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Compound Detail

CHEMBL1714813

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COc1cc2ncnc(N[C@H](C)c3ccccc3)c2cc1OC

Basic Information

ChEMBL ID CHEMBL1714813
Phase Preclinical
Structure Type MOL
InChI Key RJFMUYZWDLSYSX-GFCCVEGCSA-N
4
Targets
6
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

309.4
MW (Da)
3.82
ALogP
5
HBA
1
HBD
56.3
PSA (Ų)
0.78
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H19N3O2
MW 309.37
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -0.86

Activity Summary

IC50 4 meas. best 9.0
Kd 2 meas. best 8.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 9.0 9.0 1.0 1
Son of sevenless homolog 1
CHEMBL2079846
Kd 8.01 7.265 9.7 2
SOS1-KRAS
CHEMBL5465393
IC50 5.98 5.9 1050.0 2
Unchecked
CHEMBL612545
IC50 5.8 5.8 1600.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
33719426 10.1021/acs.jmedchem.0c01949 SOS1-KRAS 1
33719426 10.1021/acs.jmedchem.0c01949 Son of sevenless homolog 1 1
33719426 10.1021/acs.jmedchem.0c01949 Epidermal growth factor receptor 1
34520956 10.1016/j.ejmech.2021.113816 Unchecked 1
38430853 10.1016/j.ejmech.2024.116282 SOS1-KRAS 1
38430853 10.1016/j.ejmech.2024.116282 Son of sevenless homolog 1 1

Data from ChEMBL 36 via Core Engine