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Compound Detail

CHEMBL4640206

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COc1cc(F)c2c(=O)c3ccc(Oc4ccc(OC(F)(F)F)cc4)cc3[nH]c2c1

Basic Information

ChEMBL ID CHEMBL4640206
Phase Preclinical
Structure Type MOL
InChI Key OYSIWQHFVXULED-UHFFFAOYSA-N
3
Targets
6
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

419.3
MW (Da)
5.52
ALogP
4
HBA
1
HBD
60.5
PSA (Ų)
0.35
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H13F4NO4
MW 419.33
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.35

Activity Summary

IC50 6 meas. best 9.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 9.51 8.795 0.3 4
Plasmodium berghei
CHEMBL612653
IC50 9.35 9.35 0.5 1
HepG2
CHEMBL395
IC50 6.12 6.12 755.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.0 hr Homo sapiens
T1/2 0.8333 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32390431 10.1021/acs.jmedchem.0c00539 Plasmodium berghei 5
32390431 10.1021/acs.jmedchem.0c00539 Plasmodium falciparum 4
32390431 10.1021/acs.jmedchem.0c00539 ADMET 4
32390431 10.1021/acs.jmedchem.0c00539 Plasmodium yoelii 4
32390431 10.1021/acs.jmedchem.0c00539 HepG2 1
32390431 10.1021/acs.jmedchem.0c00539 Unchecked 1
32390431 10.1021/acs.jmedchem.0c00539 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine