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Compound Detail

CHEMBL5572514

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CN(C)C/C=C/C(=O)Nc1ccc2ncnc3c2c1C=CN3c1ccc(OCc2ccccn2)c(Cl)c1

Basic Information

ChEMBL ID CHEMBL5572514
Phase Preclinical
Structure Type MOL
InChI Key NXVZNVMICNOVJM-FNORWQNLSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

513.0
MW (Da)
5.44
ALogP
7
HBA
1
HBD
83.5
PSA (Ų)
0.31
QED
2
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H25ClN6O2
MW 513.00
Aromatic Rings 4
Heavy Atoms 37
NP-Likeness -1.20

Activity Summary

IC50 6 meas. best 9.09

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 9.09 9.09 0.8 1
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 8.56 8.56 2.7 1
NCI-N87
CHEMBL614197
IC50 8.1 8.1 7.9 1
BaF3
CHEMBL614524
IC50 8.01 8.01 9.7 1
BT-474
CHEMBL614529
IC50 7.75 7.75 17.9 1
HCC827
CHEMBL4296422
IC50 7.45 7.45 35.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38518121 10.1021/acs.jmedchem.3c02302 Receptor tyrosine-protein kinase erbB-2 1
38518121 10.1021/acs.jmedchem.3c02302 BaF3 1
38518121 10.1021/acs.jmedchem.3c02302 Epidermal growth factor receptor 1
38518121 10.1021/acs.jmedchem.3c02302 HCC827 1
38518121 10.1021/acs.jmedchem.3c02302 BT-474 1
38518121 10.1021/acs.jmedchem.3c02302 NCI-N87 1

Data from ChEMBL 36 via Core Engine