Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | histamine receptor H4 | Starlite/ChEMBL | No references |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | CMGC/MAPK/ERK1 protein kinase | 0.0801 | 0.5 | 0.5 |
Trypanosoma brucei | mitogen activated protein kinase 4, putative | 0.0801 | 0.5 | 0.5 |
Toxoplasma gondii | CMGC kinase, MAPK family (ERK) MAPK-1 | 0.0801 | 0.5 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0801 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen activated protein kinase 4, putative | 0.0801 | 0.5 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0801 | 0.5 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0801 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen activated protein kinase 2, putative | 0.0801 | 0.5 | 0.5 |
Giardia lamblia | Kinase, CMGC MAPK | 0.0801 | 0.5 | 0.5 |
Trypanosoma brucei | protein kinase, putative | 0.0801 | 0.5 | 0.5 |
Leishmania major | mitogen activated protein kinase, putative,map kinase, putative | 0.0801 | 0.5 | 0.5 |
Trichomonas vaginalis | CMGC family protein kinase | 0.0801 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.0801 | 0.5 | 0.5 |
Echinococcus multilocularis | mitogen activated protein kinase 3 | 0.0801 | 0.5 | 0.5 |
Echinococcus granulosus | mitogen activated protein kinase 3 | 0.0801 | 0.5 | 0.5 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0801 | 0.5 | 0.5 |
Echinococcus multilocularis | mitogen activated protein kinase | 0.0801 | 0.5 | 0.5 |
Trypanosoma cruzi | mitogen-activated protein kinase 11, putative | 0.0801 | 0.5 | 0.5 |
Echinococcus granulosus | mitogen activated protein kinase | 0.0801 | 0.5 | 0.5 |
Leishmania major | mitogen activated protein kinase 4, putative;with=GeneDB:LmxM19.1440 | 0.0801 | 0.5 | 0.5 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | = 6.26 | Agonist activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding after 90 mins by liquid scintillation counting | ChEMBL. | No reference |
Intrinsic activity (binding) | Intrinsic activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay relative to histamine | ChEMBL. | No reference | |
Intrinsic activity (functional) | = -0.52 | Intrinsic activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as [35S]GTPgammaS binding at 10 uM after 90 mins by liquid scintillation counting relative to histamine | ChEMBL. | No reference |
Intrinsic activity (functional) | = -0.02 | Intrinsic activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as [35S]GTPgammaS binding at 10 uM after 90 mins by liquid scintillation counting relative to histamine | ChEMBL. | No reference |
Intrinsic activity (functional) | = 0.74 | Intrinsic activity at human recombinant histamine H4 receptor-RGS19 fusion protein expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 assessed as [35S]GTPgammaS binding at 10 uM after 90 mins by liquid scintillation counting relative to histamine | ChEMBL. | No reference |
pEC50 (binding) | Agonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay | ChEMBL. | No reference | |
pKb (functional) | Antagonist activity at human recombinant histamine H1 receptor expressed in Sf9 cells coexpressing RGS4 assessed as inhibition of histamine-induced [gamma33P]GTP hydrolysis preincubated for 2 mins before [gamma32P]GTP addition measured after 20 mins by steady-state GTPase activity assay | ChEMBL. | No reference | |
pKb (functional) | < 5 | Antagonist activity at human recombinant histamine H2 receptor-Gsalphas fusion protein expressed in Sf9 cells assessed as inhibition of histamine-induced [35S]GTPgammaS binding after 90 mins by liquid scintillation counting | ChEMBL. | No reference |
pKb (functional) | < 5 | Antagonist activity at human recombinant histamine H3 receptor expressed in Sf9 cells coexpressing Galphai2,Gbeta1gamma2 and RGS4 assessed as inhibition of histamine-induced [35S]GTPgammaS binding after 90 mins by liquid scintillation counting | ChEMBL. | No reference |
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.