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Assay Detail

CHEMBL5522372

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

Binding
Inhibition of CLK2 (unknown origin) incubated for 10 mins in presence of ATP
27
Total Activities
27
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 protein kinase CLK2 (CHEMBL4225)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Guided Discovery of Potent and Selective CLK2 Inhibitors for the Treatment of Knee Osteoarthritis.
Sun Y, Hu T, Zhang M, Song J, Qin Z, Liu M, Ji J, Li Z, Qiu Z, Bian J.
J Med Chem (2024) 67 : 4603 -4623
PubMed 38500250 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 27 7.80 8.85

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5561941 1 8.85
CHEMBL5560595 1 8.43
CHEMBL5563432 1 8.25
CHEMBL5559906 1 8.17
CHEMBL5558849 1 8.12
CHEMBL4297639 LORECIVIVINT 3.0 1 8.11
CHEMBL5559654 1 8.00
CHEMBL5568383 1 7.99
CHEMBL5287080 1 7.91
CHEMBL5564232 1 7.88
CHEMBL5565284 1 7.86
CHEMBL5555969 1 7.80
CHEMBL5559924 1 7.77
CHEMBL5567834 1 7.67
CHEMBL5566340 1 7.57
CHEMBL5562209 1 7.55
CHEMBL5560569 1 7.50
CHEMBL5560831 1 7.45
CHEMBL5565578 1 7.40
CHEMBL5561762 1 7.40
CHEMBL5557860 1 7.30
CHEMBL5560522 1 7.20
CHEMBL5559843 1 7.20
CHEMBL5568024 1 -
CHEMBL5542986 1 -
CHEMBL5561870 1 -
CHEMBL5542457 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5561941 IC50 = 1.4 nM 8.85
CHEMBL5560595 IC50 = 3.7 nM 8.43
CHEMBL5563432 IC50 = 5.6 nM 8.25
CHEMBL5559906 IC50 = 6.8 nM 8.17
CHEMBL5558849 IC50 = 7.6 nM 8.12
CHEMBL4297639 LORECIVIVINT IC50 = 7.8 nM 8.11
CHEMBL5559654 IC50 = 10.0 nM 8.00
CHEMBL5568383 IC50 = 10.2 nM 7.99
CHEMBL5287080 IC50 = 12.3 nM 7.91
CHEMBL5564232 IC50 = 13.3 nM 7.88
CHEMBL5565284 IC50 = 13.7 nM 7.86
CHEMBL5555969 IC50 = 15.8 nM 7.80
CHEMBL5559924 IC50 = 17.1 nM 7.77
CHEMBL5567834 IC50 = 21.3 nM 7.67
CHEMBL5566340 IC50 = 27.1 nM 7.57
CHEMBL5562209 IC50 = 28.2 nM 7.55
CHEMBL5560569 IC50 = 31.6 nM 7.50
CHEMBL5560831 IC50 = 35.5 nM 7.45
CHEMBL5565578 IC50 = 39.8 nM 7.40
CHEMBL5561762 IC50 = 39.8 nM 7.40
CHEMBL5557860 IC50 = 50.1 nM 7.30
CHEMBL5560522 IC50 = 63.1 nM 7.20
CHEMBL5559843 IC50 = 63.1 nM 7.20
CHEMBL5568024 IC50 > 100.0 nM -
CHEMBL5542986 IC50 > 100.0 nM -
CHEMBL5561870 IC50 > 100.0 nM -
CHEMBL5542457 IC50 > 100.0 nM -