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 |
|---|---|---|---|---|---|---|---|---|
| casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400] | ||||||||
| ChEMBL | Inhibition of human CK2A using RRRDDDSDDD as substrate by [gamma-33P]-ATP assay | B | 6.55 | pIC50 | 279 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20] | ||||||||
| ChEMBL | Inhibition of human DYRK4 using RRRFRPASPLRGPPK as substrate by [gamma-33P]-ATP assay | B | 5.36 | pIC50 | 4380 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| 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 LC3B (unknown origin) assessed as dissociation constant | B | 7 | pKd | 100 | nM | Kd | J Med Chem (2022) 65: 15993-16032 [PMID:36490325] |
| ZAK sterile alpha motif and leucine zipper containing kinase AZK/Mixed lineage kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3886] [GtoPdb: 2289] [UniProtKB: Q9NYL2] | ||||||||
| ChEMBL | Inhibition of human ZAK using MBP as substrate by [gamma-33P]-ATP assay | B | 5.72 | pIC50 | 1890 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| Myocilin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105967] [UniProtKB: Q99972] | ||||||||
| ChEMBL | Binding affinity myocilin-OLF domain (unknown origin) by SRP assay | B | 4.47 | pKd | 33500 | nM | Kd | Bioorg Med Chem Lett (2017) 27: 4133-4139 [PMID:28739043] |
| receptor interacting serine/threonine kinase 3/Receptor-interacting serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795199] [GtoPdb: 2191] [UniProtKB: Q9Y572] | ||||||||
| ChEMBL | Inhibition of human RIPK3 using MBP as substrate by [gamma-33P]-ATP assay | B | 5.27 | pIC50 | 5400 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| A-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase A-Raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1169596] [GtoPdb: 1933] [UniProtKB: P10398] | ||||||||
| ChEMBL | Inhibition of human ARAF using MEK1 as substrate by [gamma-33P]-ATP assay | B | 7.84 | pIC50 | 14.6 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| B-Raf proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase B-raf in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5145] [GtoPdb: 1943] [UniProtKB: P15056] | ||||||||
| ChEMBL | Inhibition of human BRAF using MEK1 (K97R) as substrate by [gamma-33P]-ATP assay | B | 7.53 | pIC50 | 29.3 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| ChEMBL | Inhibition of human BRAF V600E mutant using myelin basic protein as substrate measured after 40 mins in presence of [gamma33P-ATP] by scintillation counting method | B | 7.89 | pIC50 | 13 | nM | IC50 | Bioorg Med Chem (2019) 27: 655-663 [PMID:30660499] |
| ChEMBL | Inhibition of BRAF (unknown origin) in presence of ATP | B | 7.89 | pIC50 | 12.8 | nM | IC50 | Eur J Med Chem (2020) 207: 112710-112710 [PMID:32961435] |
| ChEMBL | Inhibition of human BRAF using MEK1 (K97R) as substrate in presence of [gamma-33P]ATP by scintillation counting method | B | 7.9 | pIC50 | 12.6 | nM | IC50 | Eur J Med Chem (2020) 208: 112756-112756 [PMID:32942186] |
| ChEMBL | Inhibition of BRAF (unknown origin) | B | 7.97 | pIC50 | 10.71 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3600-3604 [PMID:24878193] |
| ChEMBL | Inhibition of human BRAF V600E mutant using MEK1 (K97R) as substrate in presence of [gamma-33P]ATP by scintillation counting method | B | 8.13 | pIC50 | 7.49 | nM | IC50 | Eur J Med Chem (2020) 208: 112756-112756 [PMID:32942186] |
| ChEMBL | Inhibition of BRAF V600E mutant (unknown origin) using MEK1 (K97R) as substrate in presence of [gamma-33P]ATP by radiometric assay | B | 8.24 | pIC50 | 5.8 | nM | IC50 | RSC Med Chem (2022) 13: 731-736 [PMID:35814929] |
| ChEMBL | Inhibition of BRAF V599E mutant (unknown origin) | B | 8.27 | pIC50 | 5.4 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3600-3604 [PMID:24878193] |
| ChEMBL | Inhibition of BRAF (unknown origin) in presence of ATP by Lanthascreen TR-FRET assay | B | 8.43 | pIC50 | 3.7 | nM | IC50 | Eur J Med Chem (2021) 217: 113327-113327 [PMID:33730678] |
| ChEMBL | Inhibition of B-Raf V600E mutant (unknown origin) using fluorescein-MAP2K1 as substrate after 1 hr by electrophoretic assay | B | 8.82 | pIC50 | 1.5 | nM | IC50 | Medchemcomm (2017) 8: 1835-1844 [PMID:30108894] |
| 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] |
| Raf-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase RAF in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1906] [GtoPdb: 2184] [UniProtKB: P04049] | ||||||||
| ChEMBL | Inhibition of human RAF1 using MEK1 as substrate by [gamma-33P]-ATP assay | B | 7.97 | pIC50 | 10.6 | nM | IC50 | Eur J Med Chem (2019) 161: 456-467 [PMID:30384048] |
| ChEMBL | Inhibition of Raf-1 (unknown origin) | B | 8.05 | pIC50 | 9 | nM | IC50 | J Med Chem (2022) 65: 9580-9606 [PMID:35802779] |
| 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] |
| ChEMBL | Inhibition of human CRAF using MEK1 (K97R) as substrate in presence of [gamma-33P]ATP by scintillation counting method | B | 8.13 | pIC50 | 7.36 | nM | IC50 | Eur J Med Chem (2020) 208: 112756-112756 [PMID:32942186] |
| ChEMBL | Inhibition of cRAF1 (unknown origin) at 10 uM | B | 8.36 | pIC50 | 4.4 | nM | IC50 | Bioorg Med Chem Lett (2014) 24: 3600-3604 [PMID:24878193] |
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]
