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Compound Detail

CHEMBL5203778

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CC(=O)N1CCc2c(c(N3CCCc4cc(-c5cnn(C)c5)c(C(F)F)cc43)nn2C2CCN(CCN3CCN(C#Cc4ccc5c(c4)n(C)c(=O)n5C4CCC(=O)NC4=O)CC3)CC2)C1

Basic Information

ChEMBL ID CHEMBL5203778
Phase Preclinical
Structure Type MOL
InChI Key JBIUUNPPXNOOOY-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

903.0
MW (Da)
4.10
ALogP
14
HBA
1
HBD
142.0
PSA (Ų)
0.18
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C48H56F2N12O4
MW 903.05
Aromatic Rings 5
Heavy Atoms 66
NP-Likeness -1.16

Activity Summary

IC50 1 meas. best 10.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
LNCaP
CHEMBL612518
IC50 10.0 10.0 0.1 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
LNCaP IC50 = 0.1 nM 10.0 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