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Compound Detail

CHEMBL4561712

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C=C[C@]1(C)C[C@@H](OC(=O)COc2ccc3c(c2C)B(O)N(C(=O)OC)N=C3)[C@]2(C)[C@H](C)CC[C@]3(CCC(=O)[C@H]32)[C@@H](C)[C@@H]1O

Basic Information

ChEMBL ID CHEMBL4561712
Phase Preclinical
Structure Type MOL
InChI Key ACBMXLNSYYMYEV-QOPDXCDOSA-N
1
Targets
1
Activities
1
Assay Types
8
PK Parameters
2
Publications
0
Known Names

Molecular Properties

594.5
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C32H43BN2O8
MW 594.51

Activity Summary

EC50 1 meas. best 7.58

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Wolbachia
CHEMBL4630676
EC50 7.58 7.58 26.1 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 1520.0 ng.hr.mL-1 Mus musculus
AUC 166.0 ng.hr.mL-1 Mus musculus
CL 217.0 mL.min-1.g-1 Mus musculus
CL 54.55 mL.min-1.kg-1 Mus musculus
Cmax 5416.23 nM Mus musculus
Cmax 381.83 nM Mus musculus
F 6.0 % Mus musculus
Fu 0.006 - Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Wolbachia EC50 = 26.1 nM 7.58 Antimicrobial activity against Wolbachia pipientis infected in Asian tiger mosqu... 30730745

Literature References

PubMed DOI Target Context # Activities
30730745 10.1021/acs.jmedchem.8b01854 ADMET 10
30730745 10.1021/acs.jmedchem.8b01854 Wolbachia 2

Data from ChEMBL 36 via Core Engine