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Compound Detail

CHEMBL4750995

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CN[C@@H](C)C(=O)N[C@H](C(=O)N1CCC[C@H]1C(=O)Nc1cc2c(N[C@H]3CC[C@@H](Nc4ncnc5cc(OC)c(NC(=O)[C@@H]6CCCN6C(=O)[C@@H](NC(=O)[C@H](C)NC)C(C)(C)C)cc45)CC3)ncnc2cc1OC)C(C)(C)C

Basic Information

ChEMBL ID CHEMBL4750995
Phase Preclinical
Structure Type MOL
InChI Key YIZXATJRZDXIBK-GGTVZAMOSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

1051.3
MW (Da)

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C54H78N14O8
MW 1051.31

Activity Summary

IC50 2 meas. best 8.23

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MDA-MB-231
CHEMBL400
IC50 8.23 8.23 5.9 1
Cytochrome P450 3A4
CHEMBL340
IC50 5.26 5.26 5530.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MDA-MB-231 IC50 = 5.93 nM 8.23 Cytotoxicity against human MDA-MB-231 cells 33166687
Cytochrome P450 3A4 IC50 = 5530.0 nM 5.26 Inhibition of CYP3A4 (unknown origin) 33166687

Literature References

PubMed DOI Target Context # Activities
33166687 10.1016/j.bmcl.2020.127676 MDA-MB-231 1
33166687 10.1016/j.bmcl.2020.127676 Cytochrome P450 3A4 1

Data from ChEMBL 36 via Core Engine