Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | potassium voltage-gated channel, subfamily H (eag-related), member 2 | Starlite/ChEMBL | References |
Homo sapiens | potassium inwardly-rectifying channel, subfamily J, member 1 | Starlite/ChEMBL | References |
Rattus norvegicus | ATP-sensitive inward rectifier potassium channel 1 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Onchocerca volvulus | ATP-sensitive inward rectifier potassium channel 1 | 391 aa | 332 aa | 44.6 % | |
Loa Loa (eye worm) | inward rectifying k channel family protein 1 | ATP-sensitive inward rectifier potassium channel 1 | 391 aa | 329 aa | 38.9 % |
Onchocerca volvulus | ATP-sensitive inward rectifier potassium channel 1 | 391 aa | 333 aa | 38.4 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus granulosus | potassium voltage gated channel subfamily H | 0.0045 | 0.183 | 1 |
Echinococcus granulosus | voltage gated potassium channel | 0.0013 | 0.021 | 0.1145 |
Loa Loa (eye worm) | hypothetical protein | 0.0204 | 1 | 1 |
Loa Loa (eye worm) | inward rectifying k channel family protein 1 | 0.0204 | 1 | 1 |
Schistosoma mansoni | voltage-gated potassium channel | 0.0049 | 0.2039 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0039 | 0.1529 | 0.1529 |
Brugia malayi | Voltage-gated potassium channel, HERG (KCNH2)-related. C. elegans unc-103 ortholog | 0.0045 | 0.183 | 1 |
Echinococcus multilocularis | potassium voltage gated channel subfamily H | 0.0045 | 0.183 | 1 |
Echinococcus multilocularis | potassium voltage gated channel subfamily H | 0.0013 | 0.021 | 0.1145 |
Echinococcus granulosus | potassium voltage gated channel subfamily H | 0.0013 | 0.021 | 0.1145 |
Schistosoma mansoni | voltage-gated potassium channel | 0.0013 | 0.021 | 0.1028 |
Schistosoma mansoni | voltage-gated potassium channel | 0.0013 | 0.021 | 0.1028 |
Schistosoma mansoni | voltage-gated potassium channel | 0.0049 | 0.2039 | 1 |
Loa Loa (eye worm) | voltage and ligand gated potassium channel | 0.0045 | 0.183 | 0.183 |
Echinococcus multilocularis | voltage gated potassium channel | 0.0013 | 0.021 | 0.1145 |
Trichomonas vaginalis | voltage and ligand gated potassium channel, putative | 0.0042 | 0.168 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0013 | 0.021 | 0.021 |
Trichomonas vaginalis | voltage and ligand gated potassium channel, putative | 0.0042 | 0.168 | 1 |
Toxoplasma gondii | hypothetical protein | 0.0204 | 1 | 0.5 |
Loa Loa (eye worm) | hypothetical protein | 0.0204 | 1 | 1 |
Brugia malayi | Voltage-gated potassium channel, EAG (KCNH1)-related. C. elegans egl-2 ortholog | 0.0013 | 0.021 | 0.1145 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 110 nM | BindingDB_Patents: Thallium Flux Assay. FluxOR Kit Components (Invitrogen F10017) FluxOR Reagent (Component A) FluxOR Assay Buffer (Component B)-10x Concentrate PowerLoad Concentrate (Component C)-100x Concentrate Probenecid (Component D)-Lyophilized sample is kept at -20 C. Water soluble, 100x after solubilization in 1 ml water. Store at 4 C. FluxOR Chloride-free Buffer (Component E)-5x Concentrate Potassium sulfate (K2SO4) Concentrate (Component F)-125 mM in water. Store at 4 C. Thallium sulfate (Tl2SO4) Concentrate (Component G)-50 mM in water. Store at 4 C. DMSO (dimethyl sulfoxide, Component H)-1 ml (100%) Reagent Preparation- FluxOR Working Solutions 1000x FluxOR Reagent: Reconstitute a vial of component A in 100 ul DMSO; Mix well; Store 10 ul aliquots at -20 C. 1x FluxOR Assay Buffer: Dilute Component B 10-fold with water; Adjust pH to 7.4 with Hepes/NaOH; Filter and store at 4 C. | ChEMBL. | No reference |
IC50 (binding) | = 110 nM | BindingDB_Patents: Thallium Flux Assay. FluxOR Kit Components (Invitrogen F10017) FluxOR Reagent (Component A) FluxOR Assay Buffer (Component B)-10x Concentrate PowerLoad Concentrate (Component C)-100x Concentrate Probenecid (Component D)-Lyophilized sample is kept at -20 C. Water soluble, 100x after solubilization in 1 ml water. Store at 4 C. FluxOR Chloride-free Buffer (Component E)-5x Concentrate Potassium sulfate (K2SO4) Concentrate (Component F)-125 mM in water. Store at 4 C. Thallium sulfate (Tl2SO4) Concentrate (Component G)-50 mM in water. Store at 4 C. DMSO (dimethyl sulfoxide, Component H)-1 ml (100%) Reagent Preparation- FluxOR Working Solutions 1000x FluxOR Reagent: Reconstitute a vial of component A in 100 ul DMSO; Mix well; Store 10 ul aliquots at -20 C. 1x FluxOR Assay Buffer: Dilute Component B 10-fold with water; Adjust pH to 7.4 with Hepes/NaOH; Filter and store at 4 C. | ChEMBL. | No reference |
IC50 (binding) | = 0.03 uM | Inhibition of ROMK by electrophysiology assay | ChEMBL. | 24900480 |
IC50 (binding) | = 0.049 uM | Inhibition of human ROMK1 channel expressed in CHO cells coexpressing DHFR assessed as inhibition of 86Rb+ efflux after 35 mins by TopCount method | ChEMBL. | 24900480 |
IC50 (binding) | = 0.055 uM | Inhibition of rat ROMK channel expressed in HEk293 cells assessed as inhibition of thallium efflux by fluorescence assay | ChEMBL. | 24900480 |
IC50 (binding) | = 0.17 uM | Displacement of [35S]MK499 from human ERG | ChEMBL. | 24900480 |
Inhibition (binding) | < 50 % | Inhibition of Kir4.1 expressed in HEK293 cells assessed as inhibition of thallium efflux up to 100 uM by fluorescence assay | ChEMBL. | 24900480 |
Inhibition (binding) | < 50 % | Inhibition of Kir7.1 expressed in HEK293 cells assessed as inhibition of thallium efflux up to 100 uM by fluorescence assay | ChEMBL. | 24900480 |
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.