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Compound Detail

CHEMBL4576867

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OCc1cccc(-c2ccc3nc(-c4ccc(Cl)cc4)cn3c2)c1

Basic Information

ChEMBL ID CHEMBL4576867
Phase Preclinical
Structure Type MOL
InChI Key IHUPABWARJLUMA-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

334.8
MW (Da)
4.81
ALogP
3
HBA
1
HBD
37.5
PSA (Ų)
0.58
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H15ClN2O
MW 334.81
Aromatic Rings 4
Heavy Atoms 24
NP-Likeness -1.25

Activity Summary

EC50 3 meas. best 9.0
IC50 1 meas. best 5.07

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Nuclear receptor subfamily 4 group A member 2
CHEMBL3879839
EC50 9.0 9.0 1.0 1
Nuclear receptor subfamily 4 group A member 2
CHEMBL5002
EC50 7.35 7.35 45.0 1
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
EC50 6.05 6.05 900.0 1
Cytochrome P450 2C9
CHEMBL3397
IC50 5.07 5.07 8600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
30773432 10.1016/j.bmcl.2019.01.024 ADMET 8
30773432 10.1016/j.bmcl.2019.01.024 Nuclear receptor subfamily 4 group A member 2 8
30773432 10.1016/j.bmcl.2019.01.024 No relevant target 3
30773432 10.1016/j.bmcl.2019.01.024 Voltage-gated inwardly rectifying potassium channel KCNH2 1
30773432 10.1016/j.bmcl.2019.01.024 Cytochrome P450 1
30773432 10.1016/j.bmcl.2019.01.024 Cytochrome P450 2C9 1
30773432 10.1016/j.bmcl.2019.01.024 Cytochrome P450 2D6 1
30773432 10.1016/j.bmcl.2019.01.024 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine