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Compound Detail

CHEMBL451892

ECTEINASCIDIN 786
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COc1cc2c(cc1O)CCN[C@]21C[S+]([O-])[C@@H]2c3c(OC(C)=O)c(C)c4c(c3[C@H](COC1=O)N1[C@@H]2[C@@H]2c3c(cc(C)c(OC)c3O)C[C@@H]([C@@H]1C#N)N2C)OCO4

Basic Information

ChEMBL ID CHEMBL451892
Name ECTEINASCIDIN 786
Phase Preclinical
Structure Type MOL
InChI Key RRCYSJADSSZEAZ-GEFZJANUSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

786.9
MW (Da)
3.00
ALogP
15
HBA
3
HBD
195.3
PSA (Ų)
0.20
QED
2
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C40H42N4O11S
MW 786.86
Aromatic Rings 3
Heavy Atoms 56
NP-Likeness 1.33

Activity Summary

IC50 2 meas. best 9.82

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
KB
CHEMBL398
IC50 9.82 9.82 0.1 1
NON-PROTEIN TARGET
CHEMBL3879801
IC50 8.12 8.12 7.6 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
KB IC50 = 0.15 nM 9.82 Cytotoxicity against human KB cells 12088444
NON-PROTEIN TARGET IC50 = 7.6 nM 8.12 Cytotoxicity against breast cancer cells 12088444

Literature References

PubMed DOI Target Context # Activities
12088444 10.1021/np010485k NON-PROTEIN TARGET 1
12088444 10.1021/np010485k KB 1
12088444 10.1021/np010485k Mycobacterium tuberculosis 1

Data from ChEMBL 36 via Core Engine