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Assay Detail

CHEMBL5105892

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

Binding
Inhibition of DYRK1A (unknown origin)
6
Total Activities
6
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

Publication

A critical update on the strategies towards small molecule inhibitors targeting Serine/arginine-rich (SR) proteins and Serine/arginine-rich proteins related kinases in alternative splicing.
Tang J, Xie Y, Huang J, Zhang L, Jiang W, Li Z, Bian J.
Bioorg Med Chem (2022) 70 : 116921 -116921
PubMed 35863237 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 6 7.12 7.57

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4297639 LORECIVIVINT 3.0 1 7.57
CHEMBL1236620 1 7.26
CHEMBL1946917 1 7.17
CHEMBL5191815 1 7.13
CHEMBL269538 HARMINE 1.0 1 7.10
CHEMBL297453 EPIGALOCATECHIN GALLATE 3.0 1 6.48

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4297639 LORECIVIVINT IC50 = 26.9 nM 7.57
CHEMBL1236620 IC50 = 55.0 nM 7.26
CHEMBL1946917 IC50 = 67.0 nM 7.17
CHEMBL5191815 IC50 = 74.0 nM 7.13
CHEMBL269538 HARMINE IC50 = 80.0 nM 7.10
CHEMBL297453 EPIGALOCATECHIN GALLATE IC50 = 330.0 nM 6.48