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Assay Detail

CHEMBL5363952

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

Binding
Inhibition of human CK1 epsilon using casein and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay
228
Total Activities
228
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

Casein kinase I isoform epsilon (CHEMBL4937)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Leucettinibs, a Class of DYRK/CLK Kinase Inhibitors Inspired by the Marine Sponge Natural Product Leucettamine B.
Deau E, Lindberg MF, Miege F, Roche D, George N, George P, Krämer A, Knapp S, Meijer L.
J Med Chem (2023) 66 : 10694 -10714
PubMed 37487467 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 228 5.62 7.21

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5422486 1 7.21
CHEMBL5396550 1 6.38
CHEMBL5438158 1 6.21
CHEMBL5405059 1 5.96
CHEMBL5422654 1 5.92
CHEMBL5412565 1 5.83
CHEMBL5417147 1 5.75
CHEMBL5438728 1 5.71
CHEMBL5418722 1 5.64
CHEMBL5400230 1 5.61
CHEMBL5406081 1 5.56
CHEMBL5397343 1 5.46
CHEMBL5441121 1 5.39
CHEMBL5404544 1 5.33
CHEMBL5421442 1 5.30
CHEMBL5409574 1 5.24
CHEMBL5439276 1 5.20
CHEMBL5436133 1 5.16
CHEMBL5411888 1 5.07
CHEMBL5430357 1 5.01
CHEMBL5428651 1 5.01
CHEMBL5395680 1 -
CHEMBL5414361 1 -
CHEMBL5410738 1 -
CHEMBL5435718 1 -
CHEMBL5394477 1 -
CHEMBL5419006 1 -
CHEMBL5437222 1 -
CHEMBL5394278 1 -
CHEMBL5412478 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5422486 IC50 = 62.0 nM 7.21
CHEMBL5396550 IC50 = 420.0 nM 6.38
CHEMBL5438158 IC50 = 612.0 nM 6.21
CHEMBL5405059 IC50 = 1100.0 nM 5.96
CHEMBL5422654 IC50 = 1200.0 nM 5.92
CHEMBL5412565 IC50 = 1476.0 nM 5.83
CHEMBL5417147 IC50 = 1760.0 nM 5.75
CHEMBL5438728 IC50 = 1948.0 nM 5.71
CHEMBL5418722 IC50 = 2267.0 nM 5.64
CHEMBL5400230 IC50 = 2434.0 nM 5.61
CHEMBL5406081 IC50 = 2746.0 nM 5.56
CHEMBL5397343 IC50 = 3427.0 nM 5.46
CHEMBL5441121 IC50 = 4048.0 nM 5.39
CHEMBL5404544 IC50 = 4694.0 nM 5.33
CHEMBL5421442 IC50 = 5000.0 nM 5.30
CHEMBL5409574 IC50 = 5807.0 nM 5.24
CHEMBL5439276 IC50 = 6345.0 nM 5.20
CHEMBL5436133 IC50 = 6926.0 nM 5.16
CHEMBL5411888 IC50 = 8460.0 nM 5.07
CHEMBL5430357 IC50 = 9752.0 nM 5.01
CHEMBL5428651 IC50 = 9800.0 nM 5.01
CHEMBL5406461 IC50 > 10000.0 nM -
CHEMBL5411626 IC50 > 10000.0 nM -
CHEMBL5401217 IC50 > 10000.0 nM -
CHEMBL5439392 IC50 > 10000.0 nM -
CHEMBL5414635 IC50 > 10000.0 nM -
CHEMBL5413503 IC50 > 10000.0 nM -
CHEMBL5430988 IC50 > 10000.0 nM -
CHEMBL5431414 IC50 > 10000.0 nM -
CHEMBL5430415 IC50 > 10000.0 nM -
CHEMBL5423063 IC50 > 10000.0 nM -
CHEMBL5417890 IC50 > 10000.0 nM -
CHEMBL5412101 IC50 > 10000.0 nM -
CHEMBL5435495 IC50 > 10000.0 nM -
CHEMBL5398161 IC50 > 10000.0 nM -
CHEMBL5424074 IC50 > 10000.0 nM -
CHEMBL5421200 IC50 > 10000.0 nM -
CHEMBL5416947 IC50 > 10000.0 nM -
CHEMBL5434955 IC50 > 10000.0 nM -
CHEMBL5404644 IC50 > 10000.0 nM -
CHEMBL5422100 IC50 > 10000.0 nM -
CHEMBL5438412 IC50 > 10000.0 nM -
CHEMBL5426735 IC50 > 10000.0 nM -
CHEMBL5428794 IC50 > 10000.0 nM -
CHEMBL5438852 IC50 > 10000.0 nM -
CHEMBL5406568 IC50 > 10000.0 nM -
CHEMBL5428107 IC50 > 10000.0 nM -
CHEMBL5395707 IC50 > 10000.0 nM -
CHEMBL5405680 IC50 > 10000.0 nM -
CHEMBL5399810 IC50 > 10000.0 nM -