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Compound Detail

CHEMBL4780715

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FC(F)Oc1ccc(-c2nnc3cncc(OCCc4ccccc4)n23)cc1

Basic Information

ChEMBL ID CHEMBL4780715
Phase Preclinical
Structure Type MOL
InChI Key AVBCIJLYABLIRW-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
2
PK Parameters
7
Publications
0
Known Names

Molecular Properties

382.4
MW (Da)
4.01
ALogP
6
HBA
0
HBD
61.5
PSA (Ų)
0.48
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H16F2N4O2
MW 382.37
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.43

Activity Summary

IC50 5 meas. best 6.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Plasmodium
CHEMBL4888483
IC50 6.77 6.77 170.0 1
Plasmodium falciparum
CHEMBL364
IC50 6.51 6.4033 310.0 3
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.13 5.13 7410.0 1

Pharmacokinetic Data

Parameter Value Units Species
T1/2 0.4333 hr Homo sapiens
T1/2 0.1167 hr Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32678591 10.1021/acs.jmedchem.0c00746 No relevant target 2
32678591 10.1021/acs.jmedchem.0c00746 ADMET 2
34748707 10.1021/acs.jmedchem.1c00313 Unchecked 2
38516592 10.1039/d3md00490b Plasmodium falciparum 2
32678591 10.1021/acs.jmedchem.0c00746 Voltage-gated inwardly rectifying potassium channel KCNH2 1
34748707 10.1021/acs.jmedchem.1c00313 Plasmodium falciparum 1
39291016 10.1021/acsmedchemlett.4c00131 Plasmodium 1

Data from ChEMBL 36 via Core Engine