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Compound Detail

CHEMBL221782

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O=C(/C=C(O)/C=C/c1ccc(O)c(Br)c1)/C=C/c1ccc(O)c(Br)c1

Basic Information

ChEMBL ID CHEMBL221782
Phase Preclinical
Structure Type MOL
InChI Key MFFJMPAOJWWEKY-XVVYLEPSSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

466.1
MW (Da)
5.36
ALogP
4
HBA
3
HBD
77.8
PSA (Ų)
0.32
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H14Br2O4
MW 466.13
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness 0.86

Activity Summary

IC50 1 meas. best 4.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone acetyltransferase p300
CHEMBL3784
IC50 4.48 4.48 33000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone acetyltransferase p300 IC50 = 33000.0 nM 4.48 Inhibition of GST-p300 HAT assessed as histone acetylation 17348637

Literature References

PubMed DOI Target Context # Activities
23276449 10.1016/j.bmc.2012.11.033 Vitamin D3 receptor 2
17348637 10.1021/jm060943s Histone acetyltransferase p300 1
23276449 10.1016/j.bmc.2012.11.033 Retinoic acid receptor RXR-alpha 1
23276449 10.1016/j.bmc.2012.11.033 Retinoic acid receptor 1
23276449 10.1016/j.bmc.2012.11.033 Retinoid X receptor 1
23276449 10.1016/j.bmc.2012.11.033 Glucocorticoid receptor 1
23276449 10.1016/j.bmc.2012.11.033 Retinoic acid receptor RXR-alpha/Vitamin D3 receptor 1

Data from ChEMBL 36 via Core Engine