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Compound Detail

CHEMBL4165119

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COc1ccc2c(OCc3nnc4sc(-c5cc6ccccc6[nH]5)nn34)ccnc2c1

Basic Information

ChEMBL ID CHEMBL4165119
Phase Preclinical
Structure Type MOL
InChI Key QXHQEQPUACOBBC-UHFFFAOYSA-N
6
Targets
7
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

428.5
MW (Da)
4.47
ALogP
8
HBA
1
HBD
90.2
PSA (Ų)
0.44
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 C22H16N6O2S
MW 428.48
Aromatic Rings 6
Heavy Atoms 31
NP-Likeness -1.68

Activity Summary

IC50 7 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Hepatocyte growth factor receptor
CHEMBL3717
IC50 7.1 6.91 79.3 2
EBC-1
CHEMBL4296411
IC50 6.3 6.3 506.0 1
MKN-45
CHEMBL614354
IC50 5.93 5.93 1171.0 1
NCI-H460
CHEMBL396
IC50 5.69 5.69 2055.0 1
COLO 205
CHEMBL614561
IC50 5.65 5.65 2242.0 1
PC-3
CHEMBL390
IC50 5.53 5.53 2970.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29202410 10.1016/j.ejmech.2017.11.073 Hepatocyte growth factor receptor 1
29202410 10.1016/j.ejmech.2017.11.073 EBC-1 1
29202410 10.1016/j.ejmech.2017.11.073 MKN-45 1
29202410 10.1016/j.ejmech.2017.11.073 NCI-H460 1
29202410 10.1016/j.ejmech.2017.11.073 PC-3 1
29202410 10.1016/j.ejmech.2017.11.073 COLO 205 1
29602036 10.1016/j.ejmech.2018.03.049 Hepatocyte growth factor receptor 1

Data from ChEMBL 36 via Core Engine