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Compound Detail

CHEMBL4552106

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CC#Cc1c(Oc2ccc(NC(=O)c3cccn(-c4ccc(F)cc4)c3=O)cc2F)ccnc1N

Basic Information

ChEMBL ID CHEMBL4552106
Phase Preclinical
Structure Type MOL
InChI Key BXJAJCQUQYZMSO-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

472.4
MW (Da)
4.51
ALogP
6
HBA
2
HBD
99.2
PSA (Ų)
0.42
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H18F2N4O3
MW 472.45
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -1.36

Activity Summary

IC50 3 meas. best 7.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Receptor-interacting serine/threonine-protein kinase 3
CHEMBL1795199
IC50 7.8 7.8 16.0 1
Receptor-interacting serine/threonine-protein kinase 1
CHEMBL5464
IC50 6.22 6.22 600.0 1
Receptor-interacting serine/threonine-protein kinase 2
CHEMBL5014
IC50 5.52 5.52 3000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32184955 10.1021/acsmedchemlett.9b00065 Receptor-interacting serine/threonine-protein kinase 3 1
32184955 10.1021/acsmedchemlett.9b00065 Receptor-interacting serine/threonine-protein kinase 2 1
32184955 10.1021/acsmedchemlett.9b00065 Hepatocyte growth factor receptor 1
32184955 10.1021/acsmedchemlett.9b00065 Receptor-interacting serine/threonine-protein kinase 1 1

Data from ChEMBL 36 via Core Engine