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Assay Detail

CHEMBL5550425

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

Binding
Inhibition of recombinant rat DYRK1A kinase domain (1 to 499 residues) expressed in bacteria using KKISGRLSPIMTEQ as substrate incubated for 30 mins in presence of ATP by ADP-Glo kinase assay
10
Total Activities
10
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
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

Synthesis and biological evaluation of 1H-pyrrolo[3,2-g]isoquinolines.
Defois M, Josselin B, Brindeau P, Krämer A, Knapp S, Anizon F, Giraud F, Ruchaud S, Moreau P.
Bioorg Med Chem (2024) 100 : 117619 -117619
PubMed 38320389 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 10 6.31 6.74

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL5569099 1 6.74
CHEMBL5594716 1 6.60
CHEMBL5562930 1 6.54
CHEMBL5571626 1 6.30
CHEMBL5570490 1 6.29
CHEMBL5563473 1 6.25
CHEMBL5574139 1 6.25
CHEMBL5564481 1 6.07
CHEMBL5181620 1 6.04
CHEMBL5592689 1 6.04

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL5569099 IC50 = 182.0 nM 6.74
CHEMBL5594716 IC50 = 250.0 nM 6.60
CHEMBL5562930 IC50 = 290.0 nM 6.54
CHEMBL5571626 IC50 = 495.0 nM 6.30
CHEMBL5570490 IC50 = 513.0 nM 6.29
CHEMBL5563473 IC50 = 564.0 nM 6.25
CHEMBL5574139 IC50 = 560.0 nM 6.25
CHEMBL5564481 IC50 = 860.0 nM 6.07
CHEMBL5181620 IC50 = 917.0 nM 6.04
CHEMBL5592689 IC50 = 916.0 nM 6.04