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Compound Detail

CHEMBL4095346

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COc1cc2nc(Nc3ccc(F)cc3)nc(NCC3CCCO3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL4095346
Phase Preclinical
Structure Type MOL
InChI Key UXKWXGQTMJMRQT-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
4
PK Parameters
5
Publications
0
Known Names

Molecular Properties

398.4
MW (Da)
4.12
ALogP
7
HBA
2
HBD
77.5
PSA (Ų)
0.62
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 C21H23FN4O3
MW 398.44
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.16

Activity Summary

EC50 2 meas. best 7.24

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
EC50 7.24 7.24 57.0 1
HepG2
CHEMBL395
EC50 5.26 5.26 5500.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 27.0 mL.min-1.g-1 Homo sapiens
CL 72.0 mL.min-1.g-1 Mus musculus
T1/2 1.067 hr Homo sapiens
T1/2 0.4 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28080063 10.1021/acs.jmedchem.6b01673 Liver 8
28080063 10.1021/acs.jmedchem.6b01673 No relevant target 2
28080063 10.1021/acs.jmedchem.6b01673 Plasmodium falciparum 1
28080063 10.1021/acs.jmedchem.6b01673 HepG2 1
28080063 10.1021/acs.jmedchem.6b01673 Unchecked 1

Data from ChEMBL 36 via Core Engine