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Assay Detail

CHEMBL4810626

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Displacement of Kinase tracer 236 from biotinylated DYRK1A (unknown origin) expressed in Escherichia coli BL21 (DE3) incubated for 1.5 hrs by TR-FRET assay
ChEMBL ↗
65
Total Activities
65
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL2292) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors.
Henderson SH, Sorrell F, Bennett J, Fedorov O, Hanley MT, Godoi PH, Ruela de Sousa R, Robinson S, Ashall-Kelly A, Hopkins Navratilova I, Walter DS, Elkins JM, Ward SE.
J Med Chem (2021) 64 : 11709 -11728
PubMed 34342227 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 65 6.18 7.24

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4861396 — — 1 7.24
CHEMBL4852944 — — 1 7.18
CHEMBL4876980 — — 1 7.14
CHEMBL4848254 — — 1 7.12
CHEMBL4637319 — — 1 7.10
CHEMBL4845809 — — 1 7.10
CHEMBL4852650 — — 1 7.00
CHEMBL4859912 — — 1 6.96
CHEMBL4853444 — — 1 6.94
CHEMBL4851717 — — 1 6.94
CHEMBL4848696 — — 1 6.94
CHEMBL4852953 — — 1 6.87
CHEMBL4877372 — — 1 6.87
CHEMBL4874923 — — 1 6.86
CHEMBL4870121 — — 1 6.83
CHEMBL4872408 — — 1 6.80
CHEMBL4849576 — — 1 6.74
CHEMBL4581461 — — 1 6.74
CHEMBL360866 — — 1 6.73
CHEMBL4869255 — — 1 6.73
CHEMBL4867264 — — 1 6.72
CHEMBL4855864 — — 1 6.69
CHEMBL4870189 — — 1 6.66
CHEMBL4858763 — — 1 6.64
CHEMBL4851209 — — 1 6.61
CHEMBL4854898 — — 1 6.57
CHEMBL4874679 — — 1 6.51
CHEMBL4863003 — — 1 6.50
CHEMBL4869135 — — 1 6.48
CHEMBL4866517 — — 1 6.43

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4861396 — IC50 = 57.54 nM 7.24
CHEMBL4852944 — IC50 = 66.07 nM 7.18
CHEMBL4876980 — IC50 = 72.44 nM 7.14
CHEMBL4848254 — IC50 = 75.86 nM 7.12
CHEMBL4637319 — IC50 = 79.43 nM 7.10
CHEMBL4845809 — IC50 = 79.43 nM 7.10
CHEMBL4852650 — IC50 = 100.0 nM 7.00
CHEMBL4859912 — IC50 = 109.65 nM 6.96
CHEMBL4853444 — IC50 = 114.82 nM 6.94
CHEMBL4851717 — IC50 = 114.82 nM 6.94
CHEMBL4848696 — IC50 = 114.82 nM 6.94
CHEMBL4852953 — IC50 = 134.9 nM 6.87
CHEMBL4877372 — IC50 = 134.9 nM 6.87
CHEMBL4874923 — IC50 = 138.04 nM 6.86
CHEMBL4870121 — IC50 = 147.91 nM 6.83
CHEMBL4872408 — IC50 = 158.49 nM 6.80
CHEMBL4849576 — IC50 = 181.97 nM 6.74
CHEMBL4581461 — IC50 = 181.97 nM 6.74
CHEMBL360866 — IC50 = 186.21 nM 6.73
CHEMBL4869255 — IC50 = 186.21 nM 6.73
CHEMBL4867264 — IC50 = 190.55 nM 6.72
CHEMBL4855864 — IC50 = 204.17 nM 6.69
CHEMBL4870189 — IC50 = 218.78 nM 6.66
CHEMBL4858763 — IC50 = 229.09 nM 6.64
CHEMBL4851209 — IC50 = 245.47 nM 6.61
CHEMBL4854898 — IC50 = 269.15 nM 6.57
CHEMBL4874679 — IC50 = 309.03 nM 6.51
CHEMBL4863003 — IC50 = 316.23 nM 6.50
CHEMBL4869135 — IC50 = 331.13 nM 6.48
CHEMBL4866517 — IC50 = 371.54 nM 6.43
CHEMBL4859570 — IC50 = 426.58 nM 6.37
CHEMBL4876257 — IC50 = 457.09 nM 6.34
CHEMBL4859322 — IC50 = 512.86 nM 6.29
CHEMBL4468753 — IC50 = 524.81 nM 6.28
CHEMBL4852454 — IC50 = 676.08 nM 6.17
CHEMBL4874991 — IC50 = 691.83 nM 6.16
CHEMBL4877686 — IC50 = 724.44 nM 6.14
CHEMBL4870311 — IC50 = 758.58 nM 6.12
CHEMBL4875779 — IC50 = 870.96 nM 6.06
CHEMBL4859397 — IC50 = 891.25 nM 6.05
CHEMBL4864447 — IC50 = 912.01 nM 6.04
CHEMBL4863460 — IC50 = 977.24 nM 6.01
CHEMBL4847890 — IC50 = 1023.29 nM 5.99
CHEMBL4873095 — IC50 = 1174.9 nM 5.93
CHEMBL4854454 — IC50 = 1202.26 nM 5.92
CHEMBL4861987 — IC50 = 1230.27 nM 5.91
CHEMBL4876428 — IC50 = 1348.96 nM 5.87
CHEMBL4876669 — IC50 = 1380.38 nM 5.86
CHEMBL4859772 — IC50 = 1584.89 nM 5.80
CHEMBL4866487 — IC50 = 1621.81 nM 5.79