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Compound Detail

CHEMBL5560022

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C=C[C@]1(C)C[C@@H](OC(=O)Cn2cc(-c3ccc([C@@H](C)n4cnc5c(N)ncnc54)cc3)nn2)[C@]2(C)[C@H](C)CC[C@]3(CCC(=O)[C@H]32)[C@@H](C)[C@@H]1O

Basic Information

ChEMBL ID CHEMBL5560022
Phase Preclinical
Structure Type MOL
InChI Key DBNFTNZJEJURQM-QXKOUWKMSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

666.8
MW (Da)
5.18
ALogP
12
HBA
2
HBD
163.9
PSA (Ų)
0.20
QED
3
Ro5 Violations
7
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H46N8O4
MW 666.83
Aromatic Rings 4
Heavy Atoms 49
NP-Likeness 0.59

Activity Summary

IC50 1 meas. best 4.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 4.3 4.3 50000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 50000.0 nM 4.3 Inhibition of P-gp efflux in MDCKII-MDR1 cells using calcein-AM as substrate ass... 38385364

Literature References

PubMed DOI Target Context # Activities
38385364 10.1021/acs.jmedchem.3c02153 Enterococcus faecium 2
38385364 10.1021/acs.jmedchem.3c02153 No relevant target 1
38385364 10.1021/acs.jmedchem.3c02153 Unchecked 1
38385364 10.1021/acs.jmedchem.3c02153 Staphylococcus aureus 1
38385364 10.1021/acs.jmedchem.3c02153 Streptococcus pneumoniae 1
38385364 10.1021/acs.jmedchem.3c02153 Enterococcus faecalis 1

Data from ChEMBL 36 via Core Engine