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Compound Detail

CHEMBL552873

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COc1cc2c(cc1OCCC(=O)Nc1cc(C(=O)Nc3cc(C(=O)Nc4cc(C(=O)Nc5cc(C(=O)NCCC(=N)N)n(C)c5)n(C)c4)n(C)c3)n(C)c1)N=C[C@@H]1CCCN1C2=O.Cl

Basic Information

ChEMBL ID CHEMBL552873
Phase Preclinical
Structure Type MOL
InChI Key IVTZBYKYFIXULC-JCOPYZAKSA-N
Parent Compound CHEMBL1194569
Active Moiety CHEMBL1194569
5
Targets
7
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

876.0
MW (Da)
3.59
ALogP
14
HBA
7
HBD
266.2
PSA (Ų)
0.06
QED
3
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H50ClN13O8
MW 912.41
Aromatic Rings 5
Heavy Atoms 64
NP-Likeness -0.34

Activity Summary

IC50 7 meas. best 7.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
K562
CHEMBL385
IC50 7.4 7.4 40.0 2
Jurkat
CHEMBL397
IC50 7.16 7.16 70.0 2
Nucleic Acid
CHEMBL345
IC50 6.7 6.7 200.0 1
Human immunodeficiency virus 1
CHEMBL378
IC50 5.7 5.7 2000.0 1
Unchecked
CHEMBL612545
IC50 5.7 5.7 2000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10602698 10.1021/jm991033w Jurkat 1
10602698 10.1021/jm991033w K562 1
10602698 10.1021/jm991033w Unchecked 1
10602698 10.1021/jm991033w Nucleic Acid 1
10602698 10.1021/jm991033w Human immunodeficiency virus 1 1
17081759 10.1016/j.bmc.2006.07.004 K562 1
17081759 10.1016/j.bmc.2006.07.004 Jurkat 1
26116177 10.1016/j.bmc.2015.06.016 Unchecked 1

Data from ChEMBL 36 via Core Engine