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Compound Detail

CHEMBL3104487

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N#Cc1ccc(C(C(=O)N2CCN(c3ccc(C(F)(F)F)nc3)CC2)c2cccnc2)cc1

Basic Information

ChEMBL ID CHEMBL3104487
Phase Preclinical
Structure Type MOL
InChI Key KQYYFXSCJMMDOH-UHFFFAOYSA-N
1
Targets
3
Activities
1
Assay Types
6
PK Parameters
10
Publications
0
Known Names

Molecular Properties

451.4
MW (Da)
3.85
ALogP
5
HBA
0
HBD
73.1
PSA (Ų)
0.60
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 C24H20F3N5O
MW 451.45
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -1.78

Activity Summary

IC50 3 meas. best 7.69

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Trypanosoma cruzi
CHEMBL368
IC50 7.69 7.5433 20.5 3

Pharmacokinetic Data

Parameter Value Units Species
CL 12.0 mL.min-1.g-1 Homo sapiens
CL 22.0 mL.min-1.g-1 Homo sapiens
CL 21.0 mL.min-1.g-1 Homo sapiens
T1/2 2.4 hr Homo sapiens
T1/2 1.283 hr Homo sapiens
T1/2 1.35 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL3137386 No relevant target 12
- 10.6019/CHEMBL3137386 ADMET 9
- 10.6019/CHEMBL3137386 Trypanosoma cruzi 6
- 10.6019/CHEMBL3137386 Trypanosoma brucei rhodesiense 4
24304150 10.1021/jm401610c No relevant target 3
- 10.6019/CHEMBL3137386 Cytochrome P450 3A4 3
- 10.6019/CHEMBL3137386 L6 3
24304150 10.1021/jm401610c Cytochrome P450 3A4 1
24304150 10.1021/jm401610c L6 1
24304150 10.1021/jm401610c Trypanosoma cruzi 1

Data from ChEMBL 36 via Core Engine