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Assay Detail

CHEMBL4739016

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

Binding
Inhibition of human recombinant CLK2 using YRRAAVPPSPSLSR substrate by radiometric scintillation assay
26
Total Activities
26
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

Highly selective inhibitors of protein kinases CLK and HIPK with the furo[3,2-b]pyridine core.
Němec V,Maier L,Berger BT,Chaikuad A,Drápela S,Souček K,Knapp S,Paruch K
Eur J Med Chem (2021) 215 : 113299 -113299
PubMed 33636538 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 26 6.94 7.80

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4762964 1 7.80
CHEMBL4797457 1 7.80
CHEMBL4754195 1 7.70
CHEMBL4750420 1 7.60
CHEMBL4789951 1 7.43
CHEMBL4743939 1 7.41
CHEMBL4743730 1 7.40
CHEMBL4790030 1 7.14
CHEMBL4791451 1 7.05
CHEMBL4740998 1 6.81
CHEMBL4790791 1 6.75
CHEMBL4778370 1 6.28
CHEMBL4741919 1 6.18
CHEMBL4794825 1 6.08
CHEMBL4777288 1 5.85
CHEMBL4789373 1 5.73
CHEMBL4777540 1 -
CHEMBL4758047 1 -
CHEMBL4747210 1 -
CHEMBL4790254 1 -
CHEMBL4800422 1 -
CHEMBL4793177 1 -
CHEMBL4777533 1 -
CHEMBL4747520 1 -
CHEMBL4795812 1 -
CHEMBL4778153 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4762964 IC50 = 16.0 nM 7.80
CHEMBL4797457 IC50 = 16.0 nM 7.80
CHEMBL4754195 IC50 = 20.0 nM 7.70
CHEMBL4750420 IC50 = 25.0 nM 7.60
CHEMBL4789951 IC50 = 37.0 nM 7.43
CHEMBL4743939 IC50 = 39.0 nM 7.41
CHEMBL4743730 IC50 = 40.0 nM 7.40
CHEMBL4790030 IC50 = 72.0 nM 7.14
CHEMBL4791451 IC50 = 90.0 nM 7.05
CHEMBL4740998 IC50 = 155.0 nM 6.81
CHEMBL4790791 IC50 = 176.0 nM 6.75
CHEMBL4778370 IC50 = 529.0 nM 6.28
CHEMBL4741919 IC50 = 667.0 nM 6.18
CHEMBL4794825 IC50 = 827.0 nM 6.08
CHEMBL4777288 IC50 = 1427.0 nM 5.85
CHEMBL4789373 IC50 = 1845.0 nM 5.73
CHEMBL4777540 IC50 > 3000.0 nM -
CHEMBL4758047 IC50 > 3000.0 nM -
CHEMBL4747210 IC50 > 3000.0 nM -
CHEMBL4790254 IC50 > 3000.0 nM -
CHEMBL4800422 IC50 > 3000.0 nM -
CHEMBL4793177 IC50 > 3000.0 nM -
CHEMBL4777533 IC50 > 3000.0 nM -
CHEMBL4747520 IC50 > 3000.0 nM -
CHEMBL4795812 IC50 > 3000.0 nM -
CHEMBL4778153 IC50 > 3000.0 nM -