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Compound Detail

CHEMBL4741532

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O=C(Cc1ccc(O)cc1)N1CC(CNc2ccccc2)C2(C1)CN(c1ccc(F)cc1)C2

Basic Information

ChEMBL ID CHEMBL4741532
Phase Preclinical
Structure Type MOL
InChI Key PVOZLBJLEIOESS-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
6
PK Parameters
3
Publications
0
Known Names

Molecular Properties

445.5
MW (Da)
4.15
ALogP
4
HBA
2
HBD
55.8
PSA (Ų)
0.60
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H28FN3O2
MW 445.54
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.71

Activity Summary

IC50 1 meas. best 6.99

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 6.99 6.99 103.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 809.55 ng.hr.mL-1 Mus musculus
CL 63.0 mL.min-1.kg-1 Mus musculus
CL 5042.0 mL.min-1.kg-1 Mus musculus
F 10.0 % Mus musculus
T1/2 4.0 hr Mus musculus
Vd 22.0 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Plasmodium falciparum IC50 = 103.0 nM 6.99 Antiplasmodial activity against multidrug-sensitive Plasmodium falciparum NF54 t... 33573376

Literature References

PubMed DOI Target Context # Activities
33573376 10.1021/acs.jmedchem.1c00034 Plasmodium falciparum 10
33573376 10.1021/acs.jmedchem.1c00034 ADMET 9
33573376 10.1021/acs.jmedchem.1c00034 Unchecked 1

Data from ChEMBL 36 via Core Engine