Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | potassium intermediate/small conductance calcium-activated channel, subfamily N, member 1 | Starlite/ChEMBL | References |
Homo sapiens | potassium intermediate/small conductance calcium-activated channel, subfamily N, member 3 | Starlite/ChEMBL | References |
Homo sapiens | potassium intermediate/small conductance calcium-activated channel, subfamily N, member 2 | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Plasmodium vivax | hypothetical protein, conserved | potassium intermediate/small conductance calcium-activated channel, subfamily N, member 2 | 231 aa | 188 aa | 21.3 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Schistosoma mansoni | calcium-activated potassium channel | 0.0366 | 0.5365 | 0.5365 |
Schistosoma mansoni | hypothetical protein | 0.0615 | 1 | 1 |
Schistosoma mansoni | calcium-activated potassium channel | 0.0615 | 1 | 1 |
Brugia malayi | Calcitonin receptor-like protein seb-1 | 0.0115 | 0.0681 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0238 | 0.2972 | 0.2972 |
Loa Loa (eye worm) | hypothetical protein | 0.0615 | 1 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0225 | 0.2732 | 0.2732 |
Loa Loa (eye worm) | pigment dispersing factor receptor c | 0.0115 | 0.0681 | 0.0681 |
Loa Loa (eye worm) | hypothetical protein | 0.0115 | 0.0681 | 0.0681 |
Brugia malayi | Corticotropin releasing factor receptor 2 precursor, putative | 0.0115 | 0.0681 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.0128 | 0.0921 | 0.0921 |
Echinococcus multilocularis | small conductance calcium activated potassium | 0.0615 | 1 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
CC50 (ADMET) | = 31.1 uM | Cytotoxicity in human KB cells assessed as cell viability incubated for 72 hrs by MTT assay | ChEMBL. | 26318065 |
IC50 (binding) | = 0.004 uM | Displacement of [125I]apamin from Kca2.3 channel expressed in HEK293 cells by scintillation proximity assay | ChEMBL. | 18774291 |
IC50 (binding) | = 0.004 uM | Inhibition of Kca2.1 channel expressed in HEK293 cells by thallium flux assay | ChEMBL. | 18774291 |
IC50 (binding) | = 0.011 uM | Inhibition of Kca2.2 channel expressed in HEK293 cells by thallium flux assay | ChEMBL. | 18774291 |
IC50 (binding) | = 0.056 uM | Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay | ChEMBL. | 18774291 |
IC50 (binding) | = 0.059 uM | Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay | ChEMBL. | 18774291 |
IC50 (binding) | = 0.059 uM | Displacement of [125I]apamin from Kca2.2 channel expressed in HEK293 cells | ChEMBL. | 18774291 |
IC50 (functional) | = 0.7 uM | Antileishmanial activity against Leishmania donovani MHOM/IN/80/Dd8 expressing luciferase reporter gene infected in mouse J-774A1 cells assessed as inhibition of amastigote stage formation incubated for 72 hrs by luminometry | ChEMBL. | 26318065 |
Inhibition (binding) | = 10 % | Inhibition of Kca3.1 channel expressed in HEK293 cells at 30 uM by thallium flux assay | ChEMBL. | 18774291 |
Inhibition (binding) | = 98 % | Inhibition of Kca2.3 channel expressed in HEK293 cells at 30 uM by thallium flux assay | ChEMBL. | 18774291 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Leishmania donovani | ChEMBL23 | 26318065 |
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.