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Compound Detail

CHEMBL505589

CYCLOTHEONAMIDE E2
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CC[C@H](C)[C@H]1NC(=O)C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]2CCCN2C(=O)[C@@H](NC(=O)[C@H](C)NC(=O)c2ccccc2)CNC(=O)/C=C/[C@H](Cc2ccc(O)cc2)NC1=O

Basic Information

ChEMBL ID CHEMBL505589
Name CYCLOTHEONAMIDE E2
Phase Preclinical
Structure Type MOL
InChI Key YSNKBNIOHORIHX-MSQPAANESA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

845.0
MW (Da)
-0.75
ALogP
10
HBA
10
HBD
294.1
PSA (Ų)
0.05
QED
2
Ro5 Violations
12
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C42H56N10O9
MW 844.97
Aromatic Rings 2
Heavy Atoms 61
NP-Likeness 0.60

Activity Summary

IC50 2 meas. best 7.89

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Prothrombin
CHEMBL204
IC50 7.89 7.89 13.0 1
Unchecked
CHEMBL612545
IC50 7.26 7.26 55.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Prothrombin IC50 = 13.0 nM 7.89 Inhibition of thrombin 9599274
Unchecked IC50 = 55.0 nM 7.26 Inhibition of trypsin 9599274

Literature References

PubMed DOI Target Context # Activities
9599274 10.1021/np970544n Prothrombin 1
9599274 10.1021/np970544n Unchecked 1

Data from ChEMBL 36 via Core Engine