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Compound Detail

CHEMBL395358

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Cc1ccc(O)cc1Nc1ccnc2cc(-c3ccccn3)ccc12

Basic Information

ChEMBL ID CHEMBL395358
Phase Preclinical
Structure Type MOL
InChI Key BKDBTNDUTIFYHL-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

327.4
MW (Da)
5.05
ALogP
4
HBA
2
HBD
58.0
PSA (Ų)
0.55
QED
1
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H17N3O
MW 327.39
Aromatic Rings 4
Heavy Atoms 25
NP-Likeness -0.80

Activity Summary

IC50 2 meas. best 7.13
EC50 1 meas. best 7.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-interacting serine/threonine-protein kinase 3
CHEMBL1795199
EC50 7.13 7.13 73.6 1
Receptor-interacting serine/threonine-protein kinase 1
CHEMBL5464
IC50 7.13 7.13 73.6 1
Proto-oncogene tyrosine-protein kinase receptor Ret
CHEMBL2041
IC50 7.12 7.12 75.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17884497 10.1016/j.bmcl.2007.07.104 Proto-oncogene tyrosine-protein kinase receptor Ret 1
31622096 10.1021/acs.jmedchem.9b01317 Receptor-interacting serine/threonine-protein kinase 1 1
36781172 10.1021/acs.jmedchem.2c01621 Receptor-interacting serine/threonine-protein kinase 3 1

Data from ChEMBL 36 via Core Engine