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Compound Detail

CHEMBL436605

ANTIMYCIN A3
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CCCC[C@H]1C(=O)O[C@H](C)[C@H](NC(=O)c2cccc(NC=O)c2O)C(=O)O[C@@H](C)[C@@H]1OC(=O)CC(C)C

Basic Information

ChEMBL ID CHEMBL436605
Name ANTIMYCIN A3
Phase Preclinical
Structure Type MOL
InChI Key PVEVXUMVNWSNIG-PDPGNHKXSA-N
1
Targets
5
Activities
2
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

520.6
MW (Da)
2.70
ALogP
9
HBA
3
HBD
157.3
PSA (Ų)
0.18
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C26H36N2O9
MW 520.58
Aromatic Rings 1
Heavy Atoms 37
NP-Likeness 0.93

Activity Summary

Ki 4 meas. best 6.08
IC50 1 meas. best 5.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Apoptosis regulator Bcl-2
CHEMBL4860
Ki 6.08 6.08 831.8 1
Apoptosis regulator Bcl-2
CHEMBL4860
IC50 5.7 5.7 2000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Apoptosis regulator Bcl-2 Ki = 831.76 nM 6.08 Binding affinity to BCL2 18040043
Apoptosis regulator Bcl-2 IC50 = 2000.0 nM 5.7 Inhibitory activity against Bcl-2 11728179

Literature References

PubMed DOI Target Context # Activities
15808458 10.1016/j.bmcl.2005.02.065 Saccharomyces cerevisiae 4
20621723 10.1016/j.bmcl.2010.05.104 Escherichia coli 2
20621723 10.1016/j.bmcl.2010.05.104 Bacillus subtilis 2
20621723 10.1016/j.bmcl.2010.05.104 Staphylococcus aureus 2
20621723 10.1016/j.bmcl.2010.05.104 Candida albicans 2
30417645 10.1021/acs.jnatprod.8b00559 RBL-2H3 2
11728179 10.1021/jm010016f Apoptosis regulator Bcl-2 1
16564168 10.1016/j.bmcl.2006.03.023 Rhodotorula mucilaginosa 1
16564168 10.1016/j.bmcl.2006.03.023 Bos taurus 1
17227711 10.1016/j.bmc.2006.12.020 Apoptosis regulator Bcl-2 1
17227711 10.1016/j.bmc.2006.12.020 Unchecked 1
17227711 10.1016/j.bmc.2006.12.020 Bcl-2-like protein 2 1
18040043 10.1073/pnas.0709443104 Apoptosis regulator Bcl-2 1
16124766 10.1021/np050145p Candida albicans 1
16124766 10.1021/np050145p Parastagonospora nodorum 1

Data from ChEMBL 36 via Core Engine