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Compound Detail

CHEMBL5597724

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COc1cc(N2CCOCC2)c(-c2cnn(C)c2)cc1Nc1ncc(Cl)c(Nc2ccccc2NS(C)(=O)=O)n1

Basic Information

ChEMBL ID CHEMBL5597724
Phase Preclinical
Structure Type MOL
InChI Key KKTDBVXKCUWLIX-UHFFFAOYSA-N
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

585.1
MW (Da)
4.23
ALogP
11
HBA
3
HBD
135.5
PSA (Ų)
0.26
QED
2
Ro5 Violations
9
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H29ClN8O4S
MW 585.09
Aromatic Rings 4
Heavy Atoms 40
NP-Likeness -1.74

Activity Summary

IC50 1 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor
CHEMBL203
IC50 9.7 9.7 0.2 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Epidermal growth factor receptor IC50 = 0.2 nM 9.7 Inhibition of EGFR Del19/T790M/C797S mutant (unknown origin) 39143914

Literature References

PubMed DOI Target Context # Activities
39143914 10.1021/acs.jmedchem.4c00361 Epidermal growth factor receptor 1

Data from ChEMBL 36 via Core Engine