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Compound Detail

CHEMBL4088718

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S=C(NCc1ccccc1)Nc1ccc2ncnc(Nc3cccc(Br)c3)c2c1

Basic Information

ChEMBL ID CHEMBL4088718
Phase Preclinical
Structure Type MOL
InChI Key YVUKGISJTJAKGC-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

464.4
MW (Da)
5.62
ALogP
4
HBA
3
HBD
61.9
PSA (Ų)
0.33
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H18BrN5S
MW 464.39
Aromatic Rings 4
Heavy Atoms 29
NP-Likeness -1.82

Activity Summary

IC50 4 meas. best 7.76

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 7.76 7.76 17.2 2
Nuclear factor NF-kappa-B complex
CHEMBL2094258
IC50 5.39 5.39 4100.0 1
Unchecked
CHEMBL612545
IC50 5.39 5.39 4100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
28291344 10.1021/acs.jmedchem.6b01774 Epidermal growth factor receptor 2
28291344 10.1021/acs.jmedchem.6b01774 Unchecked 2
28291344 10.1021/acs.jmedchem.6b01774 Receptor-interacting serine/threonine-protein kinase 2 2
28291344 10.1021/acs.jmedchem.6b01774 Inhibitor of nuclear factor kappa-B kinase subunit alpha 1
28291344 10.1021/acs.jmedchem.6b01774 Inhibitor of nuclear factor kappa-B kinase subunit beta 1
28291344 10.1021/acs.jmedchem.6b01774 Protein kinase C iota type 1
28291344 10.1021/acs.jmedchem.6b01774 Protein kinase C zeta type 1
28291344 10.1021/acs.jmedchem.6b01774 Mitogen-activated protein kinase 14 1
28291344 10.1021/acs.jmedchem.6b01774 Mitogen-activated protein kinase kinase kinase 7 1
28291344 10.1021/acs.jmedchem.6b01774 Serine/threonine-protein kinase TBK1 1
28291344 10.1021/acs.jmedchem.6b01774 MDA-MB-231 1
35311289 10.1021/acs.jmedchem.1c01714 Epidermal growth factor receptor 1
35311289 10.1021/acs.jmedchem.1c01714 Nuclear factor NF-kappa-B complex 1

Data from ChEMBL 36 via Core Engine