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Assay Detail

CHEMBL4689214

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ADMET
Inhibition of rat DYRK1A (1 to 499 residues) assessed as residual activity by ADP-Glo assay
2
Total Activities
2
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type ADMET
Organism Rattus norvegicus
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Dual specificity tyrosine-phosphorylation-regulated kinase 1A (CHEMBL5508)
Type SINGLE PROTEIN
Organism Rattus norvegicus

Publication

Discovery of DB18, a potent inhibitor of CLK kinases with a high selectivity against DYRK1A kinase.
Brahmaiah D,Kanaka Durga Bhavani A,Aparna P,Sampath Kumar N,Solhi H,Le Guevel R,Baratte B,Ruchaud S,Bach S,Singh Jadav S,Raji Reddy C,Roisnel T,Mosset P,Levoin N,Grée R
Bioorg Med Chem (2021) 31 : 115962 -115962
PubMed 33422908 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 2 6.22 6.92

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4783398 1 6.92
CHEMBL4758072 1 5.52

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4783398 IC50 = 120.0 nM 6.92
CHEMBL4758072 IC50 = 3000.0 nM 5.52