Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | chemokine (C-X-C motif) receptor 2 | Starlite/ChEMBL | References |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Entamoeba histolytica | hypothetical protein, conserved | 0.0149 | 0.4298 | 1 |
Echinococcus granulosus | bloom syndrome protein | 0.0121 | 0.333 | 0.719 |
Trypanosoma cruzi | DNA repair and recombination helicase protein PIF7, putative | 0.0149 | 0.4298 | 1 |
Schistosoma mansoni | hypothetical protein | 0.0149 | 0.4298 | 1 |
Trypanosoma cruzi | DNA repair and recombination helicase protein PIF6, putative | 0.0149 | 0.4298 | 1 |
Echinococcus granulosus | ATP dependent DNA helicase PIF1 | 0.0149 | 0.4298 | 1 |
Trypanosoma cruzi | DNA repair and recombination helicase protein PIF7, putative | 0.0149 | 0.4298 | 1 |
Entamoeba histolytica | DNA repair and recombination protein, putative | 0.0149 | 0.4298 | 1 |
Trichomonas vaginalis | DNA helicase recq1, putative | 0.0121 | 0.333 | 0.6699 |
Toxoplasma gondii | ATP-dependent DNA helicase, RecQ family protein | 0.005 | 0.0854 | 0.4422 |
Giardia lamblia | Rrm3p helicase | 0.0149 | 0.4298 | 1 |
Brugia malayi | ATP-dependent DNA helicase, RecQ family protein | 0.005 | 0.0854 | 0.1942 |
Trypanosoma brucei | DNA repair and recombination helicase protein PIF6 | 0.0149 | 0.4298 | 1 |
Trichomonas vaginalis | conserved hypothetical protein | 0.0149 | 0.4298 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.005 | 0.0854 | 0.0612 |
Leishmania major | PIF1 helicase-like protein, putative,DNA repair and recombination protein, mitochondrial precursor, putative | 0.0149 | 0.4298 | 1 |
Schistosoma mansoni | DNA helicase recq1 | 0.005 | 0.0854 | 0.1986 |
Leishmania major | PIF1 helicase-like protein, putative,DNA repair and recombination protein, mitochondrial precursor, putative | 0.0149 | 0.4298 | 1 |
Loa Loa (eye worm) | RecQ helicase | 0.0121 | 0.333 | 0.3154 |
Echinococcus multilocularis | bloom syndrome protein | 0.0121 | 0.333 | 0.719 |
Schistosoma mansoni | blooms syndrome DNA helicase | 0.0096 | 0.2443 | 0.5684 |
Brugia malayi | ATP-dependent DNA helicase, RecQ family protein | 0.005 | 0.0854 | 0.1942 |
Brugia malayi | Bloom's syndrome protein homolog | 0.0121 | 0.333 | 1 |
Entamoeba histolytica | recQ family helicase, putative | 0.0065 | 0.1366 | 0.3178 |
Echinococcus multilocularis | ATP dependent DNA helicase PIF1 | 0.0149 | 0.4298 | 1 |
Trichomonas vaginalis | DNA helicase recq, putative | 0.0121 | 0.333 | 0.6699 |
Loa Loa (eye worm) | ATP-dependent DNA helicase | 0.005 | 0.0854 | 0.0612 |
Plasmodium falciparum | ADP-dependent DNA helicase RecQ | 0.0107 | 0.2818 | 1 |
Toxoplasma gondii | ATP-dependent DNA helicase, RecQ family protein | 0.0081 | 0.1931 | 1 |
Loa Loa (eye worm) | DEAH box polypeptide 35 | 0.0033 | 0.0257 | 0.00000000073679 |
Trypanosoma brucei | DNA repair and recombination helicase protein PIF7 | 0.0149 | 0.4298 | 1 |
Toxoplasma gondii | ATP-dependent DNA helicase, RecQ family protein | 0.005 | 0.0854 | 0.4422 |
Schistosoma mansoni | DNA helicase recq5 | 0.005 | 0.0854 | 0.1986 |
Plasmodium vivax | ADP-dependent DNA helicase RecQ, putative | 0.0082 | 0.1964 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
IC50 (binding) | = 520 nM | BindingDB_Patents: In Vitro Inhibition Assay. An in vitro assay showed inhibition of CXCR2-mediated intracellular calcium release. Briefly, human neutrophils were suspended in HBSS- (without Ca2+ and Mg2+) containing 10 mM HEPES and FLIPR Calcium 3 dye (3.1x107 cells in total volume 1.7 mL). Cells were aliquoted (200 uL of the cell suspension per tube, 8 tubes total) and 2 uL of the designated compound (with appropriate dilutions) were added to each of 6 tubes. As controls, 2 uL of DMSO (1% final concentration) were added to 2 other tubes. Cells were incubated for 30 min at 37 C. After dye loading, tubes were centrifuged at 6,000 rpm for 1 min, supernatant was removed and the cell pellet was re-suspended in 200 uL of HBSS+ (with Ca2+ and Mg2+) containing 10 mM HEPES. The test compound or DMSO (control) was added again at the same concentrations that were used during cell loading. The cell suspension was aliquoted into a 96-well Reading Plate (Corning) in a volume of 90 uL (105 cells/well). | ChEMBL. | No reference |
IC50 (binding) | = 520 nM | BindingDB_Patents: In Vitro Inhibition Assay. An in vitro assay showed inhibition of CXCR2-mediated intracellular calcium release. Briefly, human neutrophils were suspended in HBSS- (without Ca2+ and Mg2+) containing 10 mM HEPES and FLIPR Calcium 3 dye (3.1x107 cells in total volume 1.7 mL). Cells were aliquoted (200 uL of the cell suspension per tube, 8 tubes total) and 2 uL of the designated compound (with appropriate dilutions) were added to each of 6 tubes. As controls, 2 uL of DMSO (1% final concentration) were added to 2 other tubes. Cells were incubated for 30 min at 37 C. After dye loading, tubes were centrifuged at 6,000 rpm for 1 min, supernatant was removed and the cell pellet was re-suspended in 200 uL of HBSS+ (with Ca2+ and Mg2+) containing 10 mM HEPES. The test compound or DMSO (control) was added again at the same concentrations that were used during cell loading. The cell suspension was aliquoted into a 96-well Reading Plate (Corning) in a volume of 90 uL (105 cells/well). | ChEMBL. | No reference |
IC50 (binding) | = 0.52 uM | Antagonist activity at CXCR2 in human PMNs assessed as inhibition of CXCL1-induced intracellular Ca2+ release by fluorescence based calcium flux assay | ChEMBL. | 25254640 |
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.