XMU-MP-1 [Ligand Id: 11812] activity data from GtoPdb and ChEMBL

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ChEMBL ligand: CHEMBL4554938
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  • mitogen-activated protein kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase 2 in Human [ChEMBL: CHEMBL5914] [GtoPdb: 2077] [UniProtKB: Q9Y2U5]
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  • mitogen-activated protein kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase 3 in Human [ChEMBL: CHEMBL5970] [GtoPdb: 2078] [UniProtKB: Q99759]
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  • tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
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  • phosphatidylinositol-4-phosphate 5-kinase type 1 gamma/Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma in Human [ChEMBL: CHEMBL1908383] [GtoPdb: 2165] [UniProtKB: O60331]
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  • phosphatidylinositol-5-phosphate 4-kinase type 2 gamma/Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma in Human [ChEMBL: CHEMBL1770034] [GtoPdb: 2163] [UniProtKB: Q8TBX8]
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  • receptor interacting serine/threonine kinase 4/Receptor-interacting serine/threonine-protein kinase 4 in Human [ChEMBL: CHEMBL6083] [GtoPdb: 2192] [UniProtKB: P57078]
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  • serine/threonine kinase 24/Serine/threonine-protein kinase 24 in Human [ChEMBL: CHEMBL5082] [GtoPdb: 2217] [UniProtKB: Q9Y6E0]
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  • serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
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  • serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188]
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  • serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043]
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  • doublecortin like kinase 1/Serine/threonine-protein kinase DCLK1 in Human [ChEMBL: CHEMBL5683] [GtoPdb: 2005] [UniProtKB: O15075]
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  • TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3]
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  • TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54]
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  • TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8]
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  • unc-51 like autophagy activating kinase 2/Serine/threonine-protein kinase ULK2 in Human [ChEMBL: CHEMBL5435] [GtoPdb: 2272] [UniProtKB: Q8IYT8]
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  • ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
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  • Janus kinase 1/Tyrosine-protein kinase JAK1 in Human [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
aurora kinase A/Aurora kinase A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b STK6 B 7.89 pKd 13 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to AURKA (unknown origin) assessed as dissociation constant B 7.89 pKd 13 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b STK6 B 7.71 pIC50 19.4 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of AURKA (unknown origin) in presence of ATP by enzymatic assay B 7.71 pIC50 19.4 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
aurora kinase B/Aurora kinase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b AURKB B 7.4 pKd 40 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to AURKB (unknown origin) assessed as dissociation constant B 7.4 pKd 40 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b AURKB B 7.71 pIC50 19.4 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of AURKB (unknown origin) in presence of ATP by enzymatic assay B 7.72 pIC50 19.1 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
mitogen-activated protein kinase kinase kinase 2/Mitogen-activated protein kinase kinase kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5914] [GtoPdb: 2077] [UniProtKB: Q9Y2U5]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b MAP3K2 B 7.72 pKd 19 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to MAP3K2 (unknown origin) assessed as dissociation constant B 7.72 pKd 19 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b MAP3K2 B 7.1 pIC50 79.6 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of MAP3K2 (unknown origin) in presence of ATP by enzymatic assay B 7.1 pIC50 79.6 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
mitogen-activated protein kinase kinase kinase 3/Mitogen-activated protein kinase kinase kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5970] [GtoPdb: 2078] [UniProtKB: Q99759]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b MAP3K3 B 7.57 pKd 27 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to MAP3K3 (unknown origin) assessed as dissociation constant B 7.57 pKd 27 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of MAP3K3 (unknown origin) in presence of ATP by enzymatic assay B 7.42 pIC50 38.4 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b MAP3K3 B 7.46 pIC50 34.8 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
tyrosine kinase 2/Non-receptor tyrosine-protein kinase TYK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b TYK2 B 6.21 pKd 610 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to TYK2 JH1domain-catalytic (unknown origin) assessed as dissociation constant B 8.3 pKd 5 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b TYK2 B 6.6 pIC50 254 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of TYK2 JH1domain-catalytic (unknown origin) in presence of ATP by enzymatic assay B 8.72 pIC50 1.9 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336]
ChEMBL Binding affinity to PIK3CA H1047L mutant (unknown origin) assessed as dissociation constant B 7.47 pKd 34 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit gamma isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b PIK3CG B 8.08 pKd 8.4 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to PIK3CG (unknown origin) assessed as dissociation constant B 8.32 pKd 4.8 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b PIK3CG B 7.42 pIC50 38.4 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of PIK3CG (unknown origin) in presence of ATP by enzymatic assay B 7.42 pIC50 38.4 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
phosphatidylinositol-4-phosphate 5-kinase type 1 gamma/Phosphatidylinositol 4-phosphate 5-kinase type-1 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1908383] [GtoPdb: 2165] [UniProtKB: O60331]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b PIP5K1C B 7.11 pKd 77 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to PIP5K1C (unknown origin) assessed as dissociation constant B 7.11 pKd 77 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b PIP5K1C B 6.36 pIC50 436 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of PIP5K1C (unknown origin) in presence of ATP by enzymatic assay B 6.36 pIC50 436 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
phosphatidylinositol-5-phosphate 4-kinase type 2 gamma/Phosphatidylinositol 5-phosphate 4-kinase type-2 gamma in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1770034] [GtoPdb: 2163] [UniProtKB: Q8TBX8]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b PIP4K2C B 7.47 pKd 34 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to PIP5K2C (unknown origin) assessed as dissociation constant B 7.47 pKd 34 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
receptor interacting serine/threonine kinase 4/Receptor-interacting serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6083] [GtoPdb: 2192] [UniProtKB: P57078]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b RIPK4 B 6.85 pKd 140 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to RIPK4 (unknown origin) assessed as dissociation constant B 6.85 pKd 140 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
serine/threonine kinase 24/Serine/threonine-protein kinase 24 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5082] [GtoPdb: 2217] [UniProtKB: Q9Y6E0]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b STK24 B 7.74 pKd 18 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to MST3 (unknown origin) assessed as dissociation constant B 7.74 pKd 18 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b STK24 B 7.35 pIC50 44.8 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of MST3 (unknown origin) in presence of ATP by enzymatic assay B 7.35 pIC50 44.8 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
serine/threonine-protein kinase MST4/Serine/threonine-protein kinase 26 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b STK26 B 7.8 pKd 16 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to MST4 (unknown origin) assessed as dissociation constant B 7.8 pKd 16 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b STK26 B 7.56 pIC50 27.3 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of MST4 (unknown origin) in presence of ATP by enzymatic assay B 7.56 pIC50 27.3 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
serine/threonine kinase 3/Serine/threonine-protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188]
ChEMBL Affinity Biochemical interaction (Competition binding assay (DiscoverX)) EUB0000178b STK3 B 7.96 pKd 11 nM Kd Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to MST2 (unknown origin) assessed as dissociation constant B 7.96 pKd 11 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of recombinant His-tagged full-length MST2 Y101F/D109A mutant (unknown origin) expressing in Escherichia coli assessed as MOB1 phosphorylation level incubated for 15 min by immunoblot analysis B 5.78 pIC50 1678 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Displacement of K5 tracer from full length C-terminal NanoLuc fused human STK3 expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay B 5.82 pIC50 1510 nM IC50 J Med Chem (2022) 65: 1352-1369 [PMID:34807584]
ChEMBL Inhibition of recombinant His-tagged full-length MST2 (unknown origin) expressing in Escherichia coli assessed as MOB1a phosphorylation level incubated for 30 min in the presence of 300 uM ATP by immunoblot analysis B 5.82 pIC50 1498 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of recombinant His-tagged full-length MST2 D109A mutant (unknown origin) expressing in Escherichia coli assessed as MOB1 phosphorylation level incubated for 15 min by immunoblot analysis B 5.98 pIC50 1040 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of MST2 (unknown origin) B 6.31 pIC50 493 nM IC50 J Med Chem (2024) 67: 3813-3842 [PMID:38422480]
ChEMBL Inhibition of recombinant His-tagged full-length MST2 Y101F mutant (unknown origin) expressing in Escherichia coli assessed as MOB1 phosphorylation level incubated for 15 min by immunoblot analysis B 6.44 pIC50 361.1 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of recombinant His-tagged full-length MST2 (unknown origin) expressing in Escherichia coli assessed as MOB1a phosphorylation level incubated for 30 min in the presence of 100 uM ATP by immunoblot analysis B 6.55 pIC50 280 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of recombinant His-tagged full-length MST2 (unknown origin) expressing in Escherichia coli assessed as MOB1a phosphorylation level incubated for 30 min in the presence of 30 uM ATP by immunoblot analysis B 6.75 pIC50 177 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
GtoPdb - - 6.79 pIC50 162 nM IC50 J Med Chem (2022) 65: 1352-1369 [PMID:34807584]
ChEMBL Inhibition of recombinant His-tagged full-length MST2 (unknown origin) expressing in Escherichia coli assessed as MOB1 phosphorylation level incubated for 15 min by immunoblot analysis B 7.41 pIC50 38.8 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of recombinant His-tagged full-length MST2 (unknown origin) expressing in Escherichia coli assessed as GST-tagged MOB1a phosphorylation level incubated for 30 mins by immunoblot analysis B 7.42 pIC50 38.2 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of Flag-tagged full-length MST2 (unknown origin) transfected in HEK293T cells assessed as MOB1a phosphorylation level incubated for 3 hrs by immunoblot analysis B 7.42 pIC50 38.1 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (ELISA-based kinase assay (inhibition of MOB1a phosphorylation at 11.2 µM ATP)) EUB0000178b STK3 B 7.42 pIC50 38.1 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of recombinant His-tagged full-length MST2 (unknown origin) expressing in Escherichia coli assessed as MOB1a phosphorylation level incubated for 30 min in the presence of 10 uM ATP by immunoblot analysis B 7.47 pIC50 34 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of MST2 (unknown origin) in presence of ATP by enzymatic assay B 7.74 pIC50 18.2 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b STK3 B 7.74 pIC50 18.2 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Affinity Phenotypic Cellular interaction (Immunoblotting (phosphorylation of endogenous MOB1; LATS1/2; and YAP in human liver carcinoma (HepG2) cells)) EUB0000178b STK3 B 7 pEC50 >100 nM EC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
serine/threonine kinase 4/Serine/threonine-protein kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043]
ChEMBL Affinity Biochemical interaction (Competition binding assay (DiscoverX)) EUB0000178b STK4 B 7.77 pKd 17 nM Kd Affinity Biochemical Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to MST1 (unknown origin) assessed as dissociation constant B 7.77 pKd 17 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of recombinant His-tagged full-length MST1 (unknown origin) expressing in Escherichia coli assessed as MOB1a phosphorylation level incubated for 30 min in the presence of 300 uM ATP by immunoblot analysis B 5.39 pIC50 4036 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of recombinant His-tagged full-length MST1 (unknown origin) expressing in Escherichia coli assessed as MOB1a phosphorylation level incubated for 30 min in the presence of 100 uM ATP by immunoblot analysis B 5.91 pIC50 1228 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Displacement of K5 tracer from full length C-terminal NanoLuc fused human STK4 expressed in HEK293T cells incubated for 2 hrs by NanoBRET assay B 5.98 pIC50 1040 nM IC50 J Med Chem (2022) 65: 1352-1369 [PMID:34807584]
GtoPdb - - 6.31 pIC50 493 nM IC50 J Med Chem (2022) 65: 1352-1369 [PMID:34807584]
ChEMBL Inhibition of recombinant His-tagged full-length MST1 (unknown origin) expressing in Escherichia coli assessed as MOB1a phosphorylation level incubated for 30 min in the presence of 30 uM ATP by immunoblot analysis B 6.42 pIC50 378 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of recombinant His-tagged full-length MST1 (unknown origin) expressing in Escherichia coli assessed as MOB1a phosphorylation level incubated for 30 min in the presence of 10 uM ATP by immunoblot analysis B 6.79 pIC50 164 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of MST1 (unknown origin) B 6.79 pIC50 162 nM IC50 J Med Chem (2024) 67: 3813-3842 [PMID:38422480]
ChEMBL Inhibition of recombinant full length N-terminal GST -tagged human MST1 expressed in baculovirus infected Sf9 insect cells using KKSRGDYMTMQIG as substrate incubated for 1 hr in presence of ATP by ADP-Glo luminescent assay B 6.98 pIC50 104 nM IC50 J Med Chem (2022) 65: 11818-11839 [PMID:36037148]
ChEMBL Selectivity interaction (ELISA-based kinase assay (inhibition of MOB1a phosphorylation at 11.2 µM ATP)) EUB0000178b STK4 B 7.15 pIC50 71.1 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of Flag-tagged full-length MST1 (unknown origin) transfected in HEK293T cells assessed as MOB1a phosphorylation level incubated for 3 hrs by immunoblot analysis B 7.15 pIC50 71.1 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Inhibition of recombinant His-tagged full-length MST1 (unknown origin) expressing in Escherichia coli assessed as MOB1 phosphorylation level incubated for 15 min by immunoblot analysis B 7.15 pIC50 70.7 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b STK4 B 8.01 pIC50 9.8 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of MST1 (unknown origin) in presence of ATP by enzymatic assay B 8.01 pIC50 9.8 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Affinity Phenotypic Cellular interaction (Immunoblotting (phosphorylation of endogenous MOB1; LATS1/2; and YAP in human liver carcinoma (HepG2) cells)) EUB0000178b STK4 B 7 pEC50 >100 nM EC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
doublecortin like kinase 1/Serine/threonine-protein kinase DCLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5683] [GtoPdb: 2005] [UniProtKB: O15075]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b DCLK1 B 7.6 pKd 25 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to DCAMKL1 (unknown origin) assessed as dissociation constant B 7.6 pKd 25 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b DCLK1 B 7.55 pIC50 27.9 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of DCAMKL1 (unknown origin) in presence of ATP by enzymatic assay B 7.55 pIC50 27.9 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b TAOK1 B 6.74 pKd 180 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to TAOK1 (unknown origin) assessed as dissociation constant B 6.74 pKd 180 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b TAOK1 B 6.78 pIC50 165 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of TAOK1 (unknown origin) in presence of ATP by enzymatic assay B 6.78 pIC50 165 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
TAO kinase 2/Serine/threonine-protein kinase TAO2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075195] [GtoPdb: 2234] [UniProtKB: Q9UL54]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b TAOK2 B 7 pKd 100 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to TAOK2 (unknown origin) assessed as dissociation constant B 7 pKd 100 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b TAOK2 B 6.87 pIC50 134 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of TAOK2 (unknown origin) in presence of ATP by enzymatic assay B 6.87 pIC50 134 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
TAO kinase 3/Serine/threonine-protein kinase TAO3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5701] [GtoPdb: 2235] [UniProtKB: Q9H2K8]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b TAOK3 B 6.21 pKd 610 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to TAOK3 (unknown origin) assessed as dissociation constant B 6.21 pKd 610 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b TAOK3 B 6.6 pIC50 254 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of TAOK3 (unknown origin) in presence of ATP by enzymatic assay B 6.6 pIC50 254 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
unc-51 like autophagy activating kinase 2/Serine/threonine-protein kinase ULK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5435] [GtoPdb: 2272] [UniProtKB: Q8IYT8]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b ULK2 B 7.46 pKd 35 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to ULK2 (unknown origin) assessed as dissociation constant B 7.46 pKd 35 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b ULK2 B 7.38 pIC50 41.5 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of ULK2 (unknown origin) in presence of ATP by enzymatic assay B 7.38 pIC50 41.5 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ABL proto-oncogene 1, non-receptor tyrosine kinase/Tyrosine-protein kinase ABL1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1862] [GtoPdb: 1923] [UniProtKB: P00519]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b ABL1 B 7.38 pKd 42 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to phosphorylated ABL1 M351T mutant (unknown origin) assessed as dissociation constant B 7.38 pKd 42 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b ABL1 B 7.62 pKd 24 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to phosphorylated ABL1 Q252H mutant (unknown origin) assessed as dissociation constant B 7.62 pKd 24 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b ABL1 B 7.85 pKd 14 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b ABL1 B 7.75 pIC50 17.6 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of phosphorylated ABL1 M351T mutant (unknown origin) in presence of ATP by enzymatic assay B 7.75 pIC50 17.6 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b ABL1 B 7.78 pIC50 16.6 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b ABL1 B 7.94 pIC50 11.6 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of phosphorylated ABL1 Q252H mutant (unknown origin) in presence of ATP by enzymatic assay B 7.94 pIC50 11.6 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]
Janus kinase 1/Tyrosine-protein kinase JAK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2835] [GtoPdb: 2047] [UniProtKB: P23458]
ChEMBL Selectivity interaction (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b JAK1@kinase 2 B 7.66 pKd 22 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Binding affinity to JAK1 JH2domain-pseudokinase (unknown origin) assessed as dissociation constant B 7.66 pKd 22 nM Kd Sci Transl Med (2016) 8: null-null [PMID:27535619]
ChEMBL Selectivity interaction (Enzymatic assay) EUB0000178b JAK1@kinase 2 B 7.41 pIC50 38.7 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
ChEMBL Inhibition of JAK1 JH2domain-pseudokinase (unknown origin) in presence of ATP by enzymatic assay B 7.41 pIC50 38.7 nM IC50 Sci Transl Med (2016) 8: null-null [PMID:27535619]

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]