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Compound Detail

CHEMBL4634377

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COc1cc2[nH]c3cc(Oc4ccc(OC(F)(F)F)cc4)ccc3c(=O)c2cc1Cl

Basic Information

ChEMBL ID CHEMBL4634377
Phase Preclinical
Structure Type MOL
InChI Key JKBZBWRRXCXJDA-UHFFFAOYSA-N
2
Targets
6
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

435.8
MW (Da)
6.03
ALogP
4
HBA
1
HBD
60.5
PSA (Ų)
0.40
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 C21H13ClF3NO4
MW 435.79
Aromatic Rings 4
Heavy Atoms 30
NP-Likeness -0.56

Activity Summary

IC50 6 meas. best 9.43

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium falciparum
CHEMBL364
IC50 9.43 8.99 0.4 5
Plasmodium berghei
CHEMBL612653
IC50 8.66 8.66 2.2 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 1.0 hr Homo sapiens
T1/2 1.0 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 falciparum 5
32390431 10.1021/acs.jmedchem.0c00539 Plasmodium berghei 5
32390431 10.1021/acs.jmedchem.0c00539 Plasmodium yoelii 2
32390431 10.1021/acs.jmedchem.0c00539 ADMET 2
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