NAV2729 [Ligand Id: 14182] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3716578 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Fatty acid transport protein 2/Long-chain fatty acid transport protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4326] [GtoPdb: 1109] [UniProtKB: O14975] | ||||||||
| ChEMBL | Inhibition of FATP2 in human HepG2 cells assessed as decrease in fatty acid transport after 5 mins by trypan blue dye based fluorescence quenching method | B | 5.2 | pIC50 | 6300 | nM | IC50 | Medchemcomm (2016) 7: 612-622 [PMID:27446528] |
| PAS domain containing serine/threonine kinase/PAS domain-containing serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6054] [GtoPdb: 2139] [UniProtKB: Q96RG2] | ||||||||
| ChEMBL | Inhibition of purified full-length human PASK expressed in insect cells using MBP protein substrate incubated for 10 mins before ATP addition and measured after 1 hr by kinase-Glo luminescent kinase assay | B | 5 | pIC50 | <=10000 | nM | IC50 | WO-2012149157-A2. Heterocyclic compounds for the inhibition of pask (2012) |
| ChEMBL | Inhibition of purified human PASK kinase domain expressed in insect cells using MBP protein substrate incubated for 10 mins before ATP addition and measured after 1 hr by kinase-Glo luminescent kinase assay | B | 5 | pIC50 | <=10000 | nM | IC50 | WO-2012149157-A2. Heterocyclic compounds for the inhibition of pask (2012) |
| ChEMBL | Inhibition of purified human PASK kinase domain expressed in insect cells incubated for 10 mins using MBP protein by kinase-Glo luminescent kinase assay | B | 5 | pIC50 | <=10000 | nM | IC50 | US-20120277224-A1. Heterocyclic compounds for the inhibition of pask (2012) |
| ChEMBL | Inhibition of purified human PASK expressed in insect cells incubated for 10 mins using MBP protein by kinase-Glo luminescent kinase assay | B | 5 | pIC50 | <=10000 | nM | IC50 | US-20120277224-A1. Heterocyclic compounds for the inhibition of pask (2012) |
| ChEMBL | Kinase Luminescence Assay: Table 1: One assay for purified hPASK activity utilizes the Kinase-Glo Luminescent Kinase Assay (Promega), which quantifies the amount of ATP remaining in solution following kinase reaction. The assay is carried out in a 96-well plate format and is performed by adding a volume of Kinase-Glo Reagent (Promega, catalog #V3771) equal to the volume of solution in the well of a completed kinase reaction. Kinase-Glo reagent contains Luciferase and its substrate. After addition to a kinase reaction it allows to measure luminescence. The amount of ATP left in solution at the time of Kinase-Glo Plus addition is directly proportional to the luminescence that is measured in each well, and inversely correlated with kinase activity.Purified hPASK from insect cells (0.02 μg) is added to a 50 μL reaction mix containing 40 mM HEPES (pH 7.0), 100 mM KCl, 5 mM MgCl2, 1 mM DTT and 1 μg of MBP protein. Inhibitory compounds are then added and the mixture is incubated for 10 min at 25° C. before adding 5 μL of ATP (at desired concentration). The reaction is allowed to proceed at 25° C. for 1 hour before adding 50 μL of Kinase-Glo reagent. The luminescence is measured as soon as 10 minutes after Kinase-Glo reagent is added. | B | 5 | pIC50 | <10000 | nM | IC50 | US-10953012-B2. Heterocyclic compounds for the inhibition of pask (2021) |
| PH and SEC7 domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523105] [UniProtKB: A5PKW4] | ||||||||
| ChEMBL | Inhibition of N-terminal His-tagged and N-terminal alpha-helix lacking Arf6 (14 to 175 residues) (unknown origin) expressed in Escherichia coli using 20 nM Arf6 in presence of ARNO (50 to 255 residues) incubated for 1 hr by fluorometric high throughput assay | B | 5.74 | pIC50 | 1800 | nM | IC50 | US-20170189405-A1. Arf6 inhibitors and methods of synthesis and use thereof (2017) |
| ChEMBL | Inhibition of N-terminal His-tagged and N-terminal alpha-helix lacking Arf6 (14 to 175 residues) (unknown origin) expressed in Escherichia coli using 200 nM Arf6 in presence of ARNO (50 to 255 residues) incubated for 1 hr by fluorometric high throughput assay | B | 5.85 | pIC50 | 1400 | nM | IC50 | US-20170189405-A1. Arf6 inhibitors and methods of synthesis and use thereof (2017) |
| ARF GTPase 6 in Human [GtoPdb: 3324] [UniProtKB: P62330] | ||||||||
| GtoPdb | Evaluation of NAV2729 inhibitory potency in a fluorometric nucleotide exchange assay | - | 6 | pIC50 | 1000 | nM | IC50 | Cancer Cell (2016) 29: 889-904 [PMID:27265506] |
ChEMBL data shown on this page come from version 36:
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]
