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Compound Detail

CHEMBL4591383

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CSc1ncnc2c1c1occc1n2[C@@H]1O[C@H](CO)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL4591383
Phase Preclinical
Structure Type MOL
InChI Key SWQLIPCORWXTQV-AKAIJSEGSA-N
13
Targets
16
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

337.4
MW (Da)
0.51
ALogP
9
HBA
3
HBD
113.8
PSA (Ų)
0.47
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C14H15N3O5S
MW 337.36
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness 0.50

Activity Summary

IC50 14 meas. best 6.85
EC50 2 meas. best 6.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CCRF-CEM
CHEMBL382
IC50 6.85 6.85 140.0 1
OCI-AML2
CHEMBL2366220
IC50 6.72 6.72 190.0 1
HCT-116
CHEMBL394
IC50 6.68 6.67 210.0 2
Hepatitis C virus
CHEMBL379
EC50 6.62 6.585 240.0 2
K562
CHEMBL385
IC50 6.57 6.57 270.0 1
HL-60
CHEMBL383
IC50 6.54 6.54 290.0 1
U2OS
CHEMBL615023
IC50 6.47 6.47 340.0 1
BJ
CHEMBL614358
IC50 6.31 6.31 490.0 1
HepG2
CHEMBL395
IC50 5.7 5.7 2010.0 1
Unchecked
CHEMBL612545
IC50 5.57 5.41 2700.0 2
HeLa S3
CHEMBL4296436
IC50 5.53 5.53 2960.0 1
A549
CHEMBL392
IC50 5.31 5.31 4860.0 1
MRC5
CHEMBL614181
IC50 5.03 5.03 9370.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
CCRF-CEM IC50 = 140.0 nM 6.85 Antiproliferative activity against human CCRF-CEM cells after 3 days by MTS assa... 30281308
OCI-AML2 IC50 = 190.0 nM 6.72 Mitochondrial toxicity in human OCI-AML2 cells assessed as reduction in oxidativ... 30281308
HCT-116 IC50 = 210.0 nM 6.68 Antiproliferative activity against p53 gene knocked out human HCT116 cells after... 30281308
HCT-116 IC50 = 220.0 nM 6.66 Antiproliferative activity against human HCT116 cells after 3 days by MTS assay 30281308
Hepatitis C virus EC50 = 240.0 nM 6.62 Antiviral activity against Hepatitis C virus genotype 2a infected in human Huh-l... 30281308
K562 IC50 = 270.0 nM 6.57 Antiproliferative activity against human K562 cells after 3 days by MTS assay 30281308
Hepatitis C virus EC50 = 280.0 nM 6.55 Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh-l... 30281308
HL-60 IC50 = 290.0 nM 6.54 Antiproliferative activity against human HL60 cells after 72 hrs by XTT assay 30281308
U2OS IC50 = 340.0 nM 6.47 Antiproliferative activity against human U2OS cells after 3 days by MTS assay 30281308
BJ IC50 = 490.0 nM 6.31 Antiproliferative activity against human BJ cells after 3 days by MTS assay 30281308
HepG2 IC50 = 2010.0 nM 5.7 Antiproliferative activity against human HepG2 cells after 72 hrs by XTT assay 30281308
Unchecked IC50 = 2700.0 nM 5.57 Antiproliferative activity against human K562-TAX cells after 3 days by MTS assa... 30281308
HeLa S3 IC50 = 2960.0 nM 5.53 Antiproliferative activity against human HeLaS3 cells after 72 hrs by XTT assay 30281308
A549 IC50 = 4860.0 nM 5.31 Antiproliferative activity against human A549 cells after 3 days by MTS assay 30281308
Unchecked IC50 = 5570.0 nM 5.25 Antiproliferative activity against human CEM-DNR-bulk cells after 3 days by MTS ... 30281308
MRC5 IC50 = 9370.0 nM 5.03 Antiproliferative activity against human MRC5 cells after 3 days by MTS assay 30281308

Literature References

Data from ChEMBL 36 via Core Engine