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

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ChEMBL ligand: CHEMBL4554938
  • 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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  • 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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  • phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit in Human [ChEMBL: CHEMBL3267] [GtoPdb: 2156] [UniProtKB: P48736]
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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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  • aurora kinase A/Serine/threonine-protein kinase Aurora-A in Human [ChEMBL: CHEMBL4722] [GtoPdb: 1936] [UniProtKB: O14965]
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  • aurora kinase B/Serine/threonine-protein kinase Aurora-B in Human [ChEMBL: CHEMBL2185] [GtoPdb: 1937] [UniProtKB: Q96GD4]
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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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  • serine/threonine kinase 4/Serine/threonine-protein kinase MST1 in Human [ChEMBL: CHEMBL4598] [GtoPdb: 2225] [UniProtKB: Q13043]
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  • serine/threonine kinase 3/Serine/threonine-protein kinase MST2 in Human [ChEMBL: CHEMBL4708] [GtoPdb: 2219] [UniProtKB: Q13188]
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  • serine/threonine-protein kinase MST4/Serine/threonine-protein kinase MST4 in Human [ChEMBL: CHEMBL5941] [GtoPdb: 2287] [UniProtKB: Q9P289]
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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 ABL 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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  • tyrosine kinase 2/Tyrosine-protein kinase TYK2 in Human [ChEMBL: CHEMBL3553] [GtoPdb: 2269] [UniProtKB: P29597]
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DB Assay description Assay Type Standard value Standard parameter Original value Original units Original parameter Reference
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 Selectivity interaction (Enzymatic assay) EUB0000178b MAP3K2 B 7.1 pIC50 79.6 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Selectivity interaction (Enzymatic assay) EUB0000178b MAP3K3 B 7.46 pIC50 34.8 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Selectivity interaction (Enzymatic assay) EUB0000178b PIP5K1C B 6.36 pIC50 436 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma/PI3-kinase p110-gamma subunit 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 Selectivity interaction (Enzymatic assay) EUB0000178b PIK3CG B 7.42 pIC50 38.4 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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
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 Selectivity interaction (Enzymatic assay) EUB0000178b STK24 B 7.35 pIC50 44.8 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
aurora kinase A/Serine/threonine-protein kinase Aurora-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 Selectivity interaction (Enzymatic assay) EUB0000178b STK6 B 7.71 pIC50 19.4 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
aurora kinase B/Serine/threonine-protein kinase Aurora-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 Selectivity interaction (Enzymatic assay) EUB0000178b AURKB B 7.71 pIC50 19.4 nM IC50 Selectivity 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 Selectivity interaction (Enzymatic assay) EUB0000178b DCLK1 B 7.55 pIC50 27.9 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
serine/threonine kinase 4/Serine/threonine-protein kinase MST1 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 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 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 Selectivity interaction (Enzymatic assay) EUB0000178b STK4 B 8.01 pIC50 9.8 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 STK4 B 7 pEC50 >100 nM EC50 Affinity Phenotypic Cellular Literature for EUbOPEN Chemogenomics Library wave 3
serine/threonine kinase 3/Serine/threonine-protein kinase MST2 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 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]
GtoPdb - - 6.79 pIC50 162 nM IC50 J Med Chem (2022) 65: 1352-1369 [PMID:34807584]
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 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-protein kinase MST4/Serine/threonine-protein kinase MST4 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 Selectivity interaction (Enzymatic assay) EUB0000178b STK26 B 7.56 pIC50 27.3 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Selectivity interaction (Enzymatic assay) EUB0000178b TAOK1 B 6.78 pIC50 165 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Selectivity interaction (Enzymatic assay) EUB0000178b TAOK2 B 6.87 pIC50 134 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Selectivity interaction (Enzymatic assay) EUB0000178b TAOK3 B 6.6 pIC50 254 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 Selectivity interaction (Enzymatic assay) EUB0000178b ULK2 B 7.38 pIC50 41.5 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 (KinomeScan (DiscoverX, competition-binding assay)) EUB0000178b ABL1 B 7.38 pKd 42 nM Kd Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
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 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 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
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 Selectivity interaction (Enzymatic assay) EUB0000178b JAK1@kinase 2 B 7.41 pIC50 38.7 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3
tyrosine kinase 2/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 Selectivity interaction (Enzymatic assay) EUB0000178b TYK2 B 6.6 pIC50 254 nM IC50 Selectivity Literature for EUbOPEN Chemogenomics Library wave 3

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]