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Compound Detail

CHEMBL3137391

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O=C(C(c1ccc(Cl)cc1)c1cncnc1)N1CCN(c2ccc(C(F)(F)F)cn2)CC1

Basic Information

ChEMBL ID CHEMBL3137391
Phase Preclinical
Structure Type MOL
InChI Key PXISBMZXCKNRIL-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
2
PK Parameters
6
Publications
0
Known Names

Molecular Properties

461.9
MW (Da)
4.02
ALogP
5
HBA
0
HBD
62.2
PSA (Ų)
0.59
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H19ClF3N5O
MW 461.88
Aromatic Rings 3
Heavy Atoms 32
NP-Likeness -1.95

Activity Summary

IC50 3 meas. best 6.79

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
IC50 6.79 6.79 161.0 1
Cytochrome P450 3A4
CHEMBL340
IC50 4.75 4.75 18000.0 1
L6
CHEMBL614793
IC50 4.28 4.28 52510.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 76.0 mL.min-1.g-1 Homo sapiens
T1/2 0.3833 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Trypanosoma cruzi IC50 = 161.0 nM 6.79 DNDI: Chagas in vitro -
Cytochrome P450 3A4 IC50 = 18000.0 nM 4.75 DNDI: CYP Inhibition -
L6 IC50 = 52510.0 nM 4.28 DNDI: Cytotoxicity against L-6 rat myoblasts from skeletal muscle -

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3137386 No relevant target 4
- 10.6019/CHEMBL3137386 ADMET 3
- 10.6019/CHEMBL3137386 Trypanosoma cruzi 2
- 10.6019/CHEMBL3137386 Cytochrome P450 3A4 1
- 10.6019/CHEMBL3137386 L6 1
- 10.6019/CHEMBL3137386 Trypanosoma brucei rhodesiense 1

Data from ChEMBL 36 via Core Engine