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Compound Detail

CHEMBL372736

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COc1cc(Nc2nccc(-c3cc4ccccc4s3)n2)ccc1C(=O)N1CCC(N2CCCC2)CC1

Basic Information

ChEMBL ID CHEMBL372736
Phase Preclinical
Structure Type MOL
InChI Key MRDGEZUUEBHTNO-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

513.7
MW (Da)
5.81
ALogP
7
HBA
1
HBD
70.6
PSA (Ų)
0.35
QED
2
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H31N5O2S
MW 513.67
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.51

Activity Summary

IC50 4 meas. best 7.3

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Inhibitor of nuclear factor kappa-B kinase subunit beta
CHEMBL1991
IC50 7.3 7.3 50.0 2
Inhibitor of nuclear factor kappa-B kinase subunit alpha
CHEMBL3476
IC50 7.0 7.0 100.0 1
Inhibitor of NF-kappa-B kinase (IKK)
CHEMBL2111328
IC50 6.82 6.82 150.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
16236504 10.1016/j.bmcl.2005.09.035 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
16236504 10.1016/j.bmcl.2005.09.035 Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
16236504 10.1016/j.bmcl.2005.09.035 Inhibitor of NF-kappa-B kinase (IKK) 1
23501112 10.1016/j.ejmech.2013.01.045 Inhibitor of nuclear factor kappa-B kinase subunit beta 1

Data from ChEMBL 36 via Core Engine