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Compound Detail

CHEMBL4646329

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COc1cc([C@](O)(CCN(C)C)[C@@H](c2cc3cc(Br)ccc3nc2OC)c2cccc(OC)c2F)cc(S(C)(=O)=O)n1

Basic Information

ChEMBL ID CHEMBL4646329
Phase Preclinical
Structure Type MOL
InChI Key HCSVBNXMCYZZGD-POURPWNDSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

662.6
MW (Da)
4.93
ALogP
9
HBA
1
HBD
111.1
PSA (Ų)
0.24
QED
1
Ro5 Violations
11
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C30H33BrFN3O6S
MW 662.58
Aromatic Rings 4
Heavy Atoms 42
NP-Likeness -0.84

Activity Summary

IC50 1 meas. best 5.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.75 5.75 1800.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Voltage-gated inwardly rectifying potassium channel KCNH2 IC50 = 1800.0 nM 5.75 Inhibition of human ERG 31810890

Literature References

PubMed DOI Target Context # Activities
31810890 10.1016/j.bmc.2019.115213 Mycobacterium tuberculosis 2
31810890 10.1016/j.bmc.2019.115213 Voltage-gated inwardly rectifying potassium channel KCNH2 1

Data from ChEMBL 36 via Core Engine