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Compound Detail

CHEMBL1092943

PLATENCIN
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C=C1C[C@@]23C=CC(=O)[C@@](C)(CCC(=O)Nc4c(O)ccc(C(=O)O)c4O)[C@@H]2C[C@@H]1CC3

Basic Information

ChEMBL ID CHEMBL1092943
Name PLATENCIN
Phase Preclinical
Structure Type MOL
InChI Key DWUHGPPFFABTIY-RLWZQHMASA-N
3
Targets
11
Activities
2
Assay Types
9
PK Parameters
20
Publications
0
Known Names

Molecular Properties

425.5
MW (Da)
4.02
ALogP
5
HBA
4
HBD
123.9
PSA (Ų)
0.42
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C24H27NO6
MW 425.48
Aromatic Rings 1
Heavy Atoms 31
NP-Likeness 2.41

Activity Summary

IC50 10 meas. best 6.95
Kd 1 meas. best 7.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Kd 7.76 7.76 17.3 1
Unchecked
CHEMBL612545
IC50 6.95 5.5613 113.0 8
3-oxoacyl-[acyl-carrier-protein] synthase 2
CHEMBL5341
IC50 5.34 5.34 4580.0 1
HeLa
CHEMBL399
IC50 4.07 4.07 86000.0 1

Pharmacokinetic Data

Parameter Value Units Species
AUC 2893.26 ng.hr.mL-1 Mus musculus
AUC 978.6 ng.hr.mL-1 Mus musculus
CL 23.0 mL.min-1.kg-1 Mus musculus
Cmax 11000.0 nM Mus musculus
Cmax 4000.0 nM Mus musculus
F 10.0 % Mus musculus
T1/2 0.22 hr Mus musculus
T1/2 1.3 hr Mus musculus
Vd 0.46 L.kg-1 Mus musculus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29389125 10.1021/acs.jnatprod.7b00745 Staphylococcus aureus 12
33738071 10.1021/acsmedchemlett.0c00653 Unchecked 10
17456595 10.1073/pnas.0700746104 Staphylococcus aureus 9
28237556 10.1016/j.bmc.2017.02.028 ADMET 9
28237556 10.1016/j.bmc.2017.02.028 Mus musculus 9
- 10.1039/C3MD00016H Mycolicibacterium smegmatis 8
- 10.1039/C3MD00016H Mycobacterium tuberculosis 8
33738071 10.1021/acsmedchemlett.0c00653 Staphylococcus aureus 7
33538159 10.1021/acs.jmedchem.0c02185 Staphylococcus aureus 5
17456595 10.1073/pnas.0700746104 Unchecked 4
30108968 10.1039/C8MD00081F Staphylococcus aureus 3
20299229 10.1016/j.bmc.2010.02.030 Staphylococcus aureus 3
28237556 10.1016/j.bmc.2017.02.028 Plasma 2
19581087 10.1016/j.bmcl.2009.06.061 Unchecked 2
28237556 10.1016/j.bmc.2017.02.028 Lung 2
20299229 10.1016/j.bmc.2010.02.030 Escherichia coli 2
28237556 10.1016/j.bmc.2017.02.028 Liver 2
17456595 10.1073/pnas.0700746104 Escherichia coli 2
28237556 10.1016/j.bmc.2017.02.028 Kidney 2
17456595 10.1073/pnas.0700746104 Streptococcus pneumoniae 2

Data from ChEMBL 36 via Core Engine