XMU-MP-1 [Ligand Id: 11812] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL4554938 |
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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]
