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Compound Detail

CHEMBL4634074

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COc1cc([C@](O)(CCN(C)C)[C@@H](c2cc3cc(C#N)ccc3nc2OC)c2ccnc(OC)c2OC)cc(OC(F)F)n1

Basic Information

ChEMBL ID CHEMBL4634074
Phase Preclinical
Structure Type MOL
InChI Key OTJHOGVUZJKCQX-MXBOTTGLSA-N
1
Targets
1
Activities
1
Assay Types
3
PK Parameters
4
Publications
0
Known Names

Molecular Properties

609.6
MW (Da)
4.50
ALogP
11
HBA
1
HBD
132.1
PSA (Ų)
0.23
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 C31H33F2N5O6
MW 609.63
Aromatic Rings 4
Heavy Atoms 44
NP-Likeness -0.81

Activity Summary

IC50 1 meas. best 5.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Voltage-gated inwardly rectifying potassium channel KCNH2
CHEMBL240
IC50 5.16 5.16 7000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 3000.0 ng.hr.mL-1 Mus musculus
CL 24.0 mL.min-1.kg-1 Mus musculus
F 43.0 % 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 = 7000.0 nM 5.16 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