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Compound Detail

CHEMBL3220312

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Cc1c(Cl)ccc2c(/C=C3\NC(=O)N(C(C(=O)NC(CO)CO)c4ccc(F)c(F)c4)C3=O)c[nH]c12

Basic Information

ChEMBL ID CHEMBL3220312
Phase Preclinical
Structure Type MOL
InChI Key ZFYQBPVMECJUBO-GXHLCREISA-N
13
Targets
19
Activities
1
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

518.9
MW (Da)
2.51
ALogP
5
HBA
5
HBD
134.8
PSA (Ų)
0.24
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H21ClF2N4O5
MW 518.90
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -0.87

Activity Summary

IC50 19 meas. best 7.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Protein Mdm4
CHEMBL1255126
IC50 7.77 7.6475 17.0 4
E3 ubiquitin-protein ligase Mdm2
CHEMBL5023
IC50 7.77 7.7475 17.0 4
Tumour suppressor p53/oncoprotein Mdm2
CHEMBL1907611
IC50 7.76 7.76 17.3 1
Tumour suppressor protein p53/Mdm4
CHEMBL2221344
IC50 7.61 7.61 24.7 1
LNCaP
CHEMBL612518
IC50 5.96 5.96 1100.0 1
LAPC4
CHEMBL613292
IC50 5.92 5.92 1200.0 1
LNCaP C4-2
CHEMBL4296460
IC50 5.77 5.77 1700.0 1
HCT-116
CHEMBL394
IC50 5.52 5.52 3000.0 1
RKO
CHEMBL614879
IC50 5.5 5.5 3200.0 1
MCF7
CHEMBL387
IC50 5.46 5.46 3500.0 1
MDA-MB-435
CHEMBL614697
IC50 4.6 4.6 25300.0 1
PC-3
CHEMBL390
IC50 4.34 4.34 45300.0 1
DU-145
CHEMBL613508
IC50 4.34 4.34 45500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Protein Mdm4 IC50 = 17.0 nM 7.77 Inhibition of MDMX (unknown origin) 39185935
E3 ubiquitin-protein ligase Mdm2 IC50 = 17.0 nM 7.77 Inhibition of GST-tagged MDM2/biotinylated p53 peptide interaction (unknown orig... 24078862
Tumour suppressor p53/oncoprotein Mdm2 IC50 = 17.3 nM 7.76 Inhibition of GST-tagged MDM2/Biotin-tagged p53 interaction (unknown origin) inc... 35420431
E3 ubiquitin-protein ligase Mdm2 IC50 = 17.3 nM 7.76 Inhibition of human MDM2 34286973
E3 ubiquitin-protein ligase Mdm2 IC50 = 17.3 nM 7.76 Inhibition of MDM2 (unknown origin) by TR-FRET assay 38062557
E3 ubiquitin-protein ligase Mdm2 IC50 = 20.0 nM 7.7 Inhibition of MDM2 (unknown origin) 39185935
Tumour suppressor protein p53/Mdm4 IC50 = 24.7 nM 7.61 Inhibition of GST-tagged MDM4/Biotin-tagged p53 interaction (unknown origin) inc... 35420431
Protein Mdm4 IC50 = 24.7 nM 7.61 Inhibition of human MDM4 34286973
Protein Mdm4 IC50 = 24.7 nM 7.61 Inhibition of MDM4 (unknown origin) by TR-FRET assay 38062557
Protein Mdm4 IC50 = 25.0 nM 7.6 Inhibition of GST-tagged MDMX/biotinylated p53 peptide interaction (unknown orig... 24078862
LNCaP IC50 = 1100.0 nM 5.96 Antiproliferative activity against human LNCaP cells assessed as reduction in ce... 39185935
LAPC4 IC50 = 1200.0 nM 5.92 Antiproliferative activity against human LAPC4 cells assessed as reduction in ce... 39185935
LNCaP C4-2 IC50 = 1700.0 nM 5.77 Antiproliferative activity against human C4-2 cells assessed as reduction in cel... 39185935
HCT-116 IC50 = 3000.0 nM 5.52 Antiproliferative activity against human HCT-116 cells assessed as reduction in ... 39185935
RKO IC50 = 3200.0 nM 5.5 Antiproliferative activity against human RKO cells assessed as reduction in cell... 39185935
MCF7 IC50 = 3500.0 nM 5.46 Antiproliferative activity against human MCF7 cells assessed as reduction in cel... 39185935
MDA-MB-435 IC50 = 25300.0 nM 4.6 Antiproliferative activity against human MDA-MB-435 cells assessed as reduction ... 39185935
DU-145 IC50 = 45500.0 nM 4.34 Antiproliferative activity against human DU-145 cells assessed as reduction in c... 39185935
PC-3 IC50 = 45300.0 nM 4.34 Antiproliferative activity against human PC-3 cells assessed as reduction in cel... 39185935

Literature References

Data from ChEMBL 36 via Core Engine