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Compound Detail

CHEMBL5175873

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Cc1cc(Nc2ncnc3ccc(NC(=O)/C=C/CN(C)C)cc23)ccc1Oc1cc2nncn2cn1

Basic Information

ChEMBL ID CHEMBL5175873
Phase Preclinical
Structure Type MOL
InChI Key FHOMWNVSSMYQJF-SNAWJCMRSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

495.6
MW (Da)
3.97
ALogP
10
HBA
2
HBD
122.5
PSA (Ų)
0.31
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H25N9O2
MW 495.55
Aromatic Rings 5
Heavy Atoms 37
NP-Likeness -1.44

Activity Summary

IC50 4 meas. best 8.67

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 8.67 8.67 2.1 1
Receptor tyrosine-protein kinase erbB-2
CHEMBL1824
IC50 8.54 8.54 2.9 1
BT-474
CHEMBL614529
IC50 8.09 8.09 8.1 1
NCI-N87
CHEMBL614197
IC50 7.93 7.93 11.7 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
35319895 10.1021/acs.jmedchem.1c00710 Receptor tyrosine-protein kinase erbB-2 1
35319895 10.1021/acs.jmedchem.1c00710 Epidermal growth factor receptor 1
35319895 10.1021/acs.jmedchem.1c00710 Unchecked 1
35319895 10.1021/acs.jmedchem.1c00710 NCI-N87 1
35319895 10.1021/acs.jmedchem.1c00710 BT-474 1

Data from ChEMBL 36 via Core Engine