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Compound Detail

CHEMBL4746064

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C=C[C@]1(C)C[C@@H](OC(=O)Cn2cc(-c3ccc(Cn4cnc5c(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 CHEMBL4746064
Phase Preclinical
Structure Type MOL
InChI Key HQIWDRDUCRRUSF-JRXHTQEJSA-N
1
Targets
1
Activities
1
Assay Types
4
PK Parameters
17
Publications
0
Known Names

Molecular Properties

652.8
MW (Da)
4.62
ALogP
12
HBA
2
HBD
163.9
PSA (Ų)
0.21
QED
2
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C36H44N8O4
MW 652.80
Aromatic Rings 4
Heavy Atoms 48
NP-Likeness 0.54

Activity Summary

IC50 1 meas. best 4.44

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 4.44 4.44 36000.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 10000.0 mL.min-1.kg-1 Mus musculus
CL 5084.0 mL.min-1.kg-1 Homo sapiens
T1/2 0.008333 hr Mus musculus
T1/2 0.02 hr Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 36000.0 nM 4.44 Inhibition of P-gp efflux in MDCKII-MDR1 cells using calcein-AM as substrate ass... 38385364

Literature References

PubMed DOI Target Context # Activities
33325700 10.1021/acs.jmedchem.0c01328 Staphylococcus aureus 5
38385364 10.1021/acs.jmedchem.3c02153 ADMET 4
33325700 10.1021/acs.jmedchem.0c01328 Caco-2 3
38385364 10.1021/acs.jmedchem.3c02153 Voltage-gated inwardly rectifying potassium channel KCNH2 2
38385364 10.1021/acs.jmedchem.3c02153 Enterococcus faecium 2
38385364 10.1021/acs.jmedchem.3c02153 Staphylococcus aureus 1
38385364 10.1021/acs.jmedchem.3c02153 Staphylococcus epidermidis 1
38385364 10.1021/acs.jmedchem.3c02153 Listeria 1
38385364 10.1021/acs.jmedchem.3c02153 Escherichia coli 1
38385364 10.1021/acs.jmedchem.3c02153 Enterococcus faecalis 1
38385364 10.1021/acs.jmedchem.3c02153 Streptococcus pneumoniae 1
38385364 10.1021/acs.jmedchem.3c02153 Unchecked 1
38385364 10.1021/acs.jmedchem.3c02153 No relevant target 1
33325700 10.1021/acs.jmedchem.0c01328 Unchecked 1
33325700 10.1021/acs.jmedchem.0c01328 HEK293 1
33325700 10.1021/acs.jmedchem.0c01328 PC-3 1
33325700 10.1021/acs.jmedchem.0c01328 Staphylococcus epidermidis 1

Data from ChEMBL 36 via Core Engine