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Compound Detail

CHEMBL5193906

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CC1(N)CCN(Cc2ccn3ncnc(Nc4cc(O)cc(Br)c4)c23)CC1

Basic Information

ChEMBL ID CHEMBL5193906
Phase Preclinical
Structure Type MOL
InChI Key DBMRETDBROLHGL-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

431.3
MW (Da)
3.25
ALogP
7
HBA
3
HBD
91.7
PSA (Ų)
0.59
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H23BrN6O
MW 431.34
Aromatic Rings 3
Heavy Atoms 27
NP-Likeness -0.80

Activity Summary

IC50 5 meas. best 8.8

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tau-tubulin kinase 2
CHEMBL3337327
IC50 8.8 7.785 1.6 2
Tau-tubulin kinase 1
CHEMBL1926492
IC50 8.57 7.03 2.7 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
34978799 10.1021/acs.jmedchem.1c01942 Tau-tubulin kinase 1 1
34978799 10.1021/acs.jmedchem.1c01942 Tau-tubulin kinase 2 1
33944571 10.1021/acs.jmedchem.1c00382 Tau-tubulin kinase 1 1
38759454 10.1016/j.ejmech.2024.116496 Tau-tubulin kinase 1 1
38759454 10.1016/j.ejmech.2024.116496 Tau-tubulin kinase 2 1

Data from ChEMBL 36 via Core Engine