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Compound Detail

CHEMBL5200059

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COc1ccc2nc3cc(Cl)ccc3c(NCCC(=O)NCc3cccc(COc4nc(N)nc5[nH]cnc45)c3)c2c1

Basic Information

ChEMBL ID CHEMBL5200059
Phase Preclinical
Structure Type MOL
InChI Key JUHOVAHJTCSLRW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

583.0
MW (Da)
5.00
ALogP
9
HBA
4
HBD
153.0
PSA (Ų)
0.16
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H27ClN8O3
MW 583.05
Aromatic Rings 6
Heavy Atoms 42
NP-Likeness -1.00

Activity Summary

Kd 1 meas. best 4.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Calf thymus DNA
CHEMBL612514
Kd 4.79 4.79 16200.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Calf thymus DNA Kd = 16200.0 nM 4.79 Binding affinity to calf thymus DNA assessed as intercalation by measuring disso... 34731767

Literature References

PubMed DOI Target Context # Activities
34731767 10.1016/j.ejmech.2021.113909 No relevant target 9
34731767 10.1016/j.ejmech.2021.113909 T98G 4
34731767 10.1016/j.ejmech.2021.113909 Calf thymus DNA 3
34731767 10.1016/j.ejmech.2021.113909 Methylated-DNA--protein-cysteine methyltransferase 3

Data from ChEMBL 36 via Core Engine