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Compound Detail

CHEMBL222328

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O=C1/C(=C/c2ccc(O)c(Br)c2)CCC/C1=C\c1ccc(O)c(Br)c1

Basic Information

ChEMBL ID CHEMBL222328
Phase Preclinical
Structure Type MOL
InChI Key YOLKEKNTCBWPSD-VOMDNODZSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
9
Publications
0
Known Names

Molecular Properties

464.1
MW (Da)
5.84
ALogP
3
HBA
2
HBD
57.5
PSA (Ų)
0.55
QED
1
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16Br2O3
MW 464.15
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness 0.02

Activity Summary

IC50 2 meas. best 5.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histone acetyltransferase p300
CHEMBL3784
IC50 5.3 5.3 5000.0 1
RmtA
CHEMBL1075069
IC50 4.05 4.05 90000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Histone acetyltransferase p300 IC50 = 5000.0 nM 5.3 Inhibition of GST-p300 HAT assessed as histone acetylation 17348637
RmtA IC50 = 90000.0 nM 4.05 Inhibition of Aspergillus nidulans RmtA 18348515

Literature References

PubMed DOI Target Context # Activities
17348637 10.1021/jm060943s HeLa 4
18348515 10.1021/jm701595q U-937 3
17348637 10.1021/jm060943s Histone acetyltransferase p300 2
17348637 10.1021/jm060943s Histone acetyltransferase KAT2A 1
17348637 10.1021/jm060943s Histone acetyltransferase KAT2B 1
18348515 10.1021/jm701595q RmtA 1
18348515 10.1021/jm701595q Protein arginine N-methyltransferase 1 1
18348515 10.1021/jm701595q Histone-lysine N-methyltransferase SETD7 1
18348515 10.1021/jm701595q Histone-arginine methyltransferase CARM1 1

Data from ChEMBL 36 via Core Engine