PF-8380 [Ligand Id: 9142] activity data from GtoPdb and ChEMBL
Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
| ChEMBL ligand: CHEMBL3186509 |
|---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
|
There should be some charts here, you may need to enable JavaScript!
|
| 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 | Negative allosteric modulation activity against human ATX using FS-3 as substrate preincubated for 45 mins followed by substrate addition and measured every 30 mins by multi-mode microplate reader | B | 8.43 | pIC50 | 3.7 | nM | IC50 | Eur J Med Chem (2022) 236: 114307-114307 [PMID:35436669] |
| 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 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 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 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 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 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 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 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 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 rat ATX lysoPLD activity using LPC as substrate assessed as reduction in choline release measured after 60 mins by HVA fluorescence based analysis | B | 5.55 | pIC50 | 2800 | nM | IC50 | J Med Chem (2022) 65: 6338-6351 [PMID:35440138] |
| 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 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]
