Skip to main content
Free research Free research Free compound review with research home and workspace preview
Quick search ChEMBL 36
Compound Detail

CHEMBL4640836

Enter ChEMBL ID:
Free Research Context This compound will appear in recent viewed items on the research home for this browser.
Research home View demo workspace
COc1cc([C@](O)(CCN(C)C)[C@@H](c2cc3cc(Br)ccc3nc2OC)c2ccnc(OC)c2OC)cc(OC(C)C)n1

Basic Information

ChEMBL ID CHEMBL4640836
Phase Preclinical
Structure Type MOL
InChI Key ZTHXAYLSWHJAAQ-AKGWNBJDSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

655.6
MW (Da)
5.58
ALogP
10
HBA
1
HBD
108.3
PSA (Ų)
0.20
QED
2
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H39BrN4O6
MW 655.59
Aromatic Rings 4
Heavy Atoms 43
NP-Likeness -0.58

Activity Summary

IC50 1 meas. best 4.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 4.77 4.77 17000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 5600.0 ng.hr.mL-1 Mus musculus
CL 6.8 mL.min-1.kg-1 Mus musculus
F 22.0 % Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 17000.0 nM 4.77 Inhibition of human ERG 31810890

Literature References

PubMed DOI Target Context # Activities
31810890 10.1016/j.bmc.2019.115213 ADMET 6
31810890 10.1016/j.bmc.2019.115213 Mycobacterium tuberculosis 3
31810890 10.1016/j.bmc.2019.115213 Voltage-gated inwardly rectifying potassium channel KCNH2 1
31810890 10.1016/j.bmc.2019.115213 Vero 1

Data from ChEMBL 36 via Core Engine