EHop 016 [Ligand Id: 11061] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL3237589 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| Ras-related C3 botulinum toxin substrate 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6094] [UniProtKB: P63000] | ||||||||
| ChEMBL | Inhibition of Rac1 in human MDA-MB-231 cells assessed as reduction in Rac-GTP level after 24 hrs by ELISA-based pull down assay | B | 5.52 | pIC50 | 3000 | nM | IC50 | Bioorg Med Chem (2018) 26: 884-890 [PMID:29358027] |
| ChEMBL | Inhibition of Rac1 in human MDA-MB-231 cells by Western blotting based pulldown assay | B | 5.52 | pIC50 | 3000 | nM | IC50 | US-8884006-B2. Small-molecule inhibitors of Rac1 in metastatic breast cancer (2014) |
| ChEMBL | Inhibition of Rac1 in human MDA-MB-435 cells after 24 hrs by G-LISA assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | J Med Chem (2014) 57: 2953-2962 [PMID:24520998] |
| ChEMBL | Inhibition of Rac1 in human MDA-MB-435 cells incubated for 24 hrs by G-LISA Rac1 activation assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | US-8884006-B2. Small-molecule inhibitors of Rac1 in metastatic breast cancer (2014) |
| ChEMBL | Inhibition of Rac1 in human MDA-MB-435 cells incubated for 24 hrs by pull-down assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem (2023) 90: 117337-117337 [PMID:37253305] |
| ChEMBL | Inhibition of Vav2 binding to Rac1 G15A mutant in human MDA-MB-231 cells after 1 hr by pull down assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem (2018) 26: 884-890 [PMID:29358027] |
| ChEMBL | Inhibition of Rac1 in human MDA-MB-435 cells assessed as reduction in Rac-GTP level after 24 hrs by ELISA-based pull down assay | B | 5.96 | pIC50 | 1100 | nM | IC50 | Bioorg Med Chem (2018) 26: 884-890 [PMID:29358027] |
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]
