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Compound Detail

CHEMBL5180098

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Nc1nc(Nc2ccc(Oc3ccc(C(F)(F)F)cc3)cc2)c2cc[nH]c2n1

Basic Information

ChEMBL ID CHEMBL5180098
Phase Preclinical
Structure Type MOL
InChI Key RHCUPCBYUFBEPI-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

385.4
MW (Da)
5.09
ALogP
5
HBA
3
HBD
88.8
PSA (Ų)
0.46
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H14F3N5O
MW 385.35
Aromatic Rings 4
Heavy Atoms 28
NP-Likeness -1.05

Activity Summary

IC50 2 meas. best 6.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Tau-tubulin kinase 1
CHEMBL1926492
IC50 6.42 6.42 380.0 1
Tau-tubulin kinase 2
CHEMBL3337327
IC50 5.35 5.35 4490.0 1

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
34978799 10.1021/acs.jmedchem.1c01942 Unchecked 1
34978799 10.1021/acs.jmedchem.1c01942 ADMET 1
34978799 10.1021/acs.jmedchem.1c01942 SH-SY5Y 1

Data from ChEMBL 36 via Core Engine