Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | nuclear factor, erythroid 2-like 2 | Starlite/ChEMBL | References |
Homo sapiens | kelch-like ECH-associated protein 1 | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Brugia malayi | Kelch motif family protein | kelch-like ECH-associated protein 1 | 624 aa | 565 aa | 31.1 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Onchocerca volvulus | 0 | 0 | 0.5 | |
Schistosoma mansoni | hypothetical protein | 0 | 0.0003 | 0.0003 |
Brugia malayi | hypothetical protein | 0.0043 | 0.3781 | 1 |
Brugia malayi | Kelch motif family protein | 0 | 0.0003 | 0.0007 |
Schistosoma mansoni | hypothetical protein | 0 | 0.0003 | 0.0003 |
Echinococcus granulosus | kelch protein 12 | 0 | 0.0003 | 0.0003 |
Onchocerca volvulus | 0 | 0 | 0.5 | |
Echinococcus multilocularis | kelch protein 10 | 0 | 0.0003 | 0.0003 |
Loa Loa (eye worm) | kelch domain-containing protein family protein | 0 | 0.0003 | 1 |
Onchocerca volvulus | 0 | 0 | 0.5 | |
Brugia malayi | Kelch-like protein X | 0 | 0.0003 | 0.0007 |
Loa Loa (eye worm) | Klhl5 protein | 0 | 0.0003 | 1 |
Echinococcus multilocularis | kelch protein 18 | 0 | 0.0003 | 0.0003 |
Brugia malayi | BTB/POZ domain containing protein | 0 | 0.0003 | 0.0007 |
Echinococcus multilocularis | kelch protein 12 | 0 | 0.0003 | 0.0003 |
Echinococcus granulosus | kelch protein 18 | 0 | 0.0003 | 0.0003 |
Schistosoma mansoni | hypothetical protein | 0 | 0.0003 | 0.0003 |
Echinococcus granulosus | kelch protein 3 | 0 | 0.0003 | 0.0003 |
Echinococcus multilocularis | kelch protein 3 | 0 | 0.0003 | 0.0003 |
Echinococcus multilocularis | kelch ECH associated protein 1 | 0.0114 | 0.9972 | 0.9972 |
Entamoeba histolytica | hypothetical protein | 0.0043 | 0.3781 | 0.5 |
Echinococcus multilocularis | ectoderm neural cortex protein 1 | 0 | 0.0003 | 0.0003 |
Echinococcus multilocularis | Basic leucine zipper (bZIP) transcription | 0.0043 | 0.3781 | 0.3781 |
Entamoeba histolytica | hypothetical protein | 0.0043 | 0.3781 | 0.5 |
Onchocerca volvulus | 0 | 0 | 0.5 | |
Schistosoma mansoni | hypothetical protein | 0 | 0.0003 | 0.0003 |
Schistosoma mansoni | hypothetical protein | 0 | 0.0003 | 0.0003 |
Schistosoma mansoni | transcription factor LCR-F1 | 0.0043 | 0.3781 | 0.3781 |
Brugia malayi | Kelch motif family protein | 0 | 0.0003 | 0.0007 |
Echinococcus multilocularis | kelch ECH associated protein 1 | 0.0114 | 0.9972 | 0.9972 |
Echinococcus granulosus | kelch protein 10 | 0 | 0.0003 | 0.0003 |
Entamoeba histolytica | hypothetical protein | 0.0043 | 0.3781 | 0.5 |
Schistosoma mansoni | hypothetical protein | 0 | 0.0003 | 0.0003 |
Schistosoma mansoni | hypothetical protein | 0 | 0.0003 | 0.0003 |
Loa Loa (eye worm) | ring canal kelch protein | 0 | 0.0003 | 1 |
Echinococcus granulosus | kelch ECH associated protein 1 | 0.0114 | 0.9972 | 1 |
Schistosoma mansoni | hypothetical protein | 0.0114 | 1 | 1 |
Schistosoma mansoni | hypothetical protein | 0.0043 | 0.3781 | 0.3781 |
Echinococcus granulosus | ectoderm neural cortex protein 1 | 0 | 0.0003 | 0.0003 |
Echinococcus granulosus | kelch ECH associated protein 1 like | 0.0114 | 0.9972 | 1 |
Echinococcus granulosus | Basic leucine zipper bZIP transcription | 0.0043 | 0.3781 | 0.3792 |
Entamoeba histolytica | hypothetical protein | 0.0043 | 0.3781 | 0.5 |
Echinococcus granulosus | kelch ECH associated protein 1 like | 0.0114 | 0.9972 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
Activity (binding) | Binding affinity to kelch domain of Keap1 (unknown origin) using high affinity ETGE motif from Nrf2 unknown origin) at 200 uM by fluorescence polarization assay | ChEMBL. | 26348784 | |
CD (binding) | = 0.6 uM | Activation of Nrf2 in mouse Hepa1c1c7 cells assessed as concentration required to 2 fold induction of NQO1 production after 24 hrs by MTT colorimetric assay | ChEMBL. | 26348784 |
EC50 (binding) | = 7.1 uM | Inhibition of kelch domain of Keap1 (unknown origin) interaction to high affinity ETGE motif from Nrf2 by fluorescence polarization assay | ChEMBL. | 26348784 |
Inhibition (binding) | Inhibition of mCherry labeled Keap1 interaction to ETGE motif from Nrf2 in human HEK293 cells at 10 uM by FRET based assay | ChEMBL. | 26348784 | |
Inhibition (binding) | Inhibition of mCherry labeled Keap1 interaction to DLG motif from Nrf2 in human HEK293 cells at 10 uM by FRET based assay | ChEMBL. | 26348784 | |
Inhibition (binding) | Inhibition of kelch domain of Keap1 (unknown origin) interaction to high affinity ETGE motif from Nrf2 unknown origin) in presence of 0 to 1 % v/v Triton X100 by fluorescence polarization assay | ChEMBL. | 26348784 | |
Inhibition (binding) | = 67.2 % | Inhibition of kelch domain of Keap1 (unknown origin) interaction to high affinity ETGE motif from Nrf2 unknown origin) at 100 uM by fluorescence polarization assay | ChEMBL. | 26348784 |
Many chemical entities in TDR Targets come from high-throughput screenings with whole cells or tissue samples, and not all assayed compounds have been tested against a single a single target protein, probably because they get ruled out during screening process. Even if these compounds may have not been of interest in the original screening, they may come as interesting leads for other screening assays. Furthermore, we may be able to propose drug-target associations using chemical similarities and network patterns.
1 literature reference was collected for this gene.