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Compound Detail

CHEMBL2017007

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CCCCCCNc1ncnc2c1ncn2[C@@H]1O[C@H](COS(N)(=O)=O)[C@@H](O)[C@H]1O

Basic Information

ChEMBL ID CHEMBL2017007
Phase Preclinical
Structure Type MOL
InChI Key DWCQACBFXLNZCO-XNIJJKJLSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

430.5
MW (Da)
-0.34
ALogP
11
HBA
4
HBD
174.7
PSA (Ų)
0.36
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H26N6O6S
MW 430.49
Aromatic Rings 2
Heavy Atoms 29
NP-Likeness 0.41

Activity Summary

EC50 1 meas. best 6.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
K562
CHEMBL385
EC50 6.8 6.8 160.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
K562 EC50 = 160.0 nM 6.8 Antiproliferative activity against human K562 cells after 72 hrs by CellTiter-Gl... 24900352

Literature References

PubMed DOI Target Context # Activities
24900352 10.1021/ml2000615 Unchecked 5
24900352 10.1021/ml2000615 SUMO-activating enzyme 1
24900352 10.1021/ml2000615 Ubiquitin-like modifier-activating enzyme 5 1
24900352 10.1021/ml2000615 NEDD8-activating enzyme E1 regulatory subunit 1
24900352 10.1021/ml2000615 NEDD8-activating enzyme E1 catalytic subunit 1
24900352 10.1021/ml2000615 Tyrosine-protein kinase ABL1 1
24900352 10.1021/ml2000615 Calcium/calmodulin-dependent protein kinase type II subunit beta 1
24900352 10.1021/ml2000615 Cyclin-dependent kinase 1/cyclin B1 1
24900352 10.1021/ml2000615 Death-associated protein kinase 1 1
24900352 10.1021/ml2000615 Epidermal growth factor receptor 1
24900352 10.1021/ml2000615 Insulin-like growth factor 1 receptor 1
24900352 10.1021/ml2000615 Tyrosine-protein kinase JAK1 1
24900352 10.1021/ml2000615 Tyrosine-protein kinase JAK3 1
24900352 10.1021/ml2000615 Dual specificity mitogen-activated protein kinase kinase 1 1
24900352 10.1021/ml2000615 High affinity nerve growth factor receptor 1
24900352 10.1021/ml2000615 K562 1

Data from ChEMBL 36 via Core Engine