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 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) |
| 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 35:
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]
