Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | Pim-1 proto-oncogene, serine/threonine kinase | Starlite/ChEMBL | References |
Homo sapiens | Pim-2 proto-oncogene, serine/threonine kinase | Starlite/ChEMBL | References |
Homo sapiens | BCL2-associated agonist of cell death | Starlite/ChEMBL | References |
Species | Potential target | Known druggable target | Length | Alignment span | Identity |
---|---|---|---|---|---|
Trypanosoma brucei | protein lipid droplet kinase (LDK) | Pim-2 proto-oncogene, serine/threonine kinase | 311 aa | 278 aa | 28.8 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Echinococcus multilocularis | proto oncogene serine:threonine protein kinase | 0.0193 | 0.1341 | 0.2549 |
Echinococcus granulosus | choline O acetyltransferase | 0.0108 | 0.0178 | 0.026 |
Echinococcus multilocularis | epidermal growth factor receptor | 0.0164 | 0.0951 | 0.1808 |
Echinococcus multilocularis | epidermal growth factor receptor | 0.0306 | 0.2884 | 0.5481 |
Echinococcus granulosus | epidermal growth factor receptor | 0.0164 | 0.0951 | 0.1742 |
Loa Loa (eye worm) | choline O-acetyltransferase | 0.0108 | 0.0178 | 0.0136 |
Loa Loa (eye worm) | choline/Carnitine O-acyltransferase | 0.0186 | 0.1247 | 0.1211 |
Schistosoma mansoni | tyrosine kinase | 0.0163 | 0.0928 | 0.3117 |
Echinococcus granulosus | proto oncogene serine:threonine protein kinase | 0.0193 | 0.1341 | 0.2489 |
Schistosoma mansoni | tyrosine kinase | 0.0163 | 0.0928 | 0.3117 |
Trypanosoma brucei | carnitine O-palmitoyltransferase II, putative | 0.0186 | 0.1247 | 1 |
Brugia malayi | Protein kinase domain containing protein | 0.0193 | 0.1341 | 0.1305 |
Brugia malayi | Furin-like cysteine rich region family protein | 0.0306 | 0.2884 | 0.2854 |
Leishmania major | carnitine palmitoyltransferase-like protein | 0.0186 | 0.1247 | 0.2104 |
Loa Loa (eye worm) | CAMK/PIM protein kinase | 0.0193 | 0.1341 | 0.1305 |
Schistosoma mansoni | tyrosine kinase | 0.0163 | 0.0928 | 0.3117 |
Schistosoma mansoni | tyrosine kinase | 0.0164 | 0.0951 | 0.32 |
Loa Loa (eye worm) | hypothetical protein | 0.0108 | 0.0178 | 0.0136 |
Brugia malayi | Serine/threonine-protein kinase Pim-3 | 0.0193 | 0.1341 | 0.1305 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0193 | 0.1341 | 0.4571 |
Loa Loa (eye worm) | TK/EGFR protein kinase | 0.0306 | 0.2884 | 0.2854 |
Loa Loa (eye worm) | CAMK/PIM protein kinase | 0.0193 | 0.1341 | 0.1305 |
Leishmania major | choline/Carnitine o-acyltransferase-like protein | 0.048 | 0.5262 | 1 |
Trypanosoma cruzi | choline/carnitine O-acyltransferase, putative | 0.048 | 0.5262 | 1 |
Echinococcus granulosus | carnitine O palmitoyltransferase 1 liver | 0.048 | 0.5262 | 1 |
Echinococcus granulosus | epidermal growth factor receptor | 0.0306 | 0.2884 | 0.5445 |
Echinococcus granulosus | melanoma receptor tyrosine protein kinase | 0.0164 | 0.0951 | 0.1742 |
Echinococcus multilocularis | carnitine O palmitoyltransferase 2 | 0.0186 | 0.1247 | 0.2371 |
Schistosoma mansoni | choline o-acyltransferase | 0.0108 | 0.0178 | 0.0478 |
Schistosoma mansoni | choline o-acyltransferase | 0.0108 | 0.0178 | 0.0478 |
Trypanosoma cruzi | carnitine O-palmitoyltransferase II, putative | 0.0186 | 0.1247 | 0.2104 |
Brugia malayi | Choline/Carnitine o-acyltransferase family protein | 0.0108 | 0.0178 | 0.0136 |
Brugia malayi | Choline/Carnitine o-acyltransferase family protein | 0.0186 | 0.1247 | 0.1211 |
Brugia malayi | Choline O-acetyltransferase | 0.0108 | 0.0178 | 0.0136 |
Echinococcus multilocularis | carnitine O palmitoyltransferase 1, liver | 0.048 | 0.5262 | 1 |
Loa Loa (eye worm) | carnitine O-palmitoyltransferase I isoform | 0.0108 | 0.0178 | 0.0136 |
Loa Loa (eye worm) | hypothetical protein | 0.0828 | 1 | 1 |
Schistosoma mansoni | tyrosine kinase | 0.0164 | 0.0951 | 0.32 |
Brugia malayi | Choline O-acetyltransferase | 0.0108 | 0.0178 | 0.0136 |
Onchocerca volvulus | Serine\/threonine protein kinase homolog | 0.0193 | 0.1341 | 1 |
Echinococcus multilocularis | insulin receptor | 0.0098 | 0.0042 | 0.008 |
Echinococcus granulosus | carnitine O palmitoyltransferase 2 | 0.0186 | 0.1247 | 0.2309 |
Schistosoma mansoni | tyrosine kinase | 0.0306 | 0.2884 | 1 |
Echinococcus multilocularis | insulin growth factor 1 receptor beta | 0.0098 | 0.0042 | 0.008 |
Echinococcus multilocularis | choline O acetyltransferase | 0.0108 | 0.0178 | 0.0338 |
Trypanosoma cruzi | choline/carnitine O-acyltransferase, putative | 0.048 | 0.5262 | 1 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (binding) | Inhibition of FLT3 phosphorylation at Tyr591 in human MV-4-11 cells assessed as phospho-FLT3 level after 4 hrs by ELISA | ChEMBL. | 21982499 | |
EC50 (functional) | = 0.224 uM | Antiproliferative activity against human MV411 cells assessed as cell viability after 4 days by alamar blue assay | ChEMBL. | 21982499 |
EC50 (binding) | = 0.89 uM | Inhibition of BAD phosphorylation at Ser112 in human MV-4-11 cells assessed as phospho-BAD level after 4 hrs by ELISA | ChEMBL. | 21982499 |
EC50 (functional) | = 6.38 uM | Antiproliferative activity against human K562 cells assessed as cell viability after 4 days by alamar blue assay | ChEMBL. | 21982499 |
EC50 (functional) | = 7.47 uM | Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 4 days by alamar blue assay | ChEMBL. | 21982499 |
EC50 (functional) | = 8.06 uM | Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 4 days by alamar blue assay | ChEMBL. | 21982499 |
EC50 (functional) | > 10 uM | Antiproliferative activity against human PC3 cells assessed as cell viability after 4 days by alamar blue assay | ChEMBL. | 21982499 |
IC50 (binding) | = 0.002 uM | Inhibition of human recombinant Pim2 using RSRHSSYPAGT as substrate by radiometric assay in the presence of 5 uM [ATP] | ChEMBL. | 21982499 |
IC50 (binding) | = 0.016 uM | Inhibition of human recombinant Pim1 using RSRHSSYPAGT as substrate by radiometric assay in the presence of 30 uM [ATP] | ChEMBL. | 21982499 |
Species name | Source | Reference | Is orphan |
---|---|---|---|
Homo sapiens | ChEMBL23 | 21982499 |
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.