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Compound Detail

CHEMBL453250

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O=C(CCCN1CCCC1)Nc1ccc(NC(=O)c2cccc(NC(=O)Nc3cccc(C(=O)Nc4ccc(NC(=O)CCCN5CCCC5)cc4)c3)c2)cc1

Basic Information

ChEMBL ID CHEMBL453250
Phase Preclinical
Structure Type MOL
InChI Key MELQUPKZQBLZKT-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
5
PK Parameters
5
Publications
0
Known Names

Molecular Properties

758.9
MW (Da)
7.46
ALogP
7
HBA
6
HBD
164.0
PSA (Ų)
0.07
QED
3
Ro5 Violations
16
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C43H50N8O5
MW 758.92
Aromatic Rings 4
Heavy Atoms 56
NP-Likeness -0.90

Activity Summary

IC50 1 meas. best 4.96

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
MCF7
CHEMBL387
IC50 4.96 4.96 11100.0 1

Pharmacokinetic Data

Parameter Value Units Species
KA 0.4 10'6/M Homo sapiens
KA 0.4 10'6/M -
KA 3.1 10'6/M -
KA 0.9 10'6/M -
KA 1.0 10'3/M -

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
MCF7 IC50 = 11100.0 nM 4.96 Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay 19053833

Literature References

PubMed DOI Target Context # Activities
19053833 10.1021/jm801245v Unchecked 14
19053833 10.1021/jm801245v MCF7 6
19053833 10.1021/jm801245v A549 2
19053833 10.1021/jm801245v Telomerase reverse transcriptase 2
19053833 10.1021/jm801245v ADMET 1

Data from ChEMBL 36 via Core Engine