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Compound Detail

CHEMBL4761821

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NC(=O)c1cc(CC(=O)N2CC(CNc3ccc(F)cc3)C3(C2)CN(c2cc(F)cc(F)c2)C3)ccc1O

Basic Information

ChEMBL ID CHEMBL4761821
Phase Preclinical
Structure Type MOL
InChI Key HOXRKFZDWBNNOP-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
3
Publications
0
Known Names

Molecular Properties

524.5
MW (Da)
3.53
ALogP
5
HBA
3
HBD
98.9
PSA (Ų)
0.44
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H27F3N4O3
MW 524.54
Aromatic Rings 3
Heavy Atoms 38
NP-Likeness -0.78

Activity Summary

IC50 1 meas. best 5.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 5.34 5.34 4600.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.1833 hr Homo sapiens
T1/2 0.1333 hr Rattus norvegicus
T1/2 0.35 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmodium falciparum IC50 = 4600.0 nM 5.34 Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum NF54 t... 33573376

Literature References

PubMed DOI Target Context # Activities
33573376 10.1021/acs.jmedchem.1c00034 ADMET 6
33573376 10.1021/acs.jmedchem.1c00034 Plasmodium falciparum 1
33573376 10.1021/acs.jmedchem.1c00034 No relevant target 1

Data from ChEMBL 36 via Core Engine