ChEMBL ligand: CHEMBL393525
casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 9/CDK9/cyclin T1 in Human [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613] There should be some charts here, you may need to enable JavaScript!
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750] There should be some charts here, you may need to enable JavaScript!
CDC like kinase 1/Dual specificity protein kinase CLK1 in Human [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759] There should be some charts here, you may need to enable JavaScript!
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760] There should be some charts here, you may need to enable JavaScript!
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761] There should be some charts here, you may need to enable JavaScript!
CDC like kinase 4/Dual specificity protein kinase CLK4 in Human [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1] There should be some charts here, you may need to enable JavaScript!
dual specificity tyrosine phosphorylation regulated kinase 1A/Dual specificity tyrosine-phosphorylation-regulated kinase 1A in Human [ChEMBL: CHEMBL2292] [GtoPdb: 2009] [UniProtKB: Q13627] There should be some charts here, you may need to enable JavaScript!
dual specificity tyrosine phosphorylation regulated kinase 1B/Dual specificity tyrosine-phosphorylation-regulated kinase 1B in Human [ChEMBL: CHEMBL5543] [GtoPdb: 2010] [UniProtKB: Q9Y463] There should be some charts here, you may need to enable JavaScript!
dual specificity tyrosine phosphorylation regulated kinase 2/Dual specificity tyrosine-phosphorylation-regulated kinase 2 in Human [ChEMBL: CHEMBL4376] [GtoPdb: 2011] [UniProtKB: Q92630] There should be some charts here, you may need to enable JavaScript!
dual specificity tyrosine phosphorylation regulated kinase 3/Dual specificity tyrosine-phosphorylation-regulated kinase 3 in Human [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781] There should be some charts here, you may need to enable JavaScript!
dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20] There should be some charts here, you may need to enable JavaScript!
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841] There should be some charts here, you may need to enable JavaScript!
maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680] There should be some charts here, you may need to enable JavaScript!
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] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform in Human [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform in Human [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329] There should be some charts here, you may need to enable JavaScript!
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888] There should be some charts here, you may need to enable JavaScript!
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma in Human [GtoPdb: 2156] [UniProtKB: P48736] There should be some charts here, you may need to enable JavaScript!
protein kinase, DNA-activated, catalytic subunit in Human [GtoPdb: 2800] [UniProtKB: P78527] There should be some charts here, you may need to enable JavaScript!

DB	Assay description	Assay Type	Standard value	Standard parameter	Original value	Original units	Original parameter	Reference
casein kinase 1 epsilon/Casein kinase I isoform epsilon in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4937] [GtoPdb: 1998] [UniProtKB: P49674]
ChEMBL	Inhibition of recombinant human CK1epsilon expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	6.39	pIC50	405	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750]
ChEMBL	Inhibition of recombinant human CDK9/cyclin-T1 using H-YSPTSPSYSPTSPSYSPTSPS-KKKK-OH as substrate after 90 mins by luminescence assay	B	8.86	pIC50	1.37	nM	IC50	Bioorg Med Chem (2015) 23: 6280-6296 [PMID:26349627]
cyclin dependent kinase 2/Cyclin-dependent kinase 2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL301] [GtoPdb: 1973] [UniProtKB: P24941]
ChEMBL	Binding affinity to full length human CDK2 (1 to 298 residues) expressed in bacterial expression system by KINOMEscan competition assay	B	6.27	pKd	540	nM	Kd	J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
ChEMBL	Binding affinity to CDK2 (unknown origin) assessed as dissociation constant	B	6.27	pKd	540	nM	Kd	J Med Chem (2024) 67: 5185-5215 [PMID:38564299]
cyclin dependent kinase 5/Cyclin-dependent kinase 5/CDK5 activator 1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL1907600] [GtoPdb: 1977] [UniProtKB: Q00535, Q15078]
ChEMBL	Inhibition of recombinant human CDK5/p25 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	7.61	pIC50	24.5	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
cyclin dependent kinase 7/Cyclin-dependent kinase 7 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3055] [GtoPdb: 1979] [UniProtKB: P50613]
ChEMBL	Binding affinity to full length human CDK7 (1 to 344 residues) expressed in mammalian expression system by KINOMEscan competition assay	B	8.6	pKd	2.5	nM	Kd	J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
cyclin dependent kinase 9/Cyclin-dependent kinase 9 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3116] [GtoPdb: 1981] [UniProtKB: P50750]
ChEMBL	Binding affinity to full length human CDK9 (1 to 372 residues) expressed in bacterial expression system by KINOMEscan competition assay	B	8.39	pKd	4.1	nM	Kd	J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
ChEMBL	Binding affinity to CDK9 (unknown origin) assessed as dissociation constant	B	8.39	pKd	4.1	nM	Kd	J Med Chem (2024) 67: 5185-5215 [PMID:38564299]
ChEMBL	Inhibition of CDK9 (unknown origin)	B	8.85	pIC50	1.4	nM	IC50	J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
CDC like kinase 1/Dual specificity protein kinase CLK1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4224] [GtoPdb: 1990] [UniProtKB: P49759]
ChEMBL	Binding affinity to human CLK1 assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay	B	10.25	pKd	0.06	nM	Kd	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL	Inhibition of recombinant human CLK1 expressed in Sf9 insect cells using myelin basic protein as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay	B	7.51	pIC50	30.8	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL	Inhibition of recombinant human CLK1 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	7.73	pIC50	18.8	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
CDC like kinase 2/Dual specificity protein kinase CLK2 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4225] [GtoPdb: 1991] [UniProtKB: P49760]
ChEMBL	Inhibition of recombinant human CLK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	8.96	pIC50	1.1	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
CDC like kinase 3/Dual specificity protein kinase CLK3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4226] [GtoPdb: 1992] [UniProtKB: P49761]
ChEMBL	Inhibition of recombinant human CLK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	7.92	pIC50	11.9	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
CDC like kinase 4/Dual specificity protein kinase CLK4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4203] [GtoPdb: 1993] [UniProtKB: Q9HAZ1]
ChEMBL	Inhibition of recombinant human CLK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	8.16	pIC50	6.9	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
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 human DYRK1A assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay	B	10.05	pKd	0.09	nM	Kd	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL	Inhibition of recombinant human DYRK1A expressed in Escherichia coli using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay	B	8.15	pIC50	7	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL	Inhibition of recombinant human DYRK1A expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	8.2	pIC50	6.3	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
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 recombinant human DYRK1B expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	8.43	pIC50	3.7	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL	Inhibition of recombinant human DYRK1B expressed in Sf9 insect cells using DYRKtide peptide as substrate incubated for 110 mins in presence of ATP by non-radioactive ADP-Glo luminescence microplate reader assay	B	8.47	pIC50	3.4	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
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 DYRK2 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	6.93	pIC50	117.6	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 3/Dual specificity tyrosine-phosphorylation-regulated kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4575] [GtoPdb: 2012] [UniProtKB: O43781]
ChEMBL	Inhibition of recombinant human DYRK3 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	7.98	pIC50	10.4	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
dual specificity tyrosine phosphorylation regulated kinase 4/Dual specificity tyrosine-phosphorylation-regulated kinase 4 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075115] [GtoPdb: 2013] [UniProtKB: Q9NR20]
ChEMBL	Inhibition of recombinant human DYRK4 expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	5.59	pIC50	2589	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
glycogen synthase kinase 3 beta/Glycogen synthase kinase-3 beta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL262] [GtoPdb: 2030] [UniProtKB: P49841]
ChEMBL	Binding affinity to human GSK-3beta assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay	B	8.41	pKd	3.93	nM	Kd	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL	Inhibition of recombinant human GSK-3beta expressed in Sf9 insect cells incubated for 60 mins in presence of ATP and [gamma33-P] ATP by radiometric scintillation counter analysis	B	7.75	pIC50	17.6	nM	IC50	J Med Chem (2023) 66: 4106-4130 [PMID:36876904]
ChEMBL	Inhibition of GSK-3beta (unknown origin) expressed in Sf9 cells by spectrometry based analysis	B	8	pIC50	10	nM	IC50	Bioorg Med Chem (2023) 92: 117406-117406 [PMID:37536264]
maternal embryonic leucine zipper kinase/Maternal embryonic leucine zipper kinase in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4578] [GtoPdb: 2102] [UniProtKB: Q14680]
ChEMBL	MELK Inhibitor Library Screening assay: MELK and its substrate, Bcl-G were both recombinantly expressed and purified for use in screening assays (See Methods). 752 compounds from an in-house curated inhibitor library were subjected to a p81-based kinase assay. 10 nM MELK 340 and 10 μM Bcl-GL in kinase assay buffer (50 mM HEPES pH 7.5, 100 mM KCl, 0.1 mM EDTA, 0.1 mM EGTA, 10 mM MgCl2, 10 μg/mL BSA) with 10 mM DTT were added to either 10 μM or 1 μM inhibitor aliquoted into 96 well plates (final 1% DMSO). The mixture was incubated at room temperature for 30 minutes prior to initiation of the assay with 40 μM γ-32P-ATP (100-1000 CPM/pmol). 40 μL aliquots were spotted onto a p81 96 well filter plate (Unifilter, Whatman), quenched, and washed with 75 mM O-phosphoric acid 8 times, followed by a final wash with acetone for drying. Wells were then filled with scintillation fluid, sealed, and quantified using a MicroBeta TriLux liquid scintillation counter (PerkinElmer). Each inhibitor plate was assayed in duplicate, with at least 4 wells without MELK to establish background and at least 4 wells without inhibitor as a negative control. All readings were corrected for background signal based on the average counts from the wells without enzyme. Percent inhibition, defined as [100−(CPM+inhibitor/average CPM of positive controls)*100], was determined first at 10 μM inhibitor. The top 50 inhibitors were then re-screened in duplicate at 1 μM.	B	6.4	pIC50	400	nM	IC50	US-10981896-B2. Indolinone derivatives as inhibitors of maternal embryonic leucine zipper kinase (2021)
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	Inhibition of human recombinant p110alpha	B	8.11	pIC50	7.8	nM	IC50	Bioorg Med Chem (2007) 15: 7677-7687 [PMID:17869522]
ChEMBL	Inhibition of PI3K alpha (unknown origin)	B	8.24	pIC50	5.8	nM	IC50	J Med Chem (2022) 65: 893-921 [PMID:33539089]
GtoPdb	-	-	8.24	pIC50	5.8	nM	IC50	Cell (2006) 125: 733-47 [PMID:16647110]
ChEMBL	Inhibition of PI3Kalpha (unknown origin) by radiometric assay	B	9.3	pIC50	0.5	nM	IC50	Bioorg Med Chem (2015) 23: 6280-6296 [PMID:26349627]
ChEMBL	Inhibition of PI3Kalpha (unknown origin)	B	9.3	pIC50	0.5	nM	IC50	J Med Chem (2016) 59: 8667-8684 [PMID:27171036]
GtoPdb	-	-	9.52	pIC50	0.3	nM	IC50	Bioorg Med Chem (2007) 15: 5837-44 [PMID:17601739]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit beta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit beta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3145] [GtoPdb: 2154] [UniProtKB: P42338]
GtoPdb	-	-	5.89	pIC50	1300	nM	IC50	Cell (2006) 125: 733-47 [PMID:16647110]
GtoPdb	-	-	6.07	pIC50	850	nM	IC50	Bioorg Med Chem (2007) 15: 5837-44 [PMID:17601739]
ChEMBL	Inhibition of human recombinant p110beta	B	6.47	pIC50	340	nM	IC50	Bioorg Med Chem (2007) 15: 7677-7687 [PMID:17869522]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit delta/Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit delta isoform in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3130] [GtoPdb: 2155] [UniProtKB: O00329]
ChEMBL	Inhibition of human recombinant p110delta	B	6.04	pIC50	910	nM	IC50	Bioorg Med Chem (2007) 15: 7677-7687 [PMID:17869522]
GtoPdb	-	-	6.29	pIC50	510	nM	IC50	Cell (2006) 125: 733-47 [PMID:16647110]
fms related receptor tyrosine kinase 3/Receptor-type tyrosine-protein kinase FLT3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1974] [GtoPdb: 1807] [UniProtKB: P36888]
ChEMBL	Inhibition of FLT3 (unknown origin) using biotin-Glu-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2 as substrate after 90 mins by luminescence assay	B	8.29	pIC50	5.15	nM	IC50	Bioorg Med Chem (2015) 23: 6280-6296 [PMID:26349627]
phosphatidylinositol-4,5-bisphosphate 3-kinase catalytic subunit gamma in Human [GtoPdb: 2156] [UniProtKB: P48736]
GtoPdb	-	-	7.12	pIC50	76	nM	IC50	Cell (2006) 125: 733-47 [PMID:16647110]
GtoPdb	-	-	7.4	pIC50	40	nM	IC50	Bioorg Med Chem (2007) 15: 5837-44 [PMID:17601739]
protein kinase, DNA-activated, catalytic subunit in Human [GtoPdb: 2800] [UniProtKB: P78527]
GtoPdb	-	-	8.7	pIC50	2	nM	IC50	Cell (2006) 125: 733-47 [PMID:16647110]

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]