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Compound Detail

CHEMBL5077301

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COc1cc2c(cc1OC)CN(CCc1ccc(-n3nnc(-c4cc(OC)c(OC)cc4NC(=O)c4cc(=O)c5cc(-n6ccnc6)ccc5o4)n3)cc1)CC2

Basic Information

ChEMBL ID CHEMBL5077301
Phase Preclinical
Structure Type MOL
InChI Key POILDAQOHMNGEW-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

754.8
MW (Da)
5.51
ALogP
14
HBA
1
HBD
160.9
PSA (Ų)
0.17
QED
3
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C41H38N8O7
MW 754.80
Aromatic Rings 7
Heavy Atoms 56
NP-Likeness -1.16

Activity Summary

IC50 1 meas. best 5.48

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cytochrome P450 3A4
CHEMBL340
IC50 5.48 5.48 3341.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Cytochrome P450 3A4 IC50 = 3341.0 nM 5.48 Inhibition of CYP3A4 in human liver microsomes using IPA as substrate preincubat... 34928144

Literature References

PubMed DOI Target Context # Activities
34928144 10.1021/acs.jmedchem.1c01272 MES-SA/Dx5 1
34928144 10.1021/acs.jmedchem.1c01272 Cytochrome P450 3A4 1
34928144 10.1021/acs.jmedchem.1c01272 ATP-dependent translocase ABCB1 1

Data from ChEMBL 36 via Core Engine