leucettine L41 [Ligand Id: 8167] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL1802358 |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| phosphoinositide kinase, FYVE-type zinc finger containing/1-phosphatidylinositol 3-phosphate 5-kinase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176842] [GtoPdb: 2857] [UniProtKB: Q9Z1T6] | ||||||||
| ChEMBL | Binding affinity to phosphatidylinositol-3-phosphate 5-kinase type 3 in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | B | 5.22 | pKd | 6010 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| CB1 receptor/Cannabinoid CB1 receptor in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL218] [GtoPdb: 56] [UniProtKB: P21554] | ||||||||
| ChEMBL | Antagonist activity at CP-55940-activated CB1 receptor (unknown origin) by beta-arrestin assay | F | 6.5 | pIC50 | 314 | nM | IC50 | J Med Chem (2022) 65: 1396-1417 [PMID:34928152] |
| casein kinase 1 epsilon/Casein kinase I 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 | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| 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 human recombinant CK2 using RRREDEESDDEE as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| casein kinase 2, alpha 1 polypeptide subunit/Casein kinase II alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3537] [GtoPdb: 1549] [UniProtKB: Q60737] | ||||||||
| ChEMBL | Binding affinity to CSNK2A1 in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | B | 6.49 | pKd | 326 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| casein kinase 2, alpha prime polypeptide subunit/Casein kinase II alpha (prime) in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5326] [GtoPdb: 1550] [UniProtKB: O54833] | ||||||||
| ChEMBL | Binding affinity to CSNK2A2 in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | B | 6.24 | pKd | 574 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| casein kinase 2, beta polypeptide subunit/Casein kinase II beta in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4095] [GtoPdb: 1551] [UniProtKB: P67871] | ||||||||
| ChEMBL | Binding affinity to CSNK2N in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | B | 6.42 | pKd | 382 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| cyclin dependent kinase 2/CDK2/Cyclin A2 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL3038469] [GtoPdb: 1973] [UniProtKB: P20248, P24941] | ||||||||
| ChEMBL | Inhibition of human recombinant CDK2/cyclin A using [gamma-33P]-ATP after 30 mins by scintillation counting | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2013) 62: 728-737 [PMID:23454515] |
| cyclin dependent kinase 9/CDK9/cyclin T1 in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111389] [GtoPdb: 1981] [UniProtKB: O60563, P50750] | ||||||||
| ChEMBL | Inhibition of human recombinant CDK9/cyclin T expressed in insect cell using YSPTSPSYSPTSPSYSPTSPSKKKK as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 4.74 | pIC50 | 18000 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of human recombinant CDK9/cyclin T using YSPTSPSYSPTSPSYSPTSPSKKKK as substrate | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2013) 62: 728-737 [PMID:23454515] |
| cyclin dependent kinase 2/Cyclin-dependent kinase 2/cyclin A in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2094128] [GtoPdb: 1973] [UniProtKB: P20248, P24941, P78396] | ||||||||
| ChEMBL | Inhibition of CDK2/cyclin A using [gamma33P]ATP after 30 mins by scintillation counting | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| cyclin dependent kinase 5/Cyclin-dependent kinase 5 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4036] [GtoPdb: 1977] [UniProtKB: Q00535] | ||||||||
| ChEMBL | Inhibition of human recombinant CDK5 assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| 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 human recombinant CDK5/p25 using histone H1 as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of human recombinant CDK5/p25 using [gamma-33P]-ATP after 30 mins by scintillation counting | B | 5 | pIC50 | >10000 | nM | IC50 | Eur J Med Chem (2013) 62: 728-737 [PMID:23454515] |
| 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 | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of human recombinant CDK5/p25 | B | 6.39 | pIC50 | 410 | nM | IC50 | J Med Chem (2011) 54: 4172-4186 [PMID:21615147] |
| cyclin dependent kinase 7/Cyclin-dependent kinase 7/ cyclin H in Human (target type: PROTEIN COMPLEX) [ChEMBL: CHEMBL2111288] [GtoPdb: 1979] [UniProtKB: P50613, P51946] | ||||||||
| ChEMBL | Inhibition of human recombinant CDK7/cyclin H expressed in insect cell using YSPTSPSYSPTSPSYSPTSPSKKKK as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| 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 CLK1 | B | 7.12 | pKd | 75 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Binding affinity to human CLK1 assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay | B | 8.07 | pKd | 8.51 | nM | Kd | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Binding affinity to human CLK1 assessed as dissociation constant | B | 8.07 | pKd | 8.51 | nM | Kd | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| 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 | 7.11 | pIC50 | 77.2 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of CLK1 (unknown origin) | B | 7.15 | pIC50 | 71 | nM | IC50 | J Med Chem (2017) 60: 2052-2070 [PMID:28206758] |
| ChEMBL | Inhibition of human CLK1 | B | 7.15 | pIC50 | 71 | nM | IC50 | J Med Chem (2021) 64: 13191-13211 [PMID:34519506] |
| ChEMBL | Inhibition of human CLK1 assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis | B | 7.25 | pIC50 | 56.4 | nM | IC50 | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| 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 | 7.29 | pIC50 | 51.5 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of N-terminal GST/His6-fused human full length CLK1 (1 to 484 residues) expressed in Sf9 cells assessed as inhibition of autophosphorylation using [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2023) 66: 10694-10714 [PMID:37487467] |
| CDC like kinase 1/Dual specificity protein kinase CLK1 in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1075280] [GtoPdb: 1990] [UniProtKB: P22518] | ||||||||
| ChEMBL | Inhibition of mouse recombinant GST-tagged CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 7.15 | pIC50 | 71 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of mouse recombinant CLK1 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | B | 7.46 | pIC50 | 35 | nM | IC50 | Eur J Med Chem (2013) 62: 728-737 [PMID:23454515] |
| ChEMBL | Inhibition of GST-fused mouse recombinant CLK1 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2022) 65: 1396-1417 [PMID:34928152] |
| ChEMBL | Inhibition of mouse recombinant GST-tagged CLK1 using GRSRSRSRSRSR as substrate | B | 7.82 | pIC50 | 15 | nM | IC50 | J Med Chem (2011) 54: 4172-4186 [PMID:21615147] |
| GtoPdb | - | - | 10.82 | pIC50 | 0.01 | nM | IC50 | J Med Chem (2011) 54: 4172-86 [PMID:21615147] |
| 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 | B | 6.44 | pKd | 360 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| 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 | 5.72 | pIC50 | 1893 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of human CLK2 | B | 6.14 | pIC50 | 720 | nM | IC50 | J Med Chem (2021) 64: 13191-13211 [PMID:34519506] |
| ChEMBL | Inhibition of human recombinant CLK2 assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis | B | 6.23 | pIC50 | 587 | nM | IC50 | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| ChEMBL | Inhibition of human CLK2 using GSK3(14-27) peptide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2023) 66: 10694-10714 [PMID:37487467] |
| 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 recombinant GST-tagged CLK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 6.14 | pIC50 | 720 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of mouse recombinant CLK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | B | 6.49 | pIC50 | 320 | nM | IC50 | Eur J Med Chem (2013) 62: 728-737 [PMID:23454515] |
| ChEMBL | Inhibition of mouse recombinant GST-fused CLK2 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | B | 6.89 | pIC50 | 130 | nM | IC50 | J Med Chem (2022) 65: 1396-1417 [PMID:34928152] |
| 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 | B | 5.96 | pKd | 1100 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of human CLK3 | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2021) 64: 13191-13211 [PMID:34519506] |
| ChEMBL | Inhibition of human recombinant CLK3 assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis | B | 5.23 | pIC50 | 5840 | nM | IC50 | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| 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 | 5.66 | pIC50 | 2165 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of human full length CLK3 (1 to 490 residues) expressed in Sf9 cells using S6 peptide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2023) 66: 10694-10714 [PMID:37487467] |
| 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 recombinant GST-tagged CLK3 using GRSRSRSRSRSR as substrate | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2011) 54: 4172-4186 [PMID:21615147] |
| ChEMBL | Inhibition of mouse recombinant GST-tagged CLK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of mouse recombinant CLK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | B | 5.52 | pIC50 | 3000 | nM | IC50 | Eur J Med Chem (2013) 62: 728-737 [PMID:23454515] |
| ChEMBL | Inhibition of GST-fused mouse recombinant CLK3 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2022) 65: 1396-1417 [PMID:34928152] |
| GtoPdb | - | - | 8.35 | pIC50 | 4.5 | nM | IC50 | J Med Chem (2011) 54: 4172-86 [PMID:21615147] |
| 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 | B | 7.15 | pKd | 70 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of human CLK4 | B | 7.19 | pIC50 | 64 | nM | IC50 | J Med Chem (2021) 64: 13191-13211 [PMID:34519506] |
| ChEMBL | Inhibition of human CLK4 using MBP and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2023) 66: 10694-10714 [PMID:37487467] |
| 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 | 7.67 | pIC50 | 21.5 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of human CLK4 assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| 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 recombinant GST-tagged CLK4 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 7.19 | pIC50 | 64 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of mouse recombinant CLK4 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | B | 7.51 | pIC50 | 31 | nM | IC50 | Eur J Med Chem (2013) 62: 728-737 [PMID:23454515] |
| ChEMBL | Inhibition of GST-fused mouse recombinant CLK4 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | B | 7.64 | pIC50 | 23 | nM | IC50 | J Med Chem (2022) 65: 1396-1417 [PMID:34928152] |
| dual specificity tyrosine phosphorylation regulated kinase 1A/Dual specificity tyrosine-phosphorylation-regulated kinase 1A in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5508] [GtoPdb: 2009] [UniProtKB: Q63470] | ||||||||
| ChEMBL | Inhibition of rat recombinant GST-tagged DYRK1A using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation counting | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2011) 54: 4172-4186 [PMID:21615147] |
| ChEMBL | Inhibition of rat recombinant C-terminal truncated GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 7.4 | pIC50 | 40 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of rat DYRK1A isolated from brain using KKISGRLSPIMTEQ as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 8 | pIC50 | 10 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| GtoPdb | - | - | 10.4 | pIC50 | 0.04 | nM | IC50 | J Med Chem (2011) 54: 4172-86 [PMID:21615147] |
| 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 | B | 8.11 | pKd | 7.8 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Binding affinity to human DYRK1A assessed as equilibrium dissociation constant measured upto 240 min by TR-FRET assay | B | 8.14 | pKd | 7.24 | nM | Kd | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Binding affinity to human DYRK1A assessed as dissociation constant | B | 8.14 | pKd | 7.24 | nM | Kd | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| ChEMBL | Inhibition of human recombinant full length GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 7.22 | pIC50 | 60 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of DYRK1A (unknown origin) | B | 7.26 | pIC50 | 55 | nM | IC50 | J Med Chem (2017) 60: 2052-2070 [PMID:28206758] |
| ChEMBL | Inhibition of human recombinant C-terminal truncated GST-tagged DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 7.26 | pIC50 | 55 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of human DYRK1A assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis | B | 7.38 | pIC50 | 41.6 | nM | IC50 | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| ChEMBL | Inhibition of DYRK1A (unknown origin) | B | 7.4 | pIC50 | 40 | nM | IC50 | Eur J Med Chem (2018) 158: 559-592 [PMID:30243157] |
| 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 | 7.61 | pIC50 | 24.6 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of human DYRK1A using RBERCHKtide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2023) 66: 10694-10714 [PMID:37487467] |
| ChEMBL | Inhibition of GST-fused human recombinant DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | B | 7.62 | pIC50 | 24 | nM | IC50 | J Med Chem (2022) 65: 1396-1417 [PMID:34928152] |
| ChEMBL | Inhibition of human recombinant DYRK1A expressed in Escherichia coli using GRSRSRSRSRSR as substrate | B | 7.68 | pIC50 | 21 | nM | IC50 | Eur J Med Chem (2013) 62: 728-737 [PMID:23454515] |
| 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 | 7.74 | pIC50 | 18.1 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of human DYRK1A using [33P]-ATP incubated for 120 mins | B | 8.12 | pIC50 | 7.6 | nM | IC50 | J Med Chem (2016) 59: 10315-10321 [PMID:27766861] |
| dual specificity tyrosine phosphorylation regulated kinase 1A/Dual-specificity tyrosine-phosphorylation regulated kinase 1A in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4750] [GtoPdb: 2009] [UniProtKB: Q61214] | ||||||||
| ChEMBL | Binding affinity to DYRK1A in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | B | 7.19 | pKd | 65 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| dual specificity tyrosine phosphorylation regulated kinase 1A in Rat [GtoPdb: 2009] [UniProtKB: Q63470] | ||||||||
| GtoPdb | - | - | 10.4 | pIC50 | 0.04 | nM | IC50 | J Med Chem (2011) 54: 4172-86 [PMID:21615147] |
| 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 | B | 6.85 | pKd | 140 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| 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 | 6.87 | pIC50 | 135.8 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of human recombinant DYRK1B expressed in Escherichia coli using GRSRSRSRSRSR as substrate | B | 7.11 | pIC50 | 77 | nM | IC50 | Eur J Med Chem (2013) 62: 728-737 [PMID:23454515] |
| ChEMBL | Inhibition of human DYRK1B assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis | B | 7.12 | pIC50 | 76.6 | nM | IC50 | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| ChEMBL | Inhibition of GST-fused human recombinant DYRK1B expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | B | 7.21 | pIC50 | 62 | nM | IC50 | J Med Chem (2022) 65: 1396-1417 [PMID:34928152] |
| ChEMBL | Inhibition of human DYRK1B using RBERCHKtide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay | B | 7.21 | pIC50 | 62 | nM | IC50 | J Med Chem (2023) 66: 10694-10714 [PMID:37487467] |
| 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 | 7.26 | pIC50 | 54.4 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of human recombinant GST-tagged DYRK1B expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 7.36 | pIC50 | 44 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of human DYRK1B using [33P]-ATP incubated for 120 mins | B | 7.43 | pIC50 | 37 | nM | IC50 | J Med Chem (2016) 59: 10315-10321 [PMID:27766861] |
| 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 | Binding affinity to DYRK2 | B | 6.35 | pKd | 450 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| 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 | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of human recombinant DYRK2 assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis | B | 6.2 | pIC50 | 630.5 | nM | IC50 | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| ChEMBL | Inhibition of human recombinant DYRK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | B | 6.66 | pIC50 | 220 | nM | IC50 | Eur J Med Chem (2013) 62: 728-737 [PMID:23454515] |
| ChEMBL | Inhibition of human recombinant GST-tagged DYRK2 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 7.14 | pIC50 | 73 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of human recombinant GST-tagged DYRK2 using KKISGRLSPIMTEQ as substrate and [gamma32]-ATP after 30 mins by scintillation counting | B | 7.46 | pIC50 | 35 | nM | IC50 | J Med Chem (2011) 54: 4172-4186 [PMID:21615147] |
| ChEMBL | Inhibition of GST-fused human recombinant DYRK2 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2022) 65: 1396-1417 [PMID:34928152] |
| ChEMBL | Inhibition of human DYRK2 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay | B | 7.85 | pIC50 | 14 | nM | IC50 | J Med Chem (2023) 66: 10694-10714 [PMID:37487467] |
| GtoPdb | - | - | 9.46 | pIC50 | 0.35 | nM | IC50 | J Med Chem (2011) 54: 4172-86 [PMID:21615147] |
| 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 | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of human recombinant DYRK3 assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis | B | 5.73 | pIC50 | 1847 | nM | IC50 | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| ChEMBL | Inhibition of human recombinant DYRK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate | B | 6.15 | pIC50 | 700 | nM | IC50 | Eur J Med Chem (2013) 62: 728-737 [PMID:23454515] |
| ChEMBL | Inhibition of human recombinant GST-tagged DYRK3 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 6.49 | pIC50 | 320 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of GST-fused human recombinant DYRK3 expressed in Escherichia coli using GRSRSRSRSRSR peptide as substrate incubated for 30 mins in presence of ATP by scintillation counting method | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2022) 65: 1396-1417 [PMID:34928152] |
| ChEMBL | Inhibition of human DYRK3 using RBERIRStide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay | B | 6.64 | pIC50 | 230 | nM | IC50 | J Med Chem (2023) 66: 10694-10714 [PMID:37487467] |
| 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 | 6.09 | pIC50 | 817.2 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| GtoPdb | - | - | 6.28 | pIC50 | 520 | nM | IC50 | J Med Chem (2012) 55: 9312-30 [PMID:22998443] |
| ChEMBL | Inhibition of human recombinant GST-tagged DYRK4 expressed in Escherichia coli using GRSRSRSRSRSR as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 6.28 | pIC50 | 520 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of human recombinant DYRK4 assessed as incorporation of 33Pi using [gamma-33P]-ATP measured after 60 mins by microplate scintillation counting based radiometric analysis | B | 6.29 | pIC50 | 507.4 | nM | IC50 | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2850] [GtoPdb: 2029] [UniProtKB: P49840] | ||||||||
| ChEMBL | Binding affinity to GSK3A | B | 6.26 | pKd | 550 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| ChEMBL | Inhibition of human recombinant GSK3alpha expressed in insect cells using YRRAAVPPSPSLSRHSSPHQ-phosphoS-EDEEE as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 6.68 | pIC50 | 210 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| glycogen synthase kinase 3 alpha/Glycogen synthase kinase-3 alpha in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176843] [GtoPdb: 2029] [UniProtKB: Q2NL51] | ||||||||
| ChEMBL | Binding affinity to GSK3A in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | B | 5.48 | pKd | 3274 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| 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 | 6.25 | pKd | 561.03 | nM | Kd | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Binding affinity to human GSK3beta assessed as dissociation constant | B | 6.25 | pKd | 561 | nM | Kd | J Med Chem (2023) 66: 15648-15670 [PMID:38051674] |
| 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 | 5 | pIC50 | >10000 | nM | IC50 | J Med Chem (2023) 66: 4106-4130 [PMID:36876904] |
| ChEMBL | Inhibition of N-terminal GST/His6-fused human full length GSK-3-beta (1 to 420 residues) expressed in Sf9 cells using RBERCHKtide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay | B | 6.22 | pIC50 | 600 | nM | IC50 | J Med Chem (2023) 66: 10694-10714 [PMID:37487467] |
| ChEMBL | Inhibition of human recombinant GSK3beta expressed in insect cells using YRRAAVPPSPSLSRHSSPHQ-phosphoS-EDEEE as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 6.42 | pIC50 | 380 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| homeodomain interacting protein kinase 1/Homeodomain-interacting protein kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5427] [GtoPdb: 2033] [UniProtKB: Q86Z02] | ||||||||
| ChEMBL | Binding affinity to HIPK1 | B | 6.49 | pKd | 320 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| homeodomain interacting protein kinase 3/Homeodomain-interacting protein kinase 3 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4577] [GtoPdb: 2035] [UniProtKB: Q9H422] | ||||||||
| ChEMBL | Binding affinity to HIPK3 | B | 6.64 | pKd | 230 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| interleukin 1 receptor associated kinase 1/Interleukin-1 receptor-associated kinase 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3357] [GtoPdb: 2042] [UniProtKB: P51617] | ||||||||
| ChEMBL | Binding affinity to IRAK1 | B | 6.03 | pKd | 930 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| mitogen-activated protein kinase 1/Mitogen-activated protein kinase 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5233] [GtoPdb: 1495] [UniProtKB: P63086] | ||||||||
| ChEMBL | Inhibition of rat recombinant ERK2 using Ets1 as substrate and [gamma33P]ATP as substrate after 30 mins by scintillation counting | B | 4.52 | pIC50 | >30000 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| Protein VAC14 homolog in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176841] [UniProtKB: Q80WQ2] | ||||||||
| ChEMBL | Binding affinity to VAC14 in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | B | 4.82 | pKd | 15265 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| 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 | Inhibition of human recombinant Pim1 | B | 5.39 | pIC50 | 4100 | nM | IC50 | J Med Chem (2011) 54: 4172-4186 [PMID:21615147] |
| ChEMBL | Inhibition of human recombinant Pim1 expressed in Escherichia coli using histone H1 as substrate incubated for 30 mins in presence of ATP by scintillation counting method | B | 5.92 | pIC50 | 1200 | nM | IC50 | J Med Chem (2022) 65: 1396-1417 [PMID:34928152] |
| ChEMBL | Inhibition of human recombinant PIM1 expressed in Escherichia coli using histone H1 as substrate and [gamma33P]ATP after 30 mins by scintillation counting | B | 6.06 | pIC50 | 880 | nM | IC50 | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| GtoPdb | - | - | 8.39 | pIC50 | 4.1 | nM | IC50 | J Med Chem (2011) 54: 4172-86 [PMID:21615147] |
| TAO kinase 1/Serine/threonine-protein kinase TAO1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5261] [GtoPdb: 2233] [UniProtKB: Q7L7X3] | ||||||||
| ChEMBL | Binding affinity to TAOK1 | B | 5.77 | pKd | 1700 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
| STE20 like kinase/STE20-like serine/threonine-protein kinase in Mouse (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2176844] [GtoPdb: 2200] [UniProtKB: O54988] | ||||||||
| ChEMBL | Binding affinity to SLK1 in mouse brain homogenate after 3 hrs by competition affinity chromatographic analysis | B | 7.68 | pKd | 21 | nM | Kd | J Med Chem (2012) 55: 9312-9330 [PMID:22998443] |
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]
