Species | Target name | Source | Bibliographic reference |
---|---|---|---|
Homo sapiens | Pim-1 proto-oncogene, serine/threonine kinase | Starlite/ChEMBL | References |
Homo sapiens | fms-related tyrosine kinase 3 | Starlite/ChEMBL | References |
Homo sapiens | BCL2-associated agonist of cell death | Starlite/ChEMBL | References |
Homo sapiens | Pim-3 proto-oncogene, serine/threonine kinase | Starlite/ChEMBL | References |
Homo sapiens | Pim-2 proto-oncogene, serine/threonine kinase | 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 % |
Trypanosoma brucei | protein lipid droplet kinase (LDK) | Pim-3 proto-oncogene, serine/threonine kinase | 326 aa | 296 aa | 29.7 % |
Species | Potential target | Raw | Global | Species |
---|---|---|---|---|
Loa Loa (eye worm) | choline/Carnitine O-acyltransferase | 0.0279 | 0.1541 | 0.1541 |
Brugia malayi | Choline O-acetyltransferase | 0.0199 | 0.1064 | 0.1064 |
Brugia malayi | Protein kinase domain containing protein | 0.0385 | 0.2177 | 0.2177 |
Loa Loa (eye worm) | choline O-acetyltransferase | 0.0199 | 0.1064 | 0.1064 |
Onchocerca volvulus | Serine\/threonine protein kinase homolog | 0.0385 | 0.2177 | 1 |
Echinococcus multilocularis | proto oncogene serine:threonine protein kinase | 0.0385 | 0.2177 | 0.2406 |
Loa Loa (eye worm) | carnitine O-palmitoyltransferase I isoform | 0.0199 | 0.1064 | 0.1064 |
Leishmania major | choline/Carnitine o-acyltransferase-like protein | 0.0975 | 0.5689 | 1 |
Echinococcus multilocularis | carnitine O palmitoyltransferase 2 | 0.0279 | 0.1541 | 0.1032 |
Echinococcus granulosus | carnitine O palmitoyltransferase 2 | 0.0279 | 0.1541 | 0.2709 |
Loa Loa (eye worm) | hypothetical protein | 0.0199 | 0.1064 | 0.1064 |
Echinococcus granulosus | choline O acetyltransferase | 0.0199 | 0.1064 | 0.187 |
Brugia malayi | Choline/Carnitine o-acyltransferase family protein | 0.0199 | 0.1064 | 0.1064 |
Trypanosoma cruzi | choline/carnitine O-acyltransferase, putative | 0.0975 | 0.5689 | 1 |
Loa Loa (eye worm) | hypothetical protein | 0.1698 | 1 | 1 |
Schistosoma mansoni | serine/threonine protein kinase | 0.0385 | 0.2177 | 1 |
Echinococcus multilocularis | carnitine O palmitoyltransferase 1, liver | 0.0975 | 0.5689 | 1 |
Trypanosoma cruzi | choline/carnitine O-acyltransferase, putative | 0.0975 | 0.5689 | 1 |
Echinococcus granulosus | carnitine O palmitoyltransferase 1 liver | 0.0975 | 0.5689 | 1 |
Brugia malayi | Choline/Carnitine o-acyltransferase family protein | 0.0279 | 0.1541 | 0.1541 |
Loa Loa (eye worm) | CAMK/PIM protein kinase | 0.0385 | 0.2177 | 0.2177 |
Trypanosoma cruzi | carnitine O-palmitoyltransferase II, putative | 0.0279 | 0.1541 | 0.1032 |
Trypanosoma brucei | carnitine O-palmitoyltransferase II, putative | 0.0279 | 0.1541 | 1 |
Loa Loa (eye worm) | CAMK/PIM protein kinase | 0.0385 | 0.2177 | 0.2177 |
Leishmania major | carnitine palmitoyltransferase-like protein | 0.0279 | 0.1541 | 0.1032 |
Brugia malayi | Serine/threonine-protein kinase Pim-3 | 0.0385 | 0.2177 | 0.2177 |
Brugia malayi | Choline O-acetyltransferase | 0.0199 | 0.1064 | 0.1064 |
Echinococcus granulosus | proto oncogene serine:threonine protein kinase | 0.0385 | 0.2177 | 0.3826 |
Activity type | Activity value | Assay description | Source | Reference |
---|---|---|---|---|
EC50 (functional) | < 0.03 uM | Antiproliferative activity against human MV411 cells assessed as cell viability after 4 days by alamar blue assay | ChEMBL. | 21982499 |
EC50 (binding) | = 0.04 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) | = 0.44 uM | Antiproliferative activity against human K562 cells assessed as cell viability after 4 days by alamar blue assay | ChEMBL. | 21982499 |
EC50 (functional) | = 0.53 uM | Antiproliferative activity against human MIAPaCa2 cells assessed as cell viability after 4 days by alamar blue assay | ChEMBL. | 21982499 |
EC50 (functional) | = 0.79 uM | Antiproliferative activity against human MDA-MB-231 cells assessed as cell viability after 4 days by alamar blue assay | ChEMBL. | 21982499 |
EC50 (functional) | = 9.26 uM | Antiproliferative activity against human PC3 cells assessed as cell viability after 4 days by alamar blue assay | ChEMBL. | 21982499 |
EC50 (binding) | > 10 uM | Inhibition of FLT3 phosphorylation at Tyr591 in human MV-4-11 cells assessed as phospho-FLT3 level after 4 hrs by ELISA | ChEMBL. | 21982499 |
IC50 (binding) | = 0.004 uM | Inhibition of human recombinant Pim1 using RSRHSSYPAGT as substrate by radiometric assay in the presence of 30 uM [ATP] | ChEMBL. | 21982499 |
IC50 (binding) | = 0.005 uM | Inhibition of PIM1 using KKRNRTLTV as substrate by millipore assay in the presence of 90 uM [ATP] | ChEMBL. | 21982499 |
IC50 (binding) | = 0.012 uM | Inhibition of human recombinant Pim2 using RSRHSSYPAGT as substrate by radiometric assay in the presence of 5 uM [ATP] | ChEMBL. | 21982499 |
IC50 (binding) | = 0.028 uM | Inhibition of PIM2 by millipore assay in the presence of 15 uM [ATP] | ChEMBL. | 21982499 |
IC50 (binding) | = 0.035 uM | Inhibition of PIM3 using RSRHSSYPAGT as substrate by radiometric assay in the presence of 155 uM [ATP] | ChEMBL. | 21982499 |
IC50 (binding) | = 0.061 uM | Inhibition of FLT3 using EAIYAAPFAKKK as substrate by radiometric assay in the presence of 200 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.