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Assay Detail

CHEMBL5363962

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Binding
Inhibition of human DYRK4 using RBERCHKtide and [gamma33P]ATP as substrate incubated for 60 mins by radiometric 33PanQinase assay
ChEMBL ↗
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

Dual specificity tyrosine-phosphorylation-regulated kinase 4 (CHEMBL1075115) ↗
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 6.04 7.48

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5400230 — — 1 7.48
CHEMBL5438158 — — 1 7.33
CHEMBL5405059 — — 1 7.32
CHEMBL5420645 — — 1 7.10
CHEMBL5408907 — — 1 7.09
CHEMBL5438293 — — 1 6.97
CHEMBL5091238 — — 1 6.93
CHEMBL5440139 — — 1 6.92
CHEMBL5417207 — — 1 6.90
CHEMBL5421442 — — 1 6.90
CHEMBL5414514 — — 1 6.86
CHEMBL5441121 — — 1 6.86
CHEMBL5396991 — — 1 6.84
CHEMBL5427842 — — 1 6.84
CHEMBL5422486 — — 1 6.84
CHEMBL5414635 — — 1 6.81
CHEMBL5396550 — — 1 6.76
CHEMBL5406081 — — 1 6.76
CHEMBL5398161 — — 1 6.75
CHEMBL5428132 — — 1 6.74
CHEMBL5404416 — — 1 6.66
CHEMBL5412900 — — 1 6.66
CHEMBL5428629 — — 1 6.64
CHEMBL5409574 — — 1 6.63
CHEMBL5426285 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- 1.0 1 6.61
CHEMBL5397343 — — 1 6.61
CHEMBL5405233 — — 1 6.61
CHEMBL5418020 — — 1 6.59
CHEMBL5412998 — — 1 6.58
CHEMBL5422654 — — 1 6.58

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5400230 — IC50 = 33.0 nM 7.48
CHEMBL5438158 — IC50 = 47.0 nM 7.33
CHEMBL5405059 — IC50 = 48.0 nM 7.32
CHEMBL5420645 — IC50 = 80.0 nM 7.10
CHEMBL5408907 — IC50 = 82.0 nM 7.09
CHEMBL5438293 — IC50 = 108.0 nM 6.97
CHEMBL5091238 — IC50 = 117.0 nM 6.93
CHEMBL5440139 — IC50 = 121.0 nM 6.92
CHEMBL5417207 — IC50 = 127.0 nM 6.90
CHEMBL5421442 — IC50 = 127.0 nM 6.90
CHEMBL5414514 — IC50 = 137.0 nM 6.86
CHEMBL5441121 — IC50 = 137.0 nM 6.86
CHEMBL5422486 — IC50 = 146.0 nM 6.84
CHEMBL5396991 — IC50 = 143.0 nM 6.84
CHEMBL5427842 — IC50 = 146.0 nM 6.84
CHEMBL5414635 — IC50 = 155.0 nM 6.81
CHEMBL5396550 — IC50 = 174.0 nM 6.76
CHEMBL5406081 — IC50 = 174.0 nM 6.76
CHEMBL5398161 — IC50 = 180.0 nM 6.75
CHEMBL5428132 — IC50 = 181.0 nM 6.74
CHEMBL5412900 — IC50 = 221.0 nM 6.66
CHEMBL5404416 — IC50 = 218.0 nM 6.66
CHEMBL5428629 — IC50 = 227.0 nM 6.64
CHEMBL5409574 — IC50 = 233.0 nM 6.63
CHEMBL5405233 — IC50 = 246.0 nM 6.61
CHEMBL5426285 5-(6-BENZOTHIAZOLYLMETHYLENE)-3,5-DIHYDRO-2-(((1S)-1-(METHOXYMETHYL)-3-METHYLBUTYL)AMINO)-4H-IMIDAZOL-4-ONE, (5Z)- IC50 = 248.0 nM 6.61
CHEMBL5397343 — IC50 = 244.0 nM 6.61
CHEMBL5418020 — IC50 = 257.0 nM 6.59
CHEMBL5412998 — IC50 = 260.0 nM 6.58
CHEMBL5422654 — IC50 = 263.0 nM 6.58
CHEMBL5418722 — IC50 = 270.0 nM 6.57
CHEMBL5439276 — IC50 = 274.0 nM 6.56
CHEMBL5417147 — IC50 = 284.0 nM 6.55
CHEMBL5398512 — IC50 = 288.0 nM 6.54
CHEMBL5407057 — IC50 = 294.0 nM 6.53
CHEMBL5436133 — IC50 = 319.0 nM 6.50
CHEMBL5438728 — IC50 = 317.0 nM 6.50
CHEMBL5427398 — IC50 = 326.0 nM 6.49
CHEMBL5428651 — IC50 = 321.0 nM 6.49
CHEMBL5411888 — IC50 = 321.0 nM 6.49
CHEMBL5439392 — IC50 = 335.0 nM 6.47
CHEMBL5439952 — IC50 = 357.0 nM 6.45
CHEMBL5406461 — IC50 = 374.0 nM 6.43
CHEMBL5424272 — IC50 = 383.0 nM 6.42
CHEMBL5438412 — IC50 = 385.0 nM 6.42
CHEMBL5415462 — IC50 = 410.0 nM 6.39
CHEMBL5412565 — IC50 = 411.0 nM 6.39
CHEMBL5440511 — IC50 = 403.0 nM 6.39
CHEMBL5413743 — IC50 = 439.0 nM 6.36
CHEMBL5434955 — IC50 = 445.0 nM 6.35