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Compound Detail

CHEMBL4642317

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COc1nc2ccc(C#N)cc2cc1[C@@H](c1cccc2c1OCO2)[C@@](O)(CCN(C)C)c1cc(SC)nc(SC)c1

Basic Information

ChEMBL ID CHEMBL4642317
Phase Preclinical
Structure Type MOL
InChI Key OGBRFKMQZAEOTG-GRKNLSHJSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

588.8
MW (Da)
5.65
ALogP
10
HBA
1
HBD
100.7
PSA (Ų)
0.23
QED
2
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H32N4O4S2
MW 588.76
Aromatic Rings 4
Heavy Atoms 41
NP-Likeness -0.55

Activity Summary

IC50 1 meas. best 5.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.23 5.23 5900.0 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 = 5900.0 nM 5.23 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