 2.8 | nM | IC50 | J Med Chem (2018) 61: 3697-3711 [PMID:29620892] |
| ChEMBL | Inhibition of recombinant mouse ATX expressed in HEK293 cells using LPC 17:0 as substrate after 30 mins by LC-MS/MS method | B | 8.77 | pIC50 | 1.7 | nM | IC50 | J Med Chem (2018) 61: 3697-3711 [PMID:29620892] |
| autotaxin/Ectonucleotide pyrophosphatase/phosphodiesterase family member 2 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3826870] [GtoPdb: 2901] [UniProtKB: Q64610] | ||||||||
| ChEMBL | Inhibition of ATX in rat whole blood using LPA 17:0 as substrate after 1 hr by LC-MS/MS analysis | B | 6.51 | pIC50 | 307 | nM | IC50 | ACS Med Chem Lett (2017) 8: 1252-1257 [PMID:29259743] |
| Kv11.1/HERG in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL240] [GtoPdb: 572] [UniProtKB: Q12809] | ||||||||
| ChEMBL | Displacement of [3H]dofetilide from human ERG expressed in HEK293 cells after 45 mins by scintillation counting method | B | 5.57 | pIC50 | 2700 | nM | IC50 | Bioorg Med Chem Lett (2018) 28: 2279-2284 [PMID:29798825] |
| ChEMBL | Inhibition of human ERG expressed in HEK293 cells by patch clamp assay | B | 6.32 | pIC50 | 480 | nM | IC50 | ACS Med Chem Lett (2017) 8: 1252-1257 [PMID:29259743] |
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]
