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Compound Detail

CHEMBL1642562

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CCNc1nc2sc(-c3cccc([C@H](C)NC(=O)c4cc(C)on4)c3)nc2c2c1ncn2C

Basic Information

ChEMBL ID CHEMBL1642562
Phase Preclinical
Structure Type MOL
InChI Key LKTZHFSCSYUAPA-ZDUSSCGKSA-N
2
Targets
2
Activities
1
Assay Types
2
PK Parameters
3
Publications
0
Known Names

Molecular Properties

461.6
MW (Da)
4.46
ALogP
9
HBA
2
HBD
110.8
PSA (Ų)
0.38
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H23N7O2S
MW 461.55
Aromatic Rings 5
Heavy Atoms 33
NP-Likeness -1.67

Activity Summary

IC50 2 meas. best 7.11

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inhibitor of nuclear factor kappa-B kinase subunit beta
CHEMBL1991
IC50 7.11 7.11 78.0 1
PBMC
CHEMBL613107
IC50 6.03 6.03 940.0 1

Pharmacokinetic Data

Parameter Value Units Species
CL 2.8 mL.min-1.kg-1 Rattus norvegicus
T1/2 2.8 hr Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
21087862 10.1016/j.bmcl.2010.10.133 Rattus norvegicus 2
21087862 10.1016/j.bmcl.2010.10.133 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
21087862 10.1016/j.bmcl.2010.10.133 PBMC 1

Data from ChEMBL 36 via Core Engine