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Compound Detail

CHEMBL4059932

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Clc1cc(-c2ccnc(N3CCNCC3)c2)cc(Cl)c1OCCc1ccccn1

Basic Information

ChEMBL ID CHEMBL4059932
Phase Preclinical
Structure Type MOL
InChI Key YJEPFURSSGLPSU-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

429.4
MW (Da)
4.48
ALogP
5
HBA
1
HBD
50.3
PSA (Ų)
0.63
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H22Cl2N4O
MW 429.35
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.34

Activity Summary

IC50 1 meas. best 6.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.1 6.1 800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 800.0 nM 6.1 Inhibition of Trypanosoma brucei NMT using [3H]-myristoyl-coA/biotinylated CAP5.... 29125744

Literature References

PubMed DOI Target Context # Activities
29125744 10.1021/acs.jmedchem.7b01255 Unchecked 2
29125744 10.1021/acs.jmedchem.7b01255 Trypanosoma brucei brucei 1
29125744 10.1021/acs.jmedchem.7b01255 Glycylpeptide N-tetradecanoyltransferase 1 1
29125744 10.1021/acs.jmedchem.7b01255 MRC5 1

Data from ChEMBL 36 via Core Engine