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Compound Detail

CHEMBL4532596

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Cn1ccc2c1c1c(Cl)ncnc1n2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL4532596
Phase Preclinical
Structure Type MOL
InChI Key DLNOLRJXNFQUKA-FRJWGUMJSA-N
12
Targets
15
Activities
2
Assay Types
0
PK Parameters
19
Publications
0
Known Names

Molecular Properties

338.8
MW (Da)
0.19
ALogP
8
HBA
3
HBD
105.6
PSA (Ų)
0.58
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H15ClN4O4
MW 338.75
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness 0.47

Activity Summary

IC50 13 meas. best 7.22
EC50 2 meas. best 7.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatitis C virus
CHEMBL379
EC50 7.22 6.825 60.0 2
CCRF-CEM
CHEMBL382
IC50 7.22 7.22 60.0 1
HL-60
CHEMBL383
IC50 7.22 7.22 60.0 1
HCT-116
CHEMBL394
IC50 6.82 6.795 150.0 2
HepG2
CHEMBL395
IC50 6.8 6.8 160.0 1
K562
CHEMBL385
IC50 6.75 6.75 180.0 1
HeLa S3
CHEMBL4296436
IC50 6.24 6.24 570.0 1
U2OS
CHEMBL615023
IC50 6.21 6.21 620.0 1
BJ
CHEMBL614358
IC50 5.92 5.92 1200.0 1
A549
CHEMBL392
IC50 5.52 5.52 2990.0 1
Unchecked
CHEMBL612545
IC50 4.3 4.3 50000.0 2
MRC5
CHEMBL614181
IC50 4.3 4.3 50000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Hepatitis C virus EC50 = 60.0 nM 7.22 Antiviral activity against Hepatitis C virus genotype 2a infected in human Huh-l... 30281308
CCRF-CEM IC50 = 60.0 nM 7.22 Antiproliferative activity against human CCRF-CEM cells after 3 days by MTS assa... 30281308
HL-60 IC50 = 60.0 nM 7.22 Antiproliferative activity against human HL60 cells after 72 hrs by XTT assay 30281308
HCT-116 IC50 = 150.0 nM 6.82 Antiproliferative activity against p53 gene knocked out human HCT116 cells after... 30281308
HepG2 IC50 = 160.0 nM 6.8 Antiproliferative activity against human HepG2 cells after 72 hrs by XTT assay 30281308
HCT-116 IC50 = 170.0 nM 6.77 Antiproliferative activity against human HCT116 cells after 3 days by MTS assay 30281308
K562 IC50 = 180.0 nM 6.75 Antiproliferative activity against human K562 cells after 3 days by MTS assay 30281308
Hepatitis C virus EC50 = 370.0 nM 6.43 Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh-l... 30281308
HeLa S3 IC50 = 570.0 nM 6.24 Antiproliferative activity against human HeLaS3 cells after 72 hrs by XTT assay 30281308
U2OS IC50 = 620.0 nM 6.21 Antiproliferative activity against human U2OS cells after 3 days by MTS assay 30281308
BJ IC50 = 1200.0 nM 5.92 Antiproliferative activity against human BJ cells after 3 days by MTS assay 30281308
A549 IC50 = 2990.0 nM 5.52 Antiproliferative activity against human A549 cells after 3 days by MTS assay 30281308
MRC5 IC50 = 50000.0 nM 4.3 Antiproliferative activity against human MRC5 cells after 3 days by MTS assay 30281308
Unchecked IC50 = 50000.0 nM 4.3 Antiproliferative activity against human CEM-DNR-bulk cells after 3 days by MTS ... 30281308
Unchecked IC50 = 50000.0 nM 4.3 Antiproliferative activity against human K562-TAX cells after 3 days by MTS assa... 30281308

Literature References

Data from ChEMBL 36 via Core Engine