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Assay Detail

CHEMBL4041960

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Binding
Inhibition of GST tagged recombinant mouse CLK2 expressed in Escherichia coli using RS peptide 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 Mus musculus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dual specificity protein kinase CLK2 (CHEMBL1075281) ↗
Type SINGLE PROTEIN
Organism Mus musculus

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 6.12 7.55

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4061526 — — 1 7.55
CHEMBL4102871 — — 1 7.52
CHEMBL4071322 — — 1 7.50
CHEMBL4070189 — — 1 7.33
CHEMBL4065432 — — 1 7.28
CHEMBL4072506 — — 1 7.23
CHEMBL4077159 — — 1 6.89
CHEMBL4074499 — — 1 6.89
CHEMBL4070227 — — 1 6.80
CHEMBL4084919 — — 1 6.80
CHEMBL4092673 — — 1 6.75
CHEMBL4089652 — — 1 6.75
CHEMBL4093104 — — 1 6.66
CHEMBL4105084 — — 1 6.66
CHEMBL4090223 — — 1 6.66
CHEMBL4062820 — — 1 6.42
CHEMBL4086402 — — 1 6.42
CHEMBL4097368 — — 1 6.28
CHEMBL4069158 — — 1 6.27
CHEMBL4074132 — — 1 6.23
CHEMBL4071413 — — 1 6.21
CHEMBL4092047 — — 1 6.16
CHEMBL4079347 — — 1 6.15
CHEMBL4100956 — — 1 6.15
CHEMBL4062683 — — 1 6.09
CHEMBL4091127 — — 1 6.05
CHEMBL4091942 — — 1 6.00
CHEMBL4084364 — — 1 5.96
CHEMBL4098237 — — 1 5.96
CHEMBL4071013 — — 1 5.92

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4061526 — IC50 = 28.0 nM 7.55
CHEMBL4102871 — IC50 = 30.0 nM 7.52
CHEMBL4071322 — IC50 = 32.0 nM 7.50
CHEMBL4070189 — IC50 = 47.0 nM 7.33
CHEMBL4065432 — IC50 = 52.0 nM 7.28
CHEMBL4072506 — IC50 = 59.0 nM 7.23
CHEMBL4077159 — IC50 = 130.0 nM 6.89
CHEMBL4074499 — IC50 = 130.0 nM 6.89
CHEMBL4070227 — IC50 = 160.0 nM 6.80
CHEMBL4084919 — IC50 = 160.0 nM 6.80
CHEMBL4092673 — IC50 = 180.0 nM 6.75
CHEMBL4089652 — IC50 = 180.0 nM 6.75
CHEMBL4090223 — IC50 = 220.0 nM 6.66
CHEMBL4105084 — IC50 = 220.0 nM 6.66
CHEMBL4093104 — IC50 = 220.0 nM 6.66
CHEMBL4062820 — IC50 = 380.0 nM 6.42
CHEMBL4086402 — IC50 = 380.0 nM 6.42
CHEMBL4097368 — IC50 = 520.0 nM 6.28
CHEMBL4069158 — IC50 = 540.0 nM 6.27
CHEMBL4074132 — IC50 = 590.0 nM 6.23
CHEMBL4071413 — IC50 = 610.0 nM 6.21
CHEMBL4092047 — IC50 = 690.0 nM 6.16
CHEMBL4079347 — IC50 = 710.0 nM 6.15
CHEMBL4100956 — IC50 = 710.0 nM 6.15
CHEMBL4062683 — IC50 = 810.0 nM 6.09
CHEMBL4091127 — IC50 = 890.0 nM 6.05
CHEMBL4091942 — IC50 = 1000.0 nM 6.00
CHEMBL4084364 — IC50 = 1100.0 nM 5.96
CHEMBL4098237 — IC50 = 1100.0 nM 5.96
CHEMBL4071013 — IC50 = 1200.0 nM 5.92
CHEMBL4092117 — IC50 = 1200.0 nM 5.92
CHEMBL4075509 — IC50 = 1200.0 nM 5.92
CHEMBL4097256 — IC50 = 1300.0 nM 5.89
CHEMBL4077125 — IC50 = 1300.0 nM 5.89
CHEMBL4088717 — IC50 = 1400.0 nM 5.85
CHEMBL4104296 — IC50 = 1400.0 nM 5.85
CHEMBL4093231 — IC50 = 1400.0 nM 5.85
CHEMBL4098107 — IC50 = 1500.0 nM 5.82
CHEMBL4076448 — IC50 = 1600.0 nM 5.80
CHEMBL4071234 — IC50 = 1600.0 nM 5.80
CHEMBL4067420 — IC50 = 1800.0 nM 5.75
CHEMBL4063254 — IC50 = 1800.0 nM 5.75
CHEMBL4075820 — IC50 = 1900.0 nM 5.72
CHEMBL4082981 — IC50 = 1900.0 nM 5.72
CHEMBL4064988 — IC50 = 1900.0 nM 5.72
CHEMBL4089542 — IC50 = 1900.0 nM 5.72
CHEMBL4076663 — IC50 = 1900.0 nM 5.72
CHEMBL4061394 — IC50 = 2100.0 nM 5.68
CHEMBL4090770 — IC50 = 2200.0 nM 5.66
CHEMBL4079343 — IC50 = 2200.0 nM 5.66