Click here for a description of the charts and data table
Please tell us if you are using this feature and what you think!
ChEMBL ligand: CHEMBL3116050 |
---|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
There should be some charts here, you may need to enable JavaScript!
|
DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
---|---|---|---|---|---|---|---|---|
ALK receptor tyrosine kinase/ALK tyrosine kinase receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4247] [GtoPdb: 1839] [UniProtKB: Q9UM73] | ||||||||
ChEMBL | Inhibition of human ALK | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400] | ||||||||
ChEMBL | Inhibition of human recombinant 6 X His-tagged full length CK2alpha expressed in insect sf21 cells using CK2tide as substrate after 20 mins by fluorescence assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
casein kinase 2, alpha prime polypeptide subunit/Casein kinase II alpha (prime) in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4070] [GtoPdb: 1550] [UniProtKB: P19784] | ||||||||
ChEMBL | Inhibition of human CK2alpha2 | B | 8.57 | pIC50 | 2.7 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
ChEMBL | Inhibition of human FGFR1 | B | 7.3 | pIC50 | 50 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
LIM domain kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3836] [GtoPdb: 2054] [UniProtKB: P53667] | ||||||||
ChEMBL | Inhibition of human LIMK1 | B | 7.2 | pIC50 | 63 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
ChEMBL | Inhibition of human TrkA | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2321619] [GtoPdb: 2269] [UniProtKB: Q9R117] | ||||||||
ChEMBL | Inhibition of Tyk2 in mouse BA/F3 cells expressing TEL-Tyk2 assessed as inhibition of STAT5 phosphorylation by Western blotting analysis | B | 6.62 | pIC50 | 240 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
protein kinase C zeta/Protein kinase C zeta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3438] [GtoPdb: 1491] [UniProtKB: Q05513] | ||||||||
ChEMBL | Inhibition of human PKCzeta | B | 6.7 | pIC50 | 200 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
ChEMBL | Inhibition of human aurora A kinase | B | 7.24 | pIC50 | 58 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
salt inducible kinase 1/Serine/threonine-protein kinase SIK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6082] [GtoPdb: 2197] [UniProtKB: P57059] | ||||||||
ChEMBL | Inhibition of human SIK | B | 6.72 | pIC50 | 190 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519] | ||||||||
ChEMBL | Inhibition of human Abl | B | 7.6 | pIC50 | 25 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
FGR proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase FGR in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4454] [GtoPdb: 2024] [UniProtKB: P09769] | ||||||||
ChEMBL | Inhibition of human Fgr | B | 7.48 | pIC50 | 33 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
GtoPdb | - | - | 8.52 | pIC50 | <3 | nM | IC50 | J Med Chem (2014) 57: 144-58 [PMID:24359159] |
ChEMBL | Inhibition of Jak1 (unknown origin) | B | 8.52 | pIC50 | <3 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
ChEMBL | Inhibition of human JAK2 | B | 8.7 | pIC50 | <2 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
Janus kinase 1/Tyrosine-protein kinase JAK1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2968] [GtoPdb: 2047] [UniProtKB: P52332] | ||||||||
ChEMBL | Inhibition of Jak1 in mouse BA/F3 cells expressing TEL-Jak1 assessed as inhibition of STAT5 phosphorylation by Western blotting analysis | B | 6.59 | pIC50 | 260 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
Janus kinase 2/Tyrosine-protein kinase JAK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2971] [GtoPdb: 2048] [UniProtKB: O60674] | ||||||||
ChEMBL | Inhibition of Jak2 V617F mutant in human SET2 cells assessed as inhibition of STAT5 phosphorylation after 24 hrs by Western blotting analysis | B | 7.27 | pIC50 | 54 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
ChEMBL | Inhibition of Jak2 V617F mutant in human SET2 cells assessed as inhibition of STAT5 phosphorylation after 1 hr by Western blotting analysis | B | 7.52 | pIC50 | 30 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
ChEMBL | Inhibition of Jak2 V617F mutant in human UKE1 cells assessed as inhibition of STAT5 phosphorylation after 24 hrs by Western blotting analysis | B | 8.3 | pIC50 | 5 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
GtoPdb | - | - | 8.52 | pIC50 | <3 | nM | IC50 | J Med Chem (2014) 57: 144-58 [PMID:24359159] |
ChEMBL | Inhibition of Jak2 (unknown origin) | B | 8.52 | pIC50 | <3 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
ChEMBL | Inhibition of Jak2 V617F mutant in human UKE1 cells assessed as inhibition of STAT5 phosphorylation after 1 hr by Western blotting analysis | B | 8.7 | pIC50 | 2 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
Janus kinase 2/Tyrosine-protein kinase JAK2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1649049] [GtoPdb: 2048] [UniProtKB: Q62120] | ||||||||
ChEMBL | Inhibition of Jak2 in mouse BA/F3 cells expressing TEL-Jak2 assessed as inhibition of STAT5 phosphorylation by Western blotting analysis | B | 7.92 | pIC50 | 12 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
ChEMBL | Inhibition of Jak3 (unknown origin) | B | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
GtoPdb | - | - | 6.66 | pIC50 | 220 | nM | IC50 | J Med Chem (2014) 57: 144-58 [PMID:24359159] |
ChEMBL | Inhibition of human JAK3 | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
Janus kinase 3/Tyrosine-protein kinase JAK3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5250] [GtoPdb: 2049] [UniProtKB: Q62137] | ||||||||
ChEMBL | Inhibition of Jak3 in mouse BA/F3 cells expressing TEL-Jak3 assessed as inhibition of STAT5 phosphorylation by Western blotting analysis | B | 5.7 | pIC50 | 2000 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
ChEMBL | Inhibition of human Flt3 | B | 7.35 | pIC50 | 45 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
ChEMBL | Inhibition of human Ret | B | 7.34 | pIC50 | 46 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
ChEMBL | Inhibition of human KDR | B | 7.66 | pIC50 | 22 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
fms related receptor tyrosine kinase 4/Vascular endothelial growth factor receptor 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1955] [GtoPdb: 1814] [UniProtKB: P35916] | ||||||||
ChEMBL | Inhibition of human Flt4 | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2014) 57: 144-158 [PMID:24359159] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]