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Compound Detail

CHEMBL402370

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O=C(Cc1ccc(Br)cc1)Nc1n[nH]c2ccc(N3CCCS3(=O)=O)cc12

Basic Information

ChEMBL ID CHEMBL402370
Phase Preclinical
Structure Type MOL
InChI Key WSNJGDJRGNRVDV-UHFFFAOYSA-N
7
Targets
7
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

449.3
MW (Da)
3.05
ALogP
4
HBA
2
HBD
95.2
PSA (Ų)
0.64
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H17BrN4O3S
MW 449.33
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -2.08

Activity Summary

IC50 7 meas. best 8.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2
CHEMBL301
IC50 8.15 8.15 7.0 1
Cyclin-dependent kinase 1
CHEMBL308
IC50 7.66 7.66 22.0 1
HCT-116
CHEMBL394
IC50 5.85 5.85 1400.0 1
EJ
CHEMBL614292
IC50 5.8 5.8 1570.0 1
Cyclin-dependent kinase 4
CHEMBL331
IC50 5.7 5.7 2000.0 1
SW-620
CHEMBL612262
IC50 5.7 5.7 2000.0 1
A549
CHEMBL392
IC50 5.41 5.41 3870.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18353638 10.1016/j.bmcl.2008.03.002 Cyclin-dependent kinase 2 1
18353638 10.1016/j.bmcl.2008.03.002 Cyclin-dependent kinase 4 1
18353638 10.1016/j.bmcl.2008.03.002 Cyclin-dependent kinase 1 1
18353638 10.1016/j.bmcl.2008.03.002 EJ 1
18353638 10.1016/j.bmcl.2008.03.002 HCT-116 1
18353638 10.1016/j.bmcl.2008.03.002 A549 1
18353638 10.1016/j.bmcl.2008.03.002 SW-620 1
18353638 10.1016/j.bmcl.2008.03.002 Unchecked 1

Data from ChEMBL 36 via Core Engine