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ChEMBL ligand: CHEMBL3116050 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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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 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]