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ChEMBL ligand: CHEMBL568150 (AS-605240) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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casein kinase 2, alpha prime polypeptide subunit/casein kinase 2, beta polypeptide subunit/casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II in Human (target type: PROTEIN COMPLEX GROUP) [ChEMBL: CHEMBL2095191] [GtoPdb: 1550, 1551, 1549] [UniProtKB: P19784, P67870, P68400] | ||||||||
ChEMBL | Inhibition of CK2 (unknown origin) using RRRDDDSDDD-NH2 as susbtrate incubated for 15 mins in presence of [gamma-32P]ATP | B | 7.7 | pIC50 | 20 | nM | IC50 | Eur J Med Chem (2016) 112: 209-216 [PMID:26896709] |
CDGSH iron-sulfur domain-containing protein 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1795168] [UniProtKB: Q9NZ45] | ||||||||
ChEMBL | Displacement of [3H]-rosiglitazone from human recombinant C-terminal His-tagged cytosolic domain of mitoNEET (32-108) by scintillation proximity assay | B | 5.49 | pIC50 | 3260 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 5498-5501 [PMID:21782425] |
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627] | ||||||||
ChEMBL | Inhibition of tetracycline-inducible EGFP-DYRK1A (unknown origin) expressed in HEK293 cells coexpressing full length human EGFP-tau protein assessed as reduction in tau-Thr212 phosphorylation incubated overnight by immunofluorescence assay | B | 5.8 | pIC50 | 1600 | nM | IC50 | Eur J Med Chem (2016) 112: 209-216 [PMID:26896709] |
ChEMBL | Inhibition of recombinant human N-terminal His6-tagged DYRK1A catalytic domain expressed in Escherichia coli BL21(DE3) cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins in presence of [gamma-32P]ATP | B | 7.52 | pIC50 | 30 | nM | IC50 | Eur J Med Chem (2016) 112: 209-216 [PMID:26896709] |
dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463] | ||||||||
ChEMBL | Inhibition of full length recombinant human GST-tagged DYRK1B expressed in insect cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins in presence of [gamma-32P]ATP | B | 7.1 | pIC50 | 80 | nM | IC50 | Eur J Med Chem (2016) 112: 209-216 [PMID:26896709] |
dual specificity tyrosine phosphorylation regulated kinase 2/Dual-specificity tyrosine-phosphorylation regulated kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630] | ||||||||
ChEMBL | Inhibition of recombinant human N-terminal GST-tagged DYRK2 expressed in Escherichia coli BL21(DE3) cells using KKISGRLSPIMTEQ-NH2 as substrate incubated for 15 mins in presence of [gamma-32P]ATP | B | 7 | pIC50 | 100 | nM | IC50 | Eur J Med Chem (2016) 112: 209-216 [PMID:26896709] |
CDC like kinase 1/Dual specificty protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759] | ||||||||
ChEMBL | Inhibition of recombinant human GST-tagged CLK1 catalytic domain (129 to 484 residues) expressed in Escherichia coli using GRSRSRSRSRSRSRSR as substrate incubated for 15 mins in presence of [gamma-32P]ATP | B | 7.15 | pIC50 | 70 | nM | IC50 | Eur J Med Chem (2016) 112: 209-216 [PMID:26896709] |
epidermal growth factor receptor/Epidermal growth factor receptor erbB1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL203] [GtoPdb: 1797] [UniProtKB: P00533] | ||||||||
ChEMBL | Inhibition of EGFR (unknown origin) incubated for 15 mins in presence of [gamma-32P]ATP | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2016) 112: 209-216 [PMID:26896709] |
Monoamine oxidase B in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2039] [GtoPdb: 2490] [UniProtKB: P27338] | ||||||||
ChEMBL | Inhibition of human recombinant MAO-B after 15 mins | B | 4.89 | pIC50 | 13000 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 5295-5298 [PMID:20650633] |
ChEMBL | Inhibition of human recombinant MAOB by amplex red assay | B | 4.89 | pIC50 | 13000 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 4798-4803 [PMID:21742494] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit alpha/PI3-kinase p110-alpha subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4005] [GtoPdb: 2153] [UniProtKB: P42336] | ||||||||
GtoPdb | - | - | 7.22 | pIC50 | 60 | nM | IC50 | Nat Med (2005) 11: 936-43 [PMID:16127437] |
ChEMBL | Inhibition of PI3Kalpha (unknown origin) by lipid kinase assay | B | 7.22 | pIC50 | 60 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
ChEMBL | Inhibition of PI3Kalpha (unknown origin) | B | 7.22 | pIC50 | 60 | nM | IC50 | Eur J Med Chem (2019) 163: 413-427 [PMID:30530193] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/PI3-kinase p110-beta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] | ||||||||
ChEMBL | Inhibition of PI3Kbeta (unknown origin) | B | 5.57 | pIC50 | 2700 | nM | IC50 | Eur J Med Chem (2019) 163: 413-427 [PMID:30530193] |
ChEMBL | Inhibition of PI3Kbeta (unknown origin) by lipid kinase assay | B | 6.57 | pIC50 | 270 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
GtoPdb | - | - | 6.57 | pIC50 | 270 | nM | IC50 | Nat Med (2005) 11: 936-43 [PMID:16127437] |
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/PI3-kinase p110-delta subunit in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] | ||||||||
GtoPdb | - | - | 6.52 | pIC50 | 300 | nM | IC50 | Nat Med (2005) 11: 936-43 [PMID:16127437] |
ChEMBL | Inhibition of PI3Kdelta (unknown origin) by lipid kinase assay | B | 6.52 | pIC50 | 300 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
ChEMBL | Inhibition of PI3Kdelta (unknown origin) | B | 6.52 | pIC50 | 300 | nM | IC50 | Eur J Med Chem (2019) 163: 413-427 [PMID:30530193] |
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 | Inhibition of human recombinant GST-tagged PI3Kgamma incubated for 180 mins using [33P]gamma-ATP by scintillation proximity assay | B | 8.05 | pIC50 | 9 | nM | IC50 | Bioorg Med Chem (2015) 23: 2953-2974 [PMID:25890697] |
ChEMBL | Inhibition of PI3Kgamma (unknown origin) by lipid kinase assay | B | 8.1 | pIC50 | 8 | nM | IC50 | Medchemcomm (2012) 3: 1337-1355 |
ChEMBL | Inhibition of human recombinant N-terminal GST-tagged PI3K-gamma (39 to 1102 residues) expressed n baculovirus infected TN5 cells using phosphatidylinositol as substrate by scintillation proximity assay in presence of {33P]gammaATP | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2016) 112: 209-216 [PMID:26896709] |
ChEMBL | Inhibition of PI3Kgamma (unknown origin) | B | 8.1 | pIC50 | 8 | nM | IC50 | Eur J Med Chem (2019) 163: 413-427 [PMID:30530193] |
GtoPdb | - | - | 8.1 | pIC50 | 8 | nM | IC50 | Nat Med (2005) 11: 936-43 [PMID:16127437] |
ChEMBL data shown on this page come from version 33:
Mendez D, Gaulton A, Bento AP, Chambers J, De Veij M, Félix E, Magariños MP, Mosquera JF, Mutowo P, Nowotka M, Gordillo-Marañón M, Hunter F, Junco L, Mugumbate G, Rodriguez-Lopez M, Atkinson F, Bosc N, Radoux CJ, Segura-Cabrera A, Hersey A, Leach AR. (2019) 'ChEMBL: towards direct deposition of bioassay data' Nucleic Acids Res., 47(D1). DOI: 10.1093/nar/gky1075. [EPMCID:30398643]
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]