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Compound Detail

CHEMBL376935

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COc1cc2cc(c1Cl)N(C)C(=O)CC(OC(=O)[C@@H](C)N(C)C(=O)CCCSSC)C1(C)OC1C(C)C1CC(O)(NC(=O)O1)C(OC)/C=C/C=C(\C)C2

Basic Information

ChEMBL ID CHEMBL376935
Phase Preclinical
Structure Type MOL
InChI Key SBWFAIGFKMBQFX-ZKULSESMSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

798.4
MW (Da)
5.31
ALogP
12
HBA
2
HBD
156.5
PSA (Ų)
0.14
QED
3
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C37H52ClN3O10S2
MW 798.42
Aromatic Rings 1
Heavy Atoms 53
NP-Likeness 2.15

Activity Summary

IC50 1 meas. best 8.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
KB
CHEMBL398
IC50 8.7 8.7 2.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
KB IC50 = 2.0 nM 8.7 Cytotoxicity against human KB cell line by clonogenic plating efficiency assay a... 16821799

Literature References

PubMed DOI Target Context # Activities
16821799 10.1021/jm060319f SK-BR-3 1
16821799 10.1021/jm060319f KB 1

Data from ChEMBL 36 via Core Engine