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Assay Detail

CHEMBL4625229

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

Binding
Inhibition of recombinant Hi6-tagged deltaFOSB (unknown origin) expressed in insect cells interaction with TAMRA labeled 5'-GTCGGTGACTCAAAACA-3' AP1 oligonucleotide measured after 15 mins by fluorescence polarization assay
16
Total Activities
15
Compounds Tested
2
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Protein FosB (CHEMBL4630821)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Discovery of phenanthridine analogues as novel chemical probes disrupting the binding of DNA to ΔFosB homodimers and ΔFosB/JunD heterodimers.
Li Y, Liu Z, Aglyamova G, Chen J, Chen H, Bhandari M, White MA, Rudenko G, Zhou J.
Bioorg Med Chem Lett (2020) 30 : 127300 -127300
PubMed 32631520 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 15 4.39 4.54
Inhibition 1 - -

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL1528814 1 4.54
CHEMBL4640716 2 4.24
CHEMBL4635546 1 -
CHEMBL4634410 1 -
CHEMBL4640911 1 -
CHEMBL4642507 1 -
CHEMBL4636518 1 -
CHEMBL4646481 1 -
CHEMBL4644096 1 -
CHEMBL4648918 1 -
CHEMBL4648459 1 -
CHEMBL4638737 1 -
CHEMBL4637145 1 -
CHEMBL4648025 1 -
CHEMBL4643910 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL1528814 IC50 = 28900.0 nM 4.54
CHEMBL4640716 IC50 = 58000.0 nM 4.24
CHEMBL4635546 IC50 > 100000.0 nM -
CHEMBL4634410 IC50 > 100000.0 nM -
CHEMBL4640911 IC50 > 100000.0 nM -
CHEMBL4642507 IC50 > 100000.0 nM -
CHEMBL4636518 IC50 > 100000.0 nM -
CHEMBL4646481 IC50 > 100000.0 nM -
CHEMBL4644096 IC50 - -
CHEMBL4648918 IC50 > 100000.0 nM -
CHEMBL4648459 IC50 > 100000.0 nM -
CHEMBL4638737 IC50 > 100000.0 nM -
CHEMBL4637145 IC50 > 100000.0 nM -
CHEMBL4648025 IC50 > 100000.0 nM -
CHEMBL4643910 IC50 - -
CHEMBL4640716 Inhibition - % -