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Compound Detail

CHEMBL4581793

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N#Cc1ccccc1Nc1nc2ccc(-c3ccc(NC(=O)Cc4ccccc4)cc3)cn2n1

Basic Information

ChEMBL ID CHEMBL4581793
Phase Preclinical
Structure Type MOL
InChI Key RPGJGJRXGBZPLW-UHFFFAOYSA-N
2
Targets
4
Activities
1
Assay Types
1
PK Parameters
5
Publications
0
Known Names

Molecular Properties

444.5
MW (Da)
5.19
ALogP
6
HBA
2
HBD
95.1
PSA (Ų)
0.38
QED
1
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H20N6O
MW 444.50
Aromatic Rings 5
Heavy Atoms 34
NP-Likeness -1.77

Activity Summary

IC50 4 meas. best 9.0

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity protein kinase TTK
CHEMBL3983
IC50 9.0 8.6667 1.0 3
HeLa
CHEMBL399
IC50 6.16 6.16 695.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 12.0 % Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32338514 10.1021/acs.jmedchem.9b02035 ADMET 4
32338514 10.1021/acs.jmedchem.9b02035 Dual specificity protein kinase TTK 2
31121430 10.1016/j.ejmech.2019.04.047 Dual specificity protein kinase TTK 1
32338514 10.1021/acs.jmedchem.9b02035 HeLa 1
38095579 10.1021/acs.jmedchem.3c00963 Dual specificity protein kinase TTK 1

Data from ChEMBL 36 via Core Engine