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Compound Detail

CHEMBL2030016

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Cc1c(-c2ccc(Cc3ccc(OC(F)(F)F)cc3)cc2)[nH]c2cc(Cl)ccc2c1=O

Basic Information

ChEMBL ID CHEMBL2030016
Phase Preclinical
Structure Type MOL
InChI Key GGVLPENGSGQOOU-UHFFFAOYSA-N
2
Targets
7
Activities
1
Assay Types
2
PK Parameters
8
Publications
0
Known Names

Molecular Properties

443.9
MW (Da)
6.65
ALogP
2
HBA
1
HBD
42.1
PSA (Ų)
0.38
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H17ClF3NO2
MW 443.85
Aromatic Rings 4
Heavy Atoms 31
NP-Likeness -0.55

Activity Summary

IC50 7 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 7.8 6.405 16.0 2
Plasmodium falciparum
CHEMBL364
IC50 7.77 7.396 17.0 5

Pharmacokinetic Data

Parameter Value Units Species
CL 0.76 mL.min-1.kg-1 Homo sapiens
T1/2 3.767 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22364416 10.1021/jm201179h Unchecked 3
22364416 10.1021/jm201179h Plasmodium falciparum 3
22364416 10.1021/jm201179h Plasmodium berghei 3
22364416 10.1021/jm201179h Liver microsomes 3
22364416 10.1021/jm201179h HepG2 1
22364417 10.1021/jm201184h Plasmodium falciparum 1
35033884 10.1016/j.bmc.2022.116614 No relevant target 1
35033884 10.1016/j.bmc.2022.116614 Plasmodium falciparum 1

Data from ChEMBL 36 via Core Engine