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Assay Detail

CHEMBL4678700

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

Binding
Inhibition of ACSL1 (unknown origin) assessed as reduction in acetyl-coA prodution incubated for 90 mins in presence of Coenzyme A, ATP and MgCl2 by MALDI-TOF MS analysis
9
Total Activities
9
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

Long-chain-fatty-acid--CoA ligase 1 (CHEMBL4295746)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of a benzimidazole series as the first highly potent and selective ACSL1 inhibitors.
Hayashi K,Kondo N,Omori N,Yoshimoto R,Hato M,Shigaki S,Nagasawa A,Ito M,Okuno T
Bioorg Med Chem Lett (2021) 33 : 127722 -127722
PubMed 33285268 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 9 5.91 6.62

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4761388 1 6.62
CHEMBL4776019 1 6.51
CHEMBL222502 1 5.77
CHEMBL4751846 1 4.75
CHEMBL4749993 1 -
CHEMBL4792940 1 -
CHEMBL4798042 1 -
CHEMBL4789782 1 -
CHEMBL4757253 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4761388 IC50 = 240.0 nM 6.62
CHEMBL4776019 IC50 = 310.0 nM 6.51
CHEMBL222502 IC50 = 1700.0 nM 5.77
CHEMBL4751846 IC50 = 18000.0 nM 4.75
CHEMBL4749993 IC50 > 200000.0 nM -
CHEMBL4792940 IC50 > 200000.0 nM -
CHEMBL4798042 IC50 > 200000.0 nM -
CHEMBL4789782 IC50 > 200000.0 nM -
CHEMBL4757253 IC50 > 200000.0 nM -