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ChEMBL ligand: CHEMBL408982 |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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bromodomain containing 9/Bromodomain-containing protein 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3108640] [GtoPdb: 2728] [UniProtKB: Q9H8M2] | ||||||||
ChEMBL | Binding affinity to recombinant human His-tagged BRD9 (134 to 239 residues) expressed in Escherichia coli BL21 DE3 assessed as dissociation constant by isothermal titration calorimetry | B | 4.8 | pKd | 16000 | nM | Kd | J Med Chem (2020) 63: 3227-3237 [PMID:32091206] |
ChEMBL | Binding affinity to BRD9 (unknown origin) assessed as dissociation constant by qPCR analysis | B | 5.1 | pKd | 8000 | nM | Kd | J Med Chem (2020) 63: 3227-3237 [PMID:32091206] |
casein kinase 1 delta/Casein kinase I delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] | ||||||||
ChEMBL | Binding affinity to CSNK1D assessed as dissociation constant | B | 6.82 | pKd | 150 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
casein kinase 1 epsilon/Casein kinase I epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] | ||||||||
ChEMBL | Binding affinity to CSNK1E assessed as dissociation constant | B | 6.52 | pKd | 300 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
casein kinase 1 gamma 2/Casein kinase I gamma 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2543] [GtoPdb: 2000] [UniProtKB: P78368] | ||||||||
ChEMBL | Binding affinity to CSNK1G2 assessed as dissociation constant | B | 6.57 | pKd | 270 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
casein kinase 1 gamma 3/Casein kinase I isoform gamma-3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5084] [GtoPdb: 2001] [UniProtKB: Q9Y6M4] | ||||||||
ChEMBL | Binding affinity to CSNK1G3 assessed as dissociation constant | B | 6.54 | pKd | 290 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
CDC like kinase 1/Dual specificity protein kinase CLK1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075280] [GtoPdb: 1990] [UniProtKB: P22518] | ||||||||
GtoPdb | - | - | 8 | pKi | 10 | nM | Ki | Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363] |
ChEMBL | Inhibition of mouse Clk1 | B | 8 | pKi | 10 | nM | Ki | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Inhibition of mouse Clk1 | B | 7.7 | pIC50 | 20 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli DH5[alpha] using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH as substrate by liquid scintillation counting analysis | B | 7.7 | pIC50 | 20 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3654-3661 [PMID:23642479] |
GtoPdb | - | - | 7.7 | pIC50 | 20 | nM | IC50 | Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363] |
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760] | ||||||||
ChEMBL | Binding affinity to Clk2 assessed as dissociation constant | B | 7.02 | pKd | 95 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
CDC like kinase 2/Dual specificity protein kinase CLK2 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075281] [GtoPdb: 1991] [UniProtKB: O35491] | ||||||||
ChEMBL | Inhibition of mouse Clk2 | B | 6.7 | pIC50 | 200 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Inhibition of mouse recombinant GST-tagged CLK2 expressed in Escherichia coli DH5[alpha] using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH as substrate by liquid scintillation counting analysis | B | 6.7 | pIC50 | 200 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3654-3661 [PMID:23642479] |
GtoPdb | - | - | 6.7 | pIC50 | 200 | nM | IC50 | Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363] |
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761] | ||||||||
ChEMBL | Binding affinity to Clk3 assessed as dissociation constant | B | 5.52 | pKd | 3000 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
CDC like kinase 3/Dual specificity protein kinase CLK3 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075282] [GtoPdb: 1992] [UniProtKB: O35492] | ||||||||
ChEMBL | Inhibition of mouse Clk3 | B | 5 | pIC50 | >10000 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1] | ||||||||
ChEMBL | Binding affinity to Clk4 assessed as dissociation constant | B | 7.52 | pKd | 30 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
CDC like kinase 4/Dual specificity protein kinase CLK4 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075283] [GtoPdb: 1993] [UniProtKB: O35493] | ||||||||
ChEMBL | Inhibition of mouse Clk4 | B | 7.82 | pIC50 | 15 | nM | IC50 | Proc Natl Acad Sci U S A (2007) 104: 20523-20528 [PMID:18077363] |
ChEMBL | Inhibition of mouse recombinant GST-tagged CLK4 expressed in Escherichia coli DH5[alpha] using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH as substrate by liquid scintillation counting analysis | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2013) 23: 3654-3661 [PMID:23642479] |
ChEMBL | Inhibition of GST-tagged mouse CLK4 expressed in Escherichia coli using NH2-RSPSYGRSRSRSRSRSRSRSRSNSRSRSY-OH as substrate after 10 mins in presence of [gamma-32]-ATP by scintillation counting method | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2017) 60: 5377-5391 [PMID:28561591] |
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 | Binding affinity to Dyrk1A assessed as dissociation constant | B | 7.92 | pKd | 12 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
ChEMBL | Inhibition of DYRK1A (unknown origin) | B | 6.03 | pIC50 | 930 | nM | IC50 | J Med Chem (2013) 56: 9569-9585 [PMID:24188002] |
ChEMBL | Inhibition of Dyrk1A (unknown origin) | B | 6.03 | pIC50 | 930 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2948-2952 [PMID:26048785] |
ChEMBL | Inhibition of human recombinant full length GST-tagged DYRK1A expressed in baculovirus expression system after 10 mins in presence of [gamma33P-ATP] by liquid scintillation counting analysis | B | 6.03 | pIC50 | 930 | nM | IC50 | J Med Chem (2018) 61: 9791-9810 [PMID:29985601] |
ChEMBL | Inhibition of recombinant Dyrk1A (unknown origin) using KKISGRLSPIMTEQ-NH2 peptide substrate | B | 6.08 | pIC50 | 830 | nM | IC50 | ACS Med Chem Lett (2014) 5: 963-967 [PMID:25221649] |
ChEMBL | Inhibition of Dyrk1A kinase | B | 7.92 | pIC50 | 12 | nM | IC50 | Bioorg Med Chem Lett (2011) 21: 3152-3158 [PMID:21450467] |
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 | Binding affinity to Dyrk1B assessed as dissociation constant | B | 6.89 | pKd | 130 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
CDC like kinase 1/Dual specificty protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759] | ||||||||
ChEMBL | Binding affinity to Clk1 assessed as dissociation constant | B | 7.72 | pKd | 19 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
ChEMBL | Inhibition of recombinant Clk1 (unknown origin) using GRSRSRSRSR peptide substrate | B | 6.77 | pIC50 | 170 | nM | IC50 | ACS Med Chem Lett (2014) 5: 963-967 [PMID:25221649] |
ChEMBL | Inhibition of human C-terminus CLK1 (148 to 484 residues) expressed in Escherichia coli BL21(DE3) using AFRREWSPGKEAKK as substrate preincubated for 10 mins followed by ATP addition by pyruvate kinase-lactate dehydrogenase coupled assay | B | 7.31 | pIC50 | 49 | nM | IC50 | J Med Chem (2017) 60: 5377-5391 [PMID:28561591] |
ChEMBL | Inhibition of recombinant human CLK1 expressed in insect cells using ERMRPRKRQGSVRRRV peptide as substrate after 40 mins in presence of [gamma-33P]-ATP by scintillation counting | B | 7.77 | pIC50 | 17 | nM | IC50 | J Med Chem (2017) 60: 6337-6352 [PMID:28692292] |
CDC like kinase 1 in Mouse [GtoPdb: 1990] [UniProtKB: P22518] | ||||||||
GtoPdb | - | - | 8 | pKi | 10 | nM | Ki | Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363] |
GtoPdb | - | - | 7.7 | pIC50 | 20 | nM | IC50 | Proc Natl Acad Sci USA (2007) 104: 20523-8 [PMID:18077363] |
Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
Pim-1 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2147] [GtoPdb: 2158] [UniProtKB: P11309] | ||||||||
ChEMBL | Binding affinity to PIM1 assessed as dissociation constant | B | 6.89 | pKd | 130 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
Pim-3 proto-oncogene, serine/threonine kinase/Serine/threonine-protein kinase PIM3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5407] [GtoPdb: 2160] [UniProtKB: Q86V86] | ||||||||
ChEMBL | Binding affinity to PIM3 assessed as dissociation constant | B | 6.55 | pKd | 280 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
mitogen-activated protein kinase kinase kinase 19/SPS1/STE20-related protein kinase YSK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL6191] [GtoPdb: 2076] [UniProtKB: Q56UN5] | ||||||||
ChEMBL | Binding affinity to Ysk4 assessed as dissociation constant | B | 6.54 | pKd | 290 | nM | Kd | Bioorg Med Chem Lett (2009) 19: 6700-6705 [PMID:19837585] |
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]