NMS-P715 [Ligand Id: 9401] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1236095 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| protein kinase AMP-activated catalytic subunit alpha 1/AMP-activated protein kinase, alpha-1 subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PRKAA1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3629] [GtoPdb: 1549] [UniProtKB: P68400] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CSNK2A1 | B | 5.24 | pIC50 | 5700 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 2/CDK2/Cyclin A2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941] | ||||||||
| ChEMBL | Inhibition of full length CDK2/Cyclin A (unknown origin) using 5FAMQSPKKG-CONH2 as substrate after 60 mins by fluorescence assay | B | 4 | pIC50 | >100000 | nM | IC50 | J Med Chem (2013) 56: 10045-10065 [PMID:24256217] |
| cell division cycle 7/Cell division cycle 7-related protein kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5443] [GtoPdb: 1960] [UniProtKB: O00311] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDC7 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094127] [GtoPdb: 1961] [UniProtKB: O95067, P06493, P14635, Q8WWL7] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396] | ||||||||
| ChEMBL | Inhibition of CDK2/Cyclin A assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120] |
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin E in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094126] [GtoPdb: 1973] [UniProtKB: O96020, P24864, P24941] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 4/Cyclin-dependent kinase 4/cyclin D1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907601] [GtoPdb: 1976] [UniProtKB: P11802, P24385] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDK4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CDK5 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| TTK protein kinase/Dual specificity protein kinase TTK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3983] [GtoPdb: 2264] [UniProtKB: P33981] | ||||||||
| ChEMBL | Affinity Biochemical interaction: (Enzymatic activity assay) EUB0000612a TTK | B | 9 | pKi | 0.99 | nM | Ki | Affinity Biochemical Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using LS-174Tcell line, 72 h incubation)) EUB0000612a TTK | F | 5.71 | pIC50 | 1955 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using MDA-MB-435S cell line, 72 h incubation)) EUB0000612a TTK | F | 5.71 | pIC50 | 1955 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using LOVO cell line, 72 h incubation)) EUB0000612a TTK | F | 5.73 | pIC50 | 1870 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using MCF-7 cell line, 72 h incubation)) EUB0000612a TTK | F | 5.73 | pIC50 | 1860 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SF295 cell line, 72 h incubation)) EUB0000612a TTK | F | 5.74 | pIC50 | 1821 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using HCC2998 cell line, 72 h incubation)) EUB0000612a TTK | F | 5.74 | pIC50 | 1813 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SW403 cell line, 72 h incubation)) EUB0000612a TTK | F | 5.8 | pIC50 | 1569 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using CL-11 cell line, 72 h incubation)) EUB0000612a TTK | F | 5.88 | pIC50 | 1323 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SW480 cell line, 72 h incubation)) EUB0000612a TTK | F | 5.89 | pIC50 | 1298 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using COLO-320 cell line, 72 h incubation)) EUB0000612a TTK | F | 5.89 | pIC50 | 1284 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using COLO-206F cell line, 72 h incubation)) EUB0000612a TTK | F | 5.91 | pIC50 | 1239 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using BT-474 cell line, 72 h incubation)) EUB0000612a TTK | F | 5.94 | pIC50 | 1157 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using IGROV-1cell line, 72 h incubation)) EUB0000612a TTK | F | 5.94 | pIC50 | 1152 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using BT-549 cell line, 72 h incubation)) EUB0000612a TTK | F | 5.98 | pIC50 | 1049 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using ACHN cell line, 72 h incubation)) EUB0000612a TTK | F | 5.99 | pIC50 | 1015 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using A2780 cell line, 72 h incubation)) EUB0000612a TTK | F | 6 | pIC50 | 1000 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using 786-0 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.04 | pIC50 | 917 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using MDA-MB-231 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.05 | pIC50 | 899 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SU-DHL-6 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.08 | pIC50 | 829 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SF295 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.09 | pIC50 | 807 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using A375 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.1 | pIC50 | 796 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using M14 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.16 | pIC50 | 698 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using A431 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.21 | pIC50 | 619 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using Colo-205 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.23 | pIC50 | 592 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using KM12 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.23 | pIC50 | 586 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SW48 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.26 | pIC50 | 551 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using SW620 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.28 | pIC50 | 519 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using HCT-116 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.33 | pIC50 | 472 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using U251 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.33 | pIC50 | 469 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, inhibition of cell growth in HCT15 cells)) EUB0000612a TTK | F | 6.63 | pIC50 | 232 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Affinity Phenotypic Cellular interaction: (CellTiter-Glo assay (Promega, cell proliferation assay using MOLT4 cell line, 72 h incubation)) EUB0000612a TTK | F | 6.72 | pIC50 | 192 | nM | IC50 | Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of MPS1 assessed as [33P]-gamma-ATP incorporation into substrate P38-betatide by gamma counting | B | 6.74 | pIC50 | 182 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120] |
| ChEMBL | Inhibition of MPS1 (unknown origin) | B | 6.74 | pIC50 | 182 | nM | IC50 | Eur J Med Chem (2019) 175: 247-268 [PMID:31121430] |
| ChEMBL | Inhibition of full-length MPS1 (unknown origin) in presence of ATP | B | 6.74 | pIC50 | 182 | nM | IC50 | J Med Chem (2023) 66: 16484-16514 [PMID:38095579] |
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a TTK | B | 6.74 | pIC50 | 182 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| GtoPdb | - | - | 6.74 | pIC50 | 182 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4507-11 [PMID:21723120] |
| ChEMBL | Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132 | B | 6.8 | pIC50 | 160 | nM | IC50 | J Med Chem (2013) 56: 10045-10065 [PMID:24256217] |
| ChEMBL | Inhibition of MPS1 (unknown origin) | B | 8.1 | pIC50 | 8 | nM | IC50 | J Med Chem (2013) 56: 4343-4356 [PMID:23634759] |
| ChEMBL | Selectivity interaction (Enzymatic assay) EUB0000612a TTK | B | 8.1 | pIC50 | 8 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ChEMBL | Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay | B | 8.15 | pIC50 | 7 | nM | IC50 | J Med Chem (2013) 56: 10045-10065 [PMID:24256217] |
| ChEMBL | Affinity On-target Cellular interaction: (ArrayScan analysis of histone H3 Ser10 phosphorylation in nocodazole-arrested U20S cells) EUB0000612a TTK | B | 7.19 | pEC50 | 65 | nM | EC50 | Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library |
| epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a EGFR | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| eukaryotic translation initiation factor 2 alpha kinase 3/Eukaryotic translation initiation factor 2-alpha kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6030] [GtoPdb: 2017] [UniProtKB: Q9NZJ5] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a EIF2AK3 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| fibroblast growth factor receptor 1/Fibroblast growth factor receptor 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3650] [GtoPdb: 1808] [UniProtKB: P11362] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a FGFR1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein tyrosine kinase 2/Focal adhesion kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2695] [GtoPdb: 2180] [UniProtKB: Q05397] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PTK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a GSK3B | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MET proto-oncogene, receptor tyrosine kinase/Hepatocyte growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3717] [GtoPdb: 1815] [UniProtKB: P08581] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MET | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| component of inhibitor of nuclear factor kappa B kinase complex/Inhibitor of nuclear factor kappa B kinase alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3476] [GtoPdb: 1989] [UniProtKB: O15111] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CHUK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Insulin receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1981] [GtoPdb: 1800] [UniProtKB: P06213] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a INSR | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MAPKAPK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase 1/MAP kinase ERK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4040] [GtoPdb: 1495] [UniProtKB: P28482] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MAPK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| mitogen-activated protein kinase 14/MAP kinase p38 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL260] [GtoPdb: 1499] [UniProtKB: Q16539] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MAPK14 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| MAPK interacting serine/threonine kinase 2/MAP kinase signal-integrating kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MKNK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a MELK | B | 5.22 | pIC50 | 6010 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| BUB1 mitotic checkpoint serine/threonine kinase/Mitotic checkpoint serine/threonine-protein kinase BUB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1772932] [GtoPdb: 1949] [UniProtKB: O43683] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a BUB1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| neurotrophic receptor tyrosine kinase 1/Nerve growth factor receptor Trk-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2815] [GtoPdb: 1817] [UniProtKB: P04629] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a NTRK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| platelet derived growth factor receptor alpha/Platelet-derived growth factor receptor alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2007] [GtoPdb: 1803] [UniProtKB: P16234] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PDGFRA | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein kinase C beta/Protein kinase C beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3045] [GtoPdb: 1483] [UniProtKB: P05771] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PRKCB | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| pyruvate dehydrogenase kinase 1/Pyruvate dehydrogenase kinase isoform 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4766] [GtoPdb: 2915] [UniProtKB: Q15118] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PDK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| AKT serine/threonine kinase 1/Serine/threonine-protein kinase AKT in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4282] [GtoPdb: 1479] [UniProtKB: P31749] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a AKT1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965] | ||||||||
| ChEMBL | Inhibition of N-terminal His-tagged Aurora A (unknown origin) using 5FAM-LRRASLG-CONH2 as substrate after 60 mins by fluorescence assay | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2013) 56: 10045-10065 [PMID:24256217] |
| ChEMBL | Inhibition of Aur-A assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120] |
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a STK6 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a AURKB | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| checkpoint kinase 1/Serine/threonine-protein kinase Chk1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4630] [GtoPdb: 1987] [UniProtKB: O14757] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a CHEK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| eukaryotic elongation factor 2 kinase/Serine/threonine-protein kinase EEF2K in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5026] [GtoPdb: 2014] [UniProtKB: O00418] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a EEF2K | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| histone H3 associated protein kinase/Serine/threonine-protein kinase haspin in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075163] [GtoPdb: 2028] [UniProtKB: Q8TF76] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a GSG2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| serine/threonine-protein kinase MST4/Serine/threonine-protein kinase MST4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a STK26 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| NIMA related kinase 6/Serine/threonine-protein kinase NEK6 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4309] [GtoPdb: 2121] [UniProtKB: Q9HC98] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a NEK6 | B | 5.22 | pIC50 | 6020 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| serine/threonine-protein kinase NIM1/Serine/threonine-protein kinase NIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3542] [GtoPdb: 2291] [UniProtKB: Q8IY84] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a NIM1K | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| p21 (RAC1) activated kinase 4/Serine/threonine-protein kinase PAK 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4482] [GtoPdb: 2136] [UniProtKB: O96013] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PAK4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PIM1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Pim-2 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4523] [GtoPdb: 2159] [UniProtKB: Q9P1W9] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PIM2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| polo like kinase 1/Serine/threonine-protein kinase PLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3024] [GtoPdb: 2168] [UniProtKB: P53350] | ||||||||
| ChEMBL | Inhibition of PLK1 assessed as [33P]-gamma-ATP incorporation into substrate by gamma counting | B | 5 | pIC50 | >10000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4507-4511 [PMID:21723120] |
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PLK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| polo like kinase 2/Serine/threonine-protein kinase PLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5938] [GtoPdb: 2169] [UniProtKB: Q9NYY3] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PLK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| polo like kinase 3/Serine/threonine-protein kinase PLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4897] [GtoPdb: 2170] [UniProtKB: Q9H4B4] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PLK3 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| KIT proto-oncogene, receptor tyrosine kinase/Stem cell growth factor receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1936] [GtoPdb: 1805] [UniProtKB: P10721] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a KIT | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| tyrosine kinase non receptor 2/Tyrosine kinase non-receptor protein 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4599] [GtoPdb: 2246] [UniProtKB: Q07912] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a TNK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a ABL1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| protein tyrosine kinase 6/Tyrosine-protein kinase BRK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4601] [GtoPdb: 2182] [UniProtKB: Q13882] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a PTK6 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a JAK1 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| Janus kinase 3/Tyrosine-protein kinase JAK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2148] [GtoPdb: 2049] [UniProtKB: P52333] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a JAK3 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| LCK proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase LCK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL258] [GtoPdb: 2053] [UniProtKB: P06239] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a LCK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| LYN proto-oncogene, Src family tyrosine kinase/Tyrosine-protein kinase Lyn in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3905] [GtoPdb: 2060] [UniProtKB: P07948] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a LYN | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| fms related receptor tyrosine kinase 3/Tyrosine-protein kinase receptor FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a FLT3 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| ret proto-oncogene/Tyrosine-protein kinase receptor RET in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2041] [GtoPdb: 2185] [UniProtKB: P07949] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a RET | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| spleen associated tyrosine kinase/Tyrosine-protein kinase SYK in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2599] [GtoPdb: 2230] [UniProtKB: P43405] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a SYK | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a TYK2 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| zeta chain of T cell receptor associated protein kinase 70/Tyrosine-protein kinase ZAP-70 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2803] [GtoPdb: 2285] [UniProtKB: P43403] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a ZAP70 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| kinase insert domain receptor/Vascular endothelial growth factor receptor 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL279] [GtoPdb: 1813] [UniProtKB: P35968] | ||||||||
| ChEMBL | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a KDR | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
| 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 | Selectivity interaction (Kinase panel (Enzyme activity assay)) EUB0000612a FLT4 | B | 5 | pIC50 | >10000 | nM | IC50 | Selectivity Literature for EUbOPEN Chemogenomic Library |
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]
