GW5074 [Ligand Id: 8072] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL72365 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Huntingtin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5514] [UniProtKB: P42858] | ||||||||
| ChEMBL | Binding affinity to mutant HTT (unknown origin) mediated HD exon 1-72Q aggregation assessed as dissociation constant | B | 7 | pKd | 100 | nM | Kd | J Med Chem (2022) 65: 15993-16032 [PMID:36490325] |
| Kinesin-like protein KIF15 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3632454] [UniProtKB: Q9NS87] | ||||||||
| ChEMBL | Inhibition of recombinant His6-tagged Kif15 ATPase activity (N420 residues) (unknown origin) expressed in HeLa cells using microtubule as substrate preincubated for 15 mins followed by ATP addition and measured after 20 mins by ADP-Glo luminescence assay | B | 5.6 | pIC50 | 2500 | nM | IC50 | Bioorg Med Chem Lett (2019) 29: 148-154 [PMID:30528696] |
| Microtubule-associated proteins 1A/1B light chain 3B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4879514] [UniProtKB: Q9GZQ8] | ||||||||
| ChEMBL | Binding affinity to His8-tagged human LC3B expressed in Escherichia coli BL21 (DE3) assessed as dissociation constant | B | 6.33 | pKd | 467.7 | nM | Kd | Eur J Med Chem (2024) 270: 116345-116345 [PMID:38564826] |
| ChEMBL | Binding affinity to LC3B (unknown origin) assessed as dissociation constant | B | 7 | pKd | 100 | nM | Kd | J Med Chem (2022) 65: 15993-16032 [PMID:36490325] |
| Raf-1 proto-oncogene, serine/threonine kinase/RAF proto-oncogene serine/threonine-protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] | ||||||||
| ChEMBL | Inhibition of cRAF1 (unknown origin) | B | 8.05 | pIC50 | 9 | nM | IC50 | Eur J Med Chem (2016) 123: 858-894 [PMID:27543880] |
| GtoPdb | - | - | 8.05 | pIC50 | 9 | nM | IC50 | J Neurochem (2004) 90: 595-608 [PMID:15255937] |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Inhibition of PLK1 (unknown origin) by FRET-based homogeneous assay | B | 5.34 | pIC50 | 4600 | nM | IC50 | J Med Chem (2013) 56: 6069-6087 [PMID:23829549] |
| polo like kinase 4/Serine/threonine-protein kinase PLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3788] [GtoPdb: 2171] [UniProtKB: O00444] | ||||||||
| ChEMBL | Inhibition of N-terminal GST-tagged human PLK4 (1 to 391 amino acids) expressed in Escherichia coli using TMB as substrate after 30 mins by indirect ELISA assay | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2013) 56: 6069-6087 [PMID:23829549] |
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]
