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Compound Detail

CHEMBL3259948

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O=C(N[C@H](Cc1c[nH]c2ccccc12)C(=O)Nc1ccncc1)c1ccc(N2CCN(c3cccc(C(F)(F)F)c3)CC2)cc1F

Basic Information

ChEMBL ID CHEMBL3259948
Phase Preclinical
Structure Type MOL
InChI Key OOZYTONLGPPKPM-WJOKGBTCSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
7
Publications
0
Known Names

Molecular Properties

630.6
MW (Da)
6.03
ALogP
5
HBA
3
HBD
93.4
PSA (Ų)
0.18
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C34H30F4N6O2
MW 630.65
Aromatic Rings 5
Heavy Atoms 46
NP-Likeness -1.35

Activity Summary

EC50 1 meas. best 9.33

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
EC50 9.33 9.33 0.5 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.1333 hr Homo sapiens
T1/2 0.4 hr Rattus norvegicus
T1/2 0.1833 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma cruzi EC50 = 0.47 nM 9.33 Antitrypanosomal activity against trypomastigotes of Trypanosoma cruzi CA-I/72 i... 24900854

Literature References

PubMed DOI Target Context # Activities
24900854 10.1021/ml500010m Liver microsome 2
24900854 10.1021/ml500010m Trypanosoma cruzi 1
24900854 10.1021/ml500010m Liver 1
24900854 10.1021/ml500010m Cytochrome P450 1A2 1
24900854 10.1021/ml500010m Cytochrome P450 2C9 1
24900854 10.1021/ml500010m Cytochrome P450 2D6 1
24900854 10.1021/ml500010m Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine