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Compound Detail

CHEMBL4471189

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COc1cc2c(cc1OCCCC(=O)Nc1cn(C)c(C(=O)Nc3ccc(-c4cc(C(=O)NCC(C)(C)SSC)n(C)c4)cc3)n1)N=C[C@@H]1Cc3ccccc3CN1C2=O

Basic Information

ChEMBL ID CHEMBL4471189
Phase Preclinical
Structure Type MOL
InChI Key LTKJEPQKLCEJLH-YTTGMZPUSA-N
1
Targets
3
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

849.0
MW (Da)
7.29
ALogP
12
HBA
3
HBD
161.2
PSA (Ų)
0.07
QED
3
Ro5 Violations
15
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C44H48N8O6S2
MW 849.05
Aromatic Rings 5
Heavy Atoms 60
NP-Likeness -0.46

Activity Summary

IC50 3 meas. best 11.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 11.0 11.0 0.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked IC50 = 0.01 nM 11.0 Cytotoxicity against human NCI-H2110 cells assessed as reduction in cell viabili... 31350125

Literature References

PubMed DOI Target Context # Activities
31350125 10.1016/j.bmcl.2019.07.031 KB 1
31350125 10.1016/j.bmcl.2019.07.031 Unchecked 1
31350125 10.1016/j.bmcl.2019.07.031 NAMALVA 1

Data from ChEMBL 36 via Core Engine