Detailed information for compound 511554
Basic information
Technical information
- TDR Targets ID: 511554
- Name: 1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin- 4-amine
- MW: 217.27 | Formula: C11H15N5
-
H donors: 2
H acceptors: 2
LogP: 0.73
Rotable bonds: 1
Rule of 5 violations (Lipinski): 1 - SMILES: NC1CCN(CC1)c1ncnc2c1cc[nH]2
- InChi: 1S/C11H15N5/c12-8-2-5-16(6-3-8)11-9-1-4-13-10(9)14-7-15-11/h1,4,7-8H,2-3,5-6,12H2,(H,13,14,15)
- InChiKey: SOYJTCRGELSHIV-UHFFFAOYSA-N
Network
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Synonyms
- 1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidinamine
- [1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)-4-piperidyl]amine
Targets
Known targets for this compound
| Species | Target name | Source | Bibliographic reference |
|---|---|---|---|
| Homo sapiens | v-akt murine thymoma viral oncogene homolog 2 | Starlite/ChEMBL | References |
| Homo sapiens | glycogen synthase kinase 3 beta | Starlite/ChEMBL | References |
Predicted pathogen targets for this compound
By orthology
By sequence similarity to non orthologous known druggable targets
No druggable targets predicted by sequence similarity
Obtained from network model
Ranking Plot
Putative Targets List
| Species | Potential target | Raw | Global | Species |
|---|---|---|---|---|
| Loa Loa (eye worm) | CMGC/GSK protein kinase | 0.0058 | 0.0192 | 1 |
| Toxoplasma gondii | cell-cycle-associated protein kinase GSK, putative | 0.0058 | 0.0192 | 0.0238 |
| Echinococcus multilocularis | glycogen synthase kinase 3 beta | 0.0058 | 0.0192 | 1 |
| Trypanosoma brucei | protein kinase, putative | 0.0058 | 0.0192 | 0.0238 |
| Giardia lamblia | Kinase, CMGC GSK | 0.0058 | 0.0192 | 0.0726 |
| Echinococcus multilocularis | protein kinase shaggy | 0.0058 | 0.0192 | 1 |
| Loa Loa (eye worm) | CMGC/GSK protein kinase | 0.0058 | 0.0192 | 1 |
| Echinococcus granulosus | protein kinase shaggy | 0.0058 | 0.0192 | 1 |
| Giardia lamblia | Telomerase catalytic subunit | 0.0371 | 0.255 | 1 |
| Echinococcus multilocularis | rac serine:threonine kinase | 0.0034 | 0.0007 | 0.0365 |
| Trichomonas vaginalis | CMGC family protein kinase | 0.0058 | 0.0192 | 1 |
| Echinococcus multilocularis | serine threonine protein kinase nrc serine threonine protein kinase gad | 0.0034 | 0.0007 | 0.0365 |
| Echinococcus granulosus | serine/threonine protein kinase | 0.0034 | 0.0007 | 0.0365 |
| Echinococcus granulosus | calcium:calmodulin dependent protein kinase | 0.0034 | 0.0007 | 0.0365 |
| Trypanosoma cruzi | glycogen synthase kinase 3, putative | 0.0058 | 0.0192 | 0.0726 |
| Plasmodium vivax | telomerase reverse transcriptase, putative | 0.0371 | 0.255 | 1 |
| Entamoeba histolytica | protein kinase, putative | 0.0051 | 0.0134 | 0.688 |
| Giardia lamblia | Kinase, CMGC GSK | 0.0058 | 0.0192 | 0.0726 |
| Brugia malayi | Telomerase reverse transcriptase | 0.0987 | 0.7201 | 1 |
| Entamoeba histolytica | protein kinase, putative | 0.0051 | 0.0134 | 0.688 |
| Plasmodium falciparum | telomerase reverse transcriptase | 0.0371 | 0.255 | 1 |
| Schistosoma mansoni | glycogen synthase kinase 3-related (gsk3) (cmgc group III) | 0.0058 | 0.0192 | 1 |
| Leishmania major | telomerase reverse transcriptase, putative | 0.0371 | 0.255 | 1 |
| Plasmodium vivax | glycogen synthase kinase 3, putative | 0.0058 | 0.0192 | 0.0726 |
| Entamoeba histolytica | protein kinase, putative | 0.0051 | 0.0134 | 0.688 |
| Trichomonas vaginalis | CMGC family protein kinase | 0.0058 | 0.0192 | 1 |
| Plasmodium falciparum | glycogen synthase kinase 3 | 0.0058 | 0.0192 | 0.0726 |
| Echinococcus granulosus | serine threonine protein kinase nrc | 0.0034 | 0.0007 | 0.0365 |
| Brugia malayi | intracellular kinase | 0.0058 | 0.0192 | 0.0082 |
| Entamoeba histolytica | protein kinase domain containing protein | 0.0058 | 0.0192 | 1 |
| Echinococcus granulosus | glycogen synthase kinase 3 beta | 0.0058 | 0.0192 | 1 |
| Entamoeba histolytica | protein kinase, putative | 0.0058 | 0.0192 | 1 |
| Entamoeba histolytica | protein kinase domain containing protein | 0.0058 | 0.0192 | 1 |
| Trypanosoma brucei | telomerase reverse transcriptase | 0.0371 | 0.255 | 1 |
| Toxoplasma gondii | RNA-directed DNA polymerase | 0.0371 | 0.255 | 1 |
| Trypanosoma cruzi | telomerase reverse transcriptase, putative | 0.0371 | 0.255 | 1 |
| Trypanosoma cruzi | telomerase reverse transcriptase, putative | 0.0371 | 0.255 | 1 |
Activities
| Activity type | Activity value | Assay description | Source | Reference |
|---|---|---|---|---|
| IC50 (binding) | = 180 nM | Inhibition of PKBbeta recombinant (unknown origin) by radiometric filter binding assay | ChEMBL. | 18345609 |
| IC50 (binding) | = 180 nM | Inhibition of PKBbeta recombinant (unknown origin) by radiometric filter binding assay | ChEMBL. | 18345609 |
| IC50 (binding) | = 1550 nM | Inhibition of recombinant catalytic subunit PKA (unknown origin) by radiometric filter binding assay | ChEMBL. | 18345609 |
| IC50 (binding) | = 15 uM | Inhibition of GSK3beta (unknown origin) in human PC3M cells by ELISA | ChEMBL. | 18345609 |
| IC50 (binding) | = 15 uM | Inhibition of GSK3beta (unknown origin) in human PC3M cells by ELISA | ChEMBL. | 18345609 |
| IC50 (functional) | = 48 uM | Growth inhibition of human PC3M cells by SRB assay | ChEMBL. | 18345609 |
| Inhibition (binding) | = 0 % | Inhibition of human full length NEK2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human full length CDK2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human full length CHK2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human full length PKD3 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human full length TSSK1 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human full length MARK2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human CAMK2 gamma catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human full length RSK3 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human CK1D catalytic domain expressed in Escherichia coli cell assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human HGK catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human FLT3 D835Y mutant catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human FLT3 catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human KDR cytoplasmic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human FGFR4 catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human FGFR3 catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human MET cytoplasmic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human IGF1R catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0 % | Inhibition of human full length SRC expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0.5 % | Inhibition of rat full length DYRK1a expressed in Escherichia coli cell assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0.5 % | Inhibition of human full length MSK1 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0.5 % | Inhibition of human full length LYN expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 0.5 % | Inhibition of human full length BTK expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 1 % | Inhibition of human full length IKK beta expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 1 % | Inhibition of human full length ERK1 expressed in Escherichia coli cell assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 1 % | Inhibition of human truncated ABL T315I mutant expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 1.5 % | Inhibition of human full length p38 gamma expressed in Escherichia coli cell assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 1.5 % | Inhibition of human full length CHK1 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 1.5 % | Inhibition of human full length DCAMKL2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 1.5 % | Inhibition of human IRAK4 catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 1.5 % | Inhibition of human FGFR2 catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 1.5 % | Inhibition of human FGFR1 catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 2 % | Inhibition of human truncated p38 alpha expressed in Escherichia coli cell assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 2 % | Inhibition of human full length PIM1 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 2 % | Inhibition of human full length RSK2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 2 % | Inhibition of human full length BMX expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 2.5 % | Inhibition of human full length ERK2 expressed in Escherichia coli cell assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 2.5 % | Inhibition of human truncated BRSK2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 2.5 % | Inhibition of human truncated PKC epsilon expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 2.5 % | Inhibition of human truncated ABL H396P mutant expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 3 % | Inhibition of human full length c-TAK1 expressed in Escherichia coli cell assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 3 % | Inhibition of human HCK catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 3.5 % | Inhibition of human truncated PAK2 expressed in Escherichia coli cell assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 3.5 % | Inhibition of human EGFR catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 4.5 % | Inhibition of human full length LCK expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 5 % | Inhibition of human full length GSK-3 beta expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 5 % | Inhibition of human PDGFR alpha catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 5 % | Inhibition of human full length FYN expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 5.5 % | Inhibition of human full length p38 beta2 expressed in Escherichia coli cell assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 6.5 % | Inhibition of human full length PKD2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 6.5 % | Inhibition of human full length TSSK2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 7 % | Inhibition of human full length PRAK expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 7 % | Inhibition of human truncated c-Raf expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 7.5 % | Inhibition of human full length RSK1 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 7.5 % | Inhibition of human INSR catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 7.5 % | Inhibition of human truncated Arg expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 8 % | Inhibition of human full length p38 delta expressed in Escherichia coli cell assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 8 % | Inhibition of human full length CAMK2D expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 8.5 % | Inhibition of human full length PKG-1beta expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 9.5 % | Inhibition of human full length CSNK1A1 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 10 % | Inhibition of human full length PKG-1a expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 12 % | Inhibition of human full length CAMK4 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 13 % | Inhibition of human truncated PKC theta expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 13.5 % | Inhibition of human full length AurC expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 13.5 % | Inhibition of human FER catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 13.5 % | Inhibition of human full-length ABL expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 14.5 % | Inhibition of human full length BRSK1 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 15 % | Inhibition of human full length MSK2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 16.5 % | Inhibition of human truncated PKC beta1 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 17 % | Inhibition of human truncated ABL Q252H mutant expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 17.5 % | Inhibition of human full length MST2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 18 % | Inhibition of human truncated PKC alpha expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 20.5 % | Inhibition of human full length PKC zeta expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 25.5 % | Inhibition of human CAMK2 beta catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 26 % | Inhibition of human full length PKD1 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 27 % | Inhibition of human truncated SGK1 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 33 % | Inhibition of human full length MAPKAPK2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 33 % | Inhibition of human truncated PKC delta expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 34 % | Inhibition of human full length AurB expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 34.5 % | Inhibition of human full length MARK1 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 34.5 % | Inhibition of human full length SGK3 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 44 % | Inhibition of human ROCK2 catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 45.5 % | Inhibition of human full length MAPKAPK3 expressed in Escherichia coli cell assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 46.5 % | Inhibition of human full length SGK2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 56.5 % | Inhibition of human truncated PKC eta expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 57.5 % | Inhibition of human truncated PKC gamma expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 62.5 % | Inhibition of human full length PKC beta2 expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 64.5 % | Inhibition of human full length AurA expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
| Inhibition (binding) | = 83 % | Inhibition of human AKT1 catalytic domain expressed in baculovirus assessed as substrate phosphorylation using fluorescence-labelled peptides as substrate at 2 uM after 90 mins by microfluidic peptide phosphorylation assay | ChEMBL. | No reference |
Phenotypes
Whole-cell/tissue/organism interactions
We have no records of whole-cell/tissue assays done with this compound
What does this mean?
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.
Annotated phenotypes:
We have no manually annotated phenotypes for this drug.
What does this mean? / Care to help?
In TDR Targets, information about phenotypes that are caused by
drugs, or by genetic manipulation of cells (e.g. gene knockouts or
knockdowns) is manually curated from the literature. These
descriptions help to describe the potential of the target for drug
development. If no information is available for this gene or if the
information is incomplete, this may mean that i) the papers
containing this information either appeared after the curation
effort for this organism was carried out or they were inadvertently
missed by curators; or that ii) the curation effort for this
organism has not yet started.
In any case, if you have information about papers containing relevant validation data for this target, please log in using your TDR Targets username and password and send them to us using the corresponding form in this page (only visible to registered users) or contact us.
In any case, if you have information about papers containing relevant validation data for this target, please log in using your TDR Targets username and password and send them to us using the corresponding form in this page (only visible to registered users) or contact us.
External resources for this compound
- ChEMBL: CHEMBL259141
- PubChem: 11564772
Bibliographic References
1 literature reference was collected for this gene.
If you have references for this compound, please enter them in a user comment (below) or Contact us.