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Assay Detail

CHEMBL4678699

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

Binding
Inhibition of recombinant human ACSL1 assessed as reduction in acetyl-coA prodution incubated for 90 mins in presence of Coenzyme A, ATP and MgCl2 by MALDI-TOF MS analysis
30
Total Activities
30
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 30 6.37 8.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4764916 1 8.52
CHEMBL4750346 1 7.89
CHEMBL4746996 1 7.89
CHEMBL4787746 1 7.55
CHEMBL4749130 1 7.47
CHEMBL4781788 1 7.41
CHEMBL4778736 1 7.38
CHEMBL4797544 1 7.36
CHEMBL4755109 1 7.35
CHEMBL4748671 1 7.33
CHEMBL4740366 1 7.33
CHEMBL4783346 1 6.82
CHEMBL4800541 1 6.72
CHEMBL4757253 1 6.62
CHEMBL4757057 1 6.40
CHEMBL4748493 1 6.22
CHEMBL4751045 1 6.02
CHEMBL4787809 1 5.72
CHEMBL4800499 1 5.36
CHEMBL4746718 1 5.34
CHEMBL4752206 1 5.11
CHEMBL4791698 1 4.77
CHEMBL4754540 1 4.39
CHEMBL4747319 1 4.29
CHEMBL4745357 1 4.21
CHEMBL4746709 1 4.11
CHEMBL4744155 1 -
CHEMBL4744967 1 -
CHEMBL4785177 1 -
CHEMBL4761105 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4764916 IC50 = 3.0 nM 8.52
CHEMBL4750346 IC50 = 13.0 nM 7.89
CHEMBL4746996 IC50 = 13.0 nM 7.89
CHEMBL4787746 IC50 = 28.0 nM 7.55
CHEMBL4749130 IC50 = 34.0 nM 7.47
CHEMBL4781788 IC50 = 39.0 nM 7.41
CHEMBL4778736 IC50 = 42.0 nM 7.38
CHEMBL4797544 IC50 = 44.0 nM 7.36
CHEMBL4755109 IC50 = 45.0 nM 7.35
CHEMBL4748671 IC50 = 47.0 nM 7.33
CHEMBL4740366 IC50 = 47.0 nM 7.33
CHEMBL4783346 IC50 = 150.0 nM 6.82
CHEMBL4800541 IC50 = 190.0 nM 6.72
CHEMBL4757253 IC50 = 240.0 nM 6.62
CHEMBL4757057 IC50 = 400.0 nM 6.40
CHEMBL4748493 IC50 = 600.0 nM 6.22
CHEMBL4751045 IC50 = 950.0 nM 6.02
CHEMBL4787809 IC50 = 1900.0 nM 5.72
CHEMBL4800499 IC50 = 4400.0 nM 5.36
CHEMBL4746718 IC50 = 4600.0 nM 5.34
CHEMBL4752206 IC50 = 7800.0 nM 5.11
CHEMBL4791698 IC50 = 17000.0 nM 4.77
CHEMBL4754540 IC50 = 41000.0 nM 4.39
CHEMBL4747319 IC50 = 51000.0 nM 4.29
CHEMBL4745357 IC50 = 61000.0 nM 4.21
CHEMBL4746709 IC50 = 78000.0 nM 4.11
CHEMBL4744155 IC50 = 141000.0 nM -
CHEMBL4744967 IC50 > 200000.0 nM -
CHEMBL4785177 IC50 > 200000.0 nM -
CHEMBL4761105 IC50 > 200000.0 nM -