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Compound Detail

CHEMBL1203026

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COc1cc2ncc(C#N)c(Nc3cccc(SC)c3)c2cc1OC.Cl

Basic Information

ChEMBL ID CHEMBL1203026
Phase Preclinical
Structure Type MOL
InChI Key DDLVKNCHMPSZAJ-UHFFFAOYSA-N
Parent Compound CHEMBL114496
Active Moiety CHEMBL114496
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

351.4
MW (Da)
4.59
ALogP
6
HBA
1
HBD
67.2
PSA (Ų)
0.68
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 C19H18ClN3O2S
MW 387.89
Aromatic Rings 3
Heavy Atoms 25
NP-Likeness -1.38

Activity Summary

IC50 4 meas. best 6.12

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Epidermal growth factor receptor and ErbB2 (HER1 and HER2)
CHEMBL2111431
IC50 6.12 6.12 760.0 1
A-431
CHEMBL614069
IC50 5.84 5.84 1451.0 1
SK-BR-3
CHEMBL613834
IC50 5.81 5.81 1540.0 1
SW-620
CHEMBL612262
IC50 5.3 5.3 4980.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10966743 10.1021/jm000206a Epidermal growth factor receptor and ErbB2 (HER1 and HER2) 1
10966743 10.1021/jm000206a A-431 1
10966743 10.1021/jm000206a SK-BR-3 1
10966743 10.1021/jm000206a SW-620 1

Data from ChEMBL 36 via Core Engine