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Assay Detail

CHEMBL4041965

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Binding
Inhibition of GST tagged recombinant human DYRK2 expressed in Escherichia coli using using woodtide as substrate after 30 mins by [gamma-33P]ATP based scintillation counting analysis
ChEMBL ↗
60
Total Activities
60
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 2 (CHEMBL4376) ↗
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Exploration of the imidazo[1,2-b]pyridazine scaffold as a protein kinase inhibitor.
Bendjeddou LZ, Loaëc N, Villiers B, Prina E, Späth GF, Galons H, Meijer L, Oumata N.
Eur J Med Chem (2017) 125 : 696 -709
PubMed 27721154 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 60 6.06 7.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4102871 — — 1 7.40
CHEMBL4061526 — — 1 7.37
CHEMBL4071322 — — 1 7.32
CHEMBL4105084 — — 1 7.30
CHEMBL4093104 — — 1 7.20
CHEMBL4070189 — — 1 7.09
CHEMBL4074499 — — 1 6.96
CHEMBL4092673 — — 1 6.92
CHEMBL4089652 — — 1 6.92
CHEMBL4072506 — — 1 6.77
CHEMBL4086402 — — 1 6.75
CHEMBL4074132 — — 1 6.72
CHEMBL4062820 — — 1 6.68
CHEMBL4079347 — — 1 6.50
CHEMBL4090770 — — 1 6.42
CHEMBL4084919 — — 1 6.42
CHEMBL4065432 — — 1 6.41
CHEMBL4084364 — — 1 6.40
CHEMBL4090223 — — 1 6.36
CHEMBL4071013 — — 1 6.36
CHEMBL4070065 — — 1 6.32
CHEMBL4070227 — — 1 6.30
CHEMBL4100956 — — 1 6.22
CHEMBL4097368 — — 1 6.22
CHEMBL4091942 — — 1 6.21
CHEMBL4077159 — — 1 6.14
CHEMBL4104296 — — 1 6.11
CHEMBL4076448 — — 1 6.09
CHEMBL4082981 — — 1 5.92
CHEMBL4067420 — — 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4102871 — IC50 = 40.0 nM 7.40
CHEMBL4061526 — IC50 = 43.0 nM 7.37
CHEMBL4071322 — IC50 = 48.0 nM 7.32
CHEMBL4105084 — IC50 = 50.0 nM 7.30
CHEMBL4093104 — IC50 = 63.0 nM 7.20
CHEMBL4070189 — IC50 = 82.0 nM 7.09
CHEMBL4074499 — IC50 = 110.0 nM 6.96
CHEMBL4092673 — IC50 = 120.0 nM 6.92
CHEMBL4089652 — IC50 = 120.0 nM 6.92
CHEMBL4072506 — IC50 = 170.0 nM 6.77
CHEMBL4086402 — IC50 = 180.0 nM 6.75
CHEMBL4074132 — IC50 = 190.0 nM 6.72
CHEMBL4062820 — IC50 = 210.0 nM 6.68
CHEMBL4079347 — IC50 = 320.0 nM 6.50
CHEMBL4084919 — IC50 = 380.0 nM 6.42
CHEMBL4090770 — IC50 = 380.0 nM 6.42
CHEMBL4065432 — IC50 = 390.0 nM 6.41
CHEMBL4084364 — IC50 = 400.0 nM 6.40
CHEMBL4090223 — IC50 = 440.0 nM 6.36
CHEMBL4071013 — IC50 = 440.0 nM 6.36
CHEMBL4070065 — IC50 = 480.0 nM 6.32
CHEMBL4070227 — IC50 = 500.0 nM 6.30
CHEMBL4100956 — IC50 = 600.0 nM 6.22
CHEMBL4097368 — IC50 = 600.0 nM 6.22
CHEMBL4091942 — IC50 = 610.0 nM 6.21
CHEMBL4077159 — IC50 = 730.0 nM 6.14
CHEMBL4104296 — IC50 = 780.0 nM 6.11
CHEMBL4076448 — IC50 = 820.0 nM 6.09
CHEMBL4082981 — IC50 = 1200.0 nM 5.92
CHEMBL4067420 — IC50 = 1200.0 nM 5.92
CHEMBL4098107 — IC50 = 1200.0 nM 5.92
CHEMBL4061394 — IC50 = 1300.0 nM 5.89
CHEMBL4077125 — IC50 = 1400.0 nM 5.85
CHEMBL4092117 — IC50 = 1600.0 nM 5.80
CHEMBL4075509 — IC50 = 1600.0 nM 5.80
CHEMBL4069158 — IC50 = 1800.0 nM 5.75
CHEMBL4088717 — IC50 = 1900.0 nM 5.72
CHEMBL4071413 — IC50 = 2500.0 nM 5.60
CHEMBL4063254 — IC50 = 2500.0 nM 5.60
CHEMBL4081668 — IC50 = 3000.0 nM 5.52
CHEMBL4093231 — IC50 = 3100.0 nM 5.51
CHEMBL4064988 — IC50 = 3200.0 nM 5.50
CHEMBL4079343 — IC50 = 3900.0 nM 5.41
CHEMBL4098237 — IC50 = 4500.0 nM 5.35
CHEMBL4099677 — IC50 = 6300.0 nM 5.20
CHEMBL4089542 — IC50 = 7000.0 nM 5.16
CHEMBL4097256 — IC50 = 7100.0 nM 5.15
CHEMBL4076663 — IC50 = 7200.0 nM 5.14
CHEMBL4075820 — IC50 = 8200.0 nM 5.09
CHEMBL4085467 — IC50 = 8600.0 nM 5.07