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Assay Detail

CHEMBL4727754

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

Binding
Inhibition of human ALK2 R206H mutant using casein as substrate in presence of [gamma-33P]-ATP by radiometric hotspot assay
5
Total Activities
5
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 0 — Uncurated / Unknown
Curated By Autocuration

Target

Unchecked (CHEMBL612545)
Type UNCHECKED

Publication

Discovery, synthesis and characterization of a series of 7-aryl-imidazo[1,2-a]pyridine-3-ylquinolines as activin-like kinase (ALK) inhibitors.
Engers DW,Bollinger SR,Felts AS,Vadukoot AK,Williams CH,Blobaum AL,Lindsley CW,Hong CC,Hopkins CR
Bioorg Med Chem Lett (2020) 30 : 127418 -127418
PubMed 32750526 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 5 8.24 8.42

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4740381 1 8.42
CHEMBL4788859 1 8.25
CHEMBL4786529 1 8.06
CHEMBL4742906 1 -
CHEMBL4778971 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4740381 IC50 = 3.8 nM 8.42
CHEMBL4788859 IC50 = 5.6 nM 8.25
CHEMBL4786529 IC50 = 8.8 nM 8.06
CHEMBL4742906 IC50 < 5.0 nM -
CHEMBL4778971 IC50 < 5.0 nM -