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Compound Detail

CHEMBL25999

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N=C(NC1CCCC1)c1ccc(-c2ccc(-c3ccc(C(=N)NC4CCCC4)cc3)o2)cc1

Basic Information

ChEMBL ID CHEMBL25999
Phase Preclinical
Structure Type MOL
InChI Key QWOAXYIWWNHZBQ-UHFFFAOYSA-N
5
Targets
7
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

440.6
MW (Da)
6.33
ALogP
3
HBA
4
HBD
84.9
PSA (Ų)
0.27
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H32N4O
MW 440.59
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.21

Activity Summary

IC50 7 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma brucei rhodesiense
CHEMBL612348
IC50 7.22 7.22 60.0 1
Trypanosoma brucei brucei
CHEMBL612851
IC50 7.0 7.0 100.0 1
CH1
CHEMBL614455
IC50 5.44 5.44 3600.0 1
A2780
CHEMBL614004
IC50 5.42 5.0867 3800.0 3
SK-OV-3
CHEMBL614925
IC50 4.77 4.77 17000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9438029 10.1021/jm970570i Rattus norvegicus 4
9438029 10.1021/jm970570i ADMET 4
9748362 10.1021/jm980230c Rattus norvegicus 4
9748362 10.1021/jm980230c ADMET 4
11128631 10.1016/s0960-894x(00)00511-4 Rattus norvegicus 2
- 10.1016/S0960-894X(97)00229-1 A2780 2
17499888 10.1016/j.ejmech.2007.03.009 Pneumocystis carinii 2
17517831 10.1128/aac.00005-07 Unchecked 2
17517831 10.1128/aac.00005-07 Trypanosoma brucei brucei 2
11128631 10.1016/s0960-894x(00)00511-4 A2780 1
- 10.1016/S0960-894X(97)00229-1 CH1 1
- 10.1016/S0960-894X(97)00229-1 SK-OV-3 1
- 10.1016/S0960-894X(97)00229-1 Unchecked 1
17499888 10.1016/j.ejmech.2007.03.009 Rattus norvegicus 1
17517831 10.1128/aac.00005-07 Trypanosoma brucei rhodesiense 1

Data from ChEMBL 36 via Core Engine