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Compound Detail

CHEMBL4856751

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COc1ccc(Br)cc1C1=C(Nc2cccc(C#N)c2)C(=O)NC1=O

Basic Information

ChEMBL ID CHEMBL4856751
Phase Preclinical
Structure Type MOL
InChI Key PJQXOWLFWLVNJN-UHFFFAOYSA-N
2
Targets
5
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

398.2
MW (Da)
2.81
ALogP
5
HBA
2
HBD
91.2
PSA (Ų)
0.77
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H12BrN3O3
MW 398.22
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -0.79

Activity Summary

IC50 3 meas. best 7.0
Ki 2 meas. best 8.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
STE20-like serine/threonine-protein kinase
CHEMBL4202
Ki 8.01 8.01 9.7 1
Serine/threonine-protein kinase 10
CHEMBL3981
Ki 7.21 7.21 61.0 1
Serine/threonine-protein kinase 10
CHEMBL3981
IC50 7.0 6.175 99.0 2
STE20-like serine/threonine-protein kinase
CHEMBL4202
IC50 4.72 4.72 19000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34463505 10.1021/acs.jmedchem.0c01579 Serine/threonine-protein kinase 10 3
34463505 10.1021/acs.jmedchem.0c01579 STE20-like serine/threonine-protein kinase 2
34463505 10.1021/acs.jmedchem.0c01579 Unchecked 1

Data from ChEMBL 36 via Core Engine