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Compound Detail

CHEMBL5281316

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CC(C)OC(=O)c1ccnc2cc(C(OCCN3CCCCC3)c3cccc(NC(=O)/C=C/CN(C)C)c3)[nH]c12

Basic Information

ChEMBL ID CHEMBL5281316
Phase Preclinical
Structure Type MOL
InChI Key MQPYAXPCLQILKZ-FMIVXFBMSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

547.7
MW (Da)
4.78
ALogP
7
HBA
2
HBD
99.8
PSA (Ų)
0.25
QED
1
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H41N5O4
MW 547.70
Aromatic Rings 3
Heavy Atoms 40
NP-Likeness -0.89

Activity Summary

EC50 1 meas. best 5.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
BT-474
CHEMBL614529
EC50 5.0 5.0 10000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
BT-474 EC50 = 10000.0 nM 5.0 Antiproliferative activity against human BT-474 cells 34555614

Literature References

PubMed DOI Target Context # Activities
34555614 10.1016/j.ejmech.2021.113855 Lysine-specific demethylase 5A 1
34555614 10.1016/j.ejmech.2021.113855 Lysine-specific demethylase 5B 1
34555614 10.1016/j.ejmech.2021.113855 Lysine-specific demethylase 4A 1
34555614 10.1016/j.ejmech.2021.113855 BT-474 1

Data from ChEMBL 36 via Core Engine