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Compound Detail

CHEMBL3234764

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CCNC(=O)c1nnn(-c2cc(C(C)C)c(O)cc2O)c1-c1ccc(CN2CCOCC2)cc1

Basic Information

ChEMBL ID CHEMBL3234764
Phase Preclinical
Structure Type MOL
InChI Key CKHCXYIYTCETLS-UHFFFAOYSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

465.6
MW (Da)
3.05
ALogP
8
HBA
3
HBD
112.7
PSA (Ų)
0.49
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H31N5O4
MW 465.55
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.17

Activity Summary

IC50 6 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 9.0 9.0 1.0 1
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 9.0 9.0 1.0 1
L6
CHEMBL614793
IC50 8.7 8.7 2.0 1
NCI-H460
CHEMBL396
IC50 8.4 8.4 4.0 1
Trypanosoma cruzi
CHEMBL368
IC50 7.57 7.57 27.0 1
Giardia intestinalis
CHEMBL612652
IC50 7.17 7.17 67.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
24588105 10.1021/jm401536b Mus musculus 12
24588105 10.1021/jm401536b Heat shock protein HSP 90-beta 4
24588105 10.1021/jm401536b NCI-H460 3
24588105 10.1021/jm401536b Heat shock protein HSP 90-alpha 1
24588105 10.1021/jm401536b A-431 1
24588105 10.1021/jm401536b NON-PROTEIN TARGET 1
24588105 10.1021/jm401536b Plasma 1
25547934 10.1016/j.bmcl.2014.12.048 Trypanosoma cruzi 1
25547934 10.1016/j.bmcl.2014.12.048 Trypanosoma brucei rhodesiense 1
25547934 10.1016/j.bmcl.2014.12.048 Plasmodium falciparum 1
25547934 10.1016/j.bmcl.2014.12.048 Giardia intestinalis 1
25547934 10.1016/j.bmcl.2014.12.048 L6 1
35973342 10.1016/j.ejmech.2022.114633 Heat shock protein HSP 90-alpha 1

Data from ChEMBL 36 via Core Engine