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Compound Detail

CHEMBL5180617

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CNC(=O)N1CCc2c(c(N3CCCc4cc(-c5cnn(C)c5)c(C(F)F)cc43)nn2C2CCN(C(=O)CCCCCNc3cccc4c3C(=O)N(C3CCC(=O)NC3=O)C4=O)CC2)C1

Basic Information

ChEMBL ID CHEMBL5180617
Phase Preclinical
Structure Type MOL
InChI Key KOXRGDZBEAJAKE-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

894.0
MW (Da)
5.24
ALogP
12
HBA
3
HBD
187.1
PSA (Ų)
0.13
QED
3
Ro5 Violations
12
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C46H53F2N11O6
MW 894.00
Aromatic Rings 4
Heavy Atoms 65
NP-Likeness -1.22

Activity Summary

IC50 1 meas. best 9.4

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
LNCaP
CHEMBL612518
IC50 9.4 9.4 0.4 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
LNCaP IC50 = 0.4 nM 9.4 Antiproliferative activity against human LNCaP cells assessed as reduction in ce... 35978697

Literature References

PubMed DOI Target Context # Activities
35978697 10.1021/acsmedchemlett.2c00317 LNCaP 1
35978697 10.1021/acsmedchemlett.2c00317 Unchecked 1

Data from ChEMBL 36 via Core Engine