PF-3644022 [Ligand Id: 8045] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL1231206
  • protein kinase AMP-activated catalytic subunit alpha 1/5`-AMP-activated protein kinase catalytic subunit alpha-1 in Human [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131]
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  • calcium/calmodulin-dependent protein kinase II alpha subunit/Calcium/calmodulin-dependent protein kinase type II subunit alpha in Human [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7]
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  • calcium/calmodulin-dependent protein kinase II beta subunit/Calcium/calmodulin-dependent protein kinase type II subunit beta in Human [ChEMBL: CHEMBL4121] [GtoPdb: 1556] [UniProtKB: Q13554]
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  • cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
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  • cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
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  • MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
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  • MAPK activated protein kinase 3/MAP kinase-activated protein kinase 3 in Human [ChEMBL: CHEMBL4670] [GtoPdb: 2095] [UniProtKB: Q16644]
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  • MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41]
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  • MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase 1 in Human [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
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  • MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
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  • mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683]
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  • phosphorylase kinase catalytic subunit gamma 2/Phosphorylase b kinase gamma catalytic chain, liver/testis isoform in Human [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735]
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  • receptor interacting serine/threonine kinase 2/Receptor-interacting serine/threonine-protein kinase 2 in Human [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
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  • serine/threonine kinase 17a/Serine/threonine-protein kinase 17A in Human [ChEMBL: CHEMBL4525] [GtoPdb: 2214] [UniProtKB: Q9UEE5]
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  • BR serine/threonine kinase 1/Serine/threonine-protein kinase BRSK1 in Human [ChEMBL: CHEMBL5650] [GtoPdb: 1946] [UniProtKB: Q8TDC3]
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  • BR serine/threonine kinase 2/Serine/threonine-protein kinase BRSK2 in Human [ChEMBL: CHEMBL4574] [GtoPdb: 1947] [UniProtKB: Q8IWQ3]
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  • Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
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  • MER proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Mer in Human [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
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  • AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
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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 1/5`-AMP-activated protein kinase catalytic subunit alpha-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4045] [GtoPdb: 1541] [UniProtKB: Q13131]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c PRKAA1 B 6.93 pIC50 117 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c PRKAA1 B 6.93 pIC50 117 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ABCB11/Bile salt export pump in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6020] [GtoPdb: 778] [UniProtKB: O95342]
ChEMBL Inhibition of human BSEP expressed in recombinant baculovirus infected insect Sf9 cell membrane vesicles assessed as [3H]-taurocholate transport preincubated for 5 mins followed by ATP or AMP addition measured after 5 mins by scintillation counting method B 5.15 pIC50 7000 nM IC50 J Med Chem (2016) 59: 3609-3634 [PMID:26502061]
calcium/calmodulin-dependent protein kinase II alpha subunit/Calcium/calmodulin-dependent protein kinase type II subunit alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4147] [GtoPdb: 1555] [UniProtKB: Q9UQM7]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c CAMK2A B 7.15 pIC50 70 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
calcium/calmodulin-dependent protein kinase II beta subunit/Calcium/calmodulin-dependent protein kinase type II subunit beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4121] [GtoPdb: 1556] [UniProtKB: Q13554]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c CAMK2B B 7.15 pIC50 70 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
cyclin dependent kinase 1/Cyclin-dependent kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL308] [GtoPdb: 1961] [UniProtKB: P06493]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c CDK1 B 6.45 pIC50 354 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c CDK1 B 6.45 pIC50 354 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
cyclin dependent kinase 1/Cyclin-dependent kinase 1/cyclin B1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907602] [GtoPdb: 1961] [UniProtKB: P06493, P14635]
ChEMBL Inhibition of CDK1/cycB (unknown origin) B 6.45 pIC50 354 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c CDK5 B 6.04 pIC50 902 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c CDK5 B 6.04 pIC50 902 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of CDK5/p35 (unknown origin) B 6.04 pIC50 902 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
MAPK activated protein kinase 2/MAP kinase-activated protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2208] [GtoPdb: 2094] [UniProtKB: P49137]
ChEMBL Binding affinity to recombinant N-terminal truncated MK2 (45 to 371 residues) (unknown origin) expressed in Escherichia coli assessed as dissociation constant measured after 15 mins by surface plasmon resonance spectroscopy analysis B 8.23 pKd 5.9 nM Kd J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
ChEMBL Inhibition of recombinant MK2 (45 to 400 residues) (unknown origin) using fluorescein isothiocyanate-KKKALSRQLSVAA as substrate B 8.3 pKi 5 nM Ki Nat Rev Drug Discov (2017) 16: 424-440 [PMID:28280261]
GtoPdb - - 8.52 pKi 3 nM Ki J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
ChEMBL Binding affinity to recombinant N-terminal truncated MK2 (45 to 371 residues) (unknown origin) expressed in Escherichia coli assessed as inhibition constant measured after 15 mins by surface plasmon resonance spectroscopy analysis B 8.52 pKi 3 nM Ki J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated IL1b production in hPBM cells)) EUB0000056c MAPKAPK2 F 5.56 pIC50 2780 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated IL8 production in hPBM cells)) EUB0000056c MAPKAPK2 F 5.68 pIC50 2090 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated IL6 production in hPBM cells)) EUB0000056c MAPKAPK2 F 5.9 pIC50 1260 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity On-target Cellular interaction (Western Blot (phosphorylation of the MK2 substrate HSP27 in U937 cells)) EUB0000056c MAPKAPK2 B 6.7 pIC50 201 nM IC50 Affinity On-target Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity On-target Cellular interaction: (Western Blot (phosphorylation of the MK2 substrate HSP27 in U937 cells)) EUB0000056c MAPKAPK2 B 6.7 pIC50 201 nM IC50 Affinity On-target Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of MK2 in human U937 cells assessed as reduction in LPS-stimulated HSP27 phosphorylation at Ser82 preincubated for 1 hr followed by LPS addition measured after 30 mins by Western blot analysis B 6.7 pIC50 201 nM IC50 J Med Chem (2016) 59: 3609-3634 [PMID:26502061]
ChEMBL Affinity Phenotypic Cellular interaction (Cell-based TNFa assay (MesoScale Discovery; inhibition of LPS stimulated TNFa production in human U937 cells)) EUB0000056c MAPKAPK2 F 6.8 pIC50 159 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated TNFa production in human U937 cells)) EUB0000056c MAPKAPK2 F 6.8 pIC50 159 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated TNFa production in hPBM cells)) EUB0000056c MAPKAPK2 F 6.89 pIC50 130 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
GtoPdb - - 8.28 pIC50 5.2 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
ChEMBL Inhibition of recombinant N-terminal truncated MK2 (45 to 371 residues) (unknown origin) expressed in Escherichia coli using KKKALSRQLSVAA as substrate incubated for 1 hr followed by substrate addition in presence of ATP B 8.28 pIC50 5.2 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
ChEMBL Affinity Biochemical interaction (Enzymatic activity assay (Ustate kinase profiler Service; Millipore)) EUB0000056c MAPKAPK2 B 8.3 pIC50 5 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Biochemical interaction: (Enzymatic activity assay (Ustate kinase profiler service, Millipore)) EUB0000056c MAPKAPK2 B 8.3 pIC50 5 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomic Library
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c MAPKAPK2 B 8.3 pIC50 5 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Binding affinity to recombinant MAPKAP-K2 using KKKALSRQLSVAA as substrate after 4 mins by surface plasmon resonance spectroscopic analysis B 8.3 pIC50 5 nM IC50 J Med Chem (2012) 55: 6700-6715 [PMID:22746295]
ChEMBL Inhibition of human MK2 B 8.7 pIC50 2 nM IC50 J Med Chem (2021) 64: 1283-1345 [PMID:33481605]
MAPK activated protein kinase 3/MAP kinase-activated protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4670] [GtoPdb: 2095] [UniProtKB: Q16644]
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated IL1b production in hPBM cells)) EUB0000056c MAPKAPK3 F 5.56 pIC50 2780 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated IL8 production in hPBM cells)) EUB0000056c MAPKAPK3 F 5.68 pIC50 2090 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated IL6 production in hPBM cells)) EUB0000056c MAPKAPK3 F 5.9 pIC50 1260 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated TNFa production in hPBM cells)) EUB0000056c MAPKAPK3 F 6.8 pIC50 160 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction (Cell-based TNFa assay (MesoScale Discovery; inhibition of LPS stimulated TNFa production in human U937 cells)) EUB0000056c MAPKAPK3 F 6.8 pIC50 159 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated TNFa production in human U937 cells)) EUB0000056c MAPKAPK3 F 6.8 pIC50 159 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Biochemical interaction (Enzymatic activity assay (Ustate kinase profiler Service; Millipore)) EUB0000056c MAPKAPK3 B 7.28 pIC50 53 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Biochemical interaction: (Enzymatic activity assay (Ustate kinase profiler service, Millipore)) EUB0000056c MAPKAPK3 B 7.28 pIC50 53 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomic Library
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c MAPKAPK3 B 7.28 pIC50 53 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant MK3 (unknown origin) expressed in Escherichia coli using KKKALSRQLSVAA as substrate incubated for 1 hr followed by substrate addition in presence of ATP B 7.28 pIC50 53 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
MAPK activated protein kinase 5/MAP kinase-activated protein kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3094] [GtoPdb: 2096] [UniProtKB: Q8IW41]
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated IL1b production in hPBM cells)) EUB0000056c MAPKAPK5 F 5.56 pIC50 2780 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated IL8 production in hPBM cells)) EUB0000056c MAPKAPK5 F 5.68 pIC50 2090 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated IL6 production in hPBM cells)) EUB0000056c MAPKAPK5 F 5.9 pIC50 1260 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated TNFa production in hPBM cells)) EUB0000056c MAPKAPK5 F 6.8 pIC50 160 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Phenotypic Cellular interaction (Cell-based TNFa assay (MesoScale Discovery; inhibition of LPS stimulated TNFa production in human U937 cells)) EUB0000056c MAPKAPK5 F 6.8 pIC50 159 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Phenotypic Cellular interaction: (Cell-based TNFa assay (MesoScale Discovery, inhibition of LPS stimulated TNFa production in human U937 cells)) EUB0000056c MAPKAPK5 F 6.8 pIC50 159 nM IC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomic Library
ChEMBL Affinity Biochemical interaction (Enzymatic activity assay (Ustate kinase profiler Service; Millipore)) EUB0000056c MAPKAPK5 B 8.3 pIC50 5 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Biochemical interaction: (Enzymatic activity assay (Ustate kinase profiler service, Millipore)) EUB0000056c MAPKAPK5 B 8.3 pIC50 5 nM IC50 Affinity Biochemical Literature for EUbOPEN Chemogenomic Library
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c MAPKAPK5 B 8.3 pIC50 5 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant PRAK (unknown origin) expressed in Escherichia coli using KKKALSRQLSVAA as substrate incubated for 1 hr followed by substrate addition in presence of ATP B 8.3 pIC50 5 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
MAPK interacting serine/threonine kinase 1/MAP kinase-interacting serine/threonine-protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4718] [GtoPdb: 2104] [UniProtKB: Q9BUB5]
ChEMBL Inhibition of recombinant MNK1 (unknown origin) expressed in Escherichia coli using KKKALSRQLSVAA as substrate incubated for 1 hr followed by substrate addition in presence of ATP B 5.52 pIC50 3000 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
MAPK interacting serine/threonine kinase 2/MAP kinase-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4204] [GtoPdb: 2105] [UniProtKB: Q9HBH9]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c MKNK2 B 6.83 pIC50 148 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c MKNK2 B 6.83 pIC50 148 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of recombinant MNK2 (unknown origin) using KKKALSRQLSVAA as substrate incubated for 1 hr followed by substrate addition in presence of ATP B 6.83 pIC50 148 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
mitogen-activated protein kinase kinase kinase 5/Mitogen-activated protein kinase kinase kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5285] [GtoPdb: 2080] [UniProtKB: Q99683]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c MAP3K5 B 7.22 pIC50 60 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c MAP3K5 B 7.22 pIC50 60 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of ASK1 (unknown origin) B 7.22 pIC50 60 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
phosphorylase kinase catalytic subunit gamma 2/Phosphorylase b kinase gamma catalytic chain, liver/testis isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2349] [GtoPdb: 2147] [UniProtKB: P15735]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c PHKG2 B 6.28 pIC50 528 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c PHKG2 B 6.28 pIC50 528 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of PhKgamma2 (unknown origin) B 6.28 pIC50 528 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
receptor interacting serine/threonine kinase 2/Receptor-interacting serine/threonine-protein kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5014] [GtoPdb: 2190] [UniProtKB: O43353]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c RIPK2 B 6.23 pIC50 590 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c RIPK2 B 6.23 pIC50 590 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of RIPK2 (unknown origin) B 6.23 pIC50 590 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
serine/threonine kinase 17a/Serine/threonine-protein kinase 17A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4525] [GtoPdb: 2214] [UniProtKB: Q9UEE5]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c STK17A B 7.15 pIC50 71 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c STK17A B 7.15 pIC50 71 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of DRAK1 (unknown origin) B 7.15 pIC50 71 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
BR serine/threonine kinase 1/Serine/threonine-protein kinase BRSK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5650] [GtoPdb: 1946] [UniProtKB: Q8TDC3]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c BRSK1 B 6.73 pIC50 187 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c BRSK1 B 6.73 pIC50 187 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of BrSK1 (unknown origin) B 6.73 pIC50 187 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
BR serine/threonine kinase 2/Serine/threonine-protein kinase BRSK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4574] [GtoPdb: 1947] [UniProtKB: Q8IWQ3]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c BRSK2 B 7.05 pIC50 90 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c BRSK2 B 7.05 pIC50 90 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of BrSK2 (unknown origin) B 7.05 pIC50 90 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase pim-1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c PIM1 B 7.06 pIC50 88 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c PIM1 B 7.06 pIC50 88 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of Pim1 (unknown origin) B 7.06 pIC50 88 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
MER proto-oncogene, tyrosine kinase/Tyrosine-protein kinase Mer in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5331] [GtoPdb: 1837] [UniProtKB: Q12866]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c MERTK B 7.12 pIC50 76 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c MERTK B 7.12 pIC50 76 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of Mer (unknown origin) B 7.12 pIC50 76 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]
AXL receptor tyrosine kinase/Tyrosine-protein kinase receptor UFO in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4895] [GtoPdb: 1835] [UniProtKB: P30530]
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore)) EUB0000056c AXL B 6.37 pIC50 428 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Upstate Kinase Profiler service (Millipore, enzymatic assay)) EUB0000056c AXL B 6.37 pIC50 428 nM IC50 Selectivity Literature for EUbOPEN Chemogenomic Library
ChEMBL Inhibition of Axl (unknown origin) B 6.37 pIC50 428 nM IC50 J Pharmacol Exp Ther (2010) 333: 797-807 [PMID:20237073]

ChEMBL data shown on this page come from version 36:

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]