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Compound Detail

CHEMBL4640148

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COc1ccccc1Nc1nc2ccc(-c3ccc(NC(=O)Cc4ccccc4)cc3)cn2n1

Basic Information

ChEMBL ID CHEMBL4640148
Phase Preclinical
Structure Type MOL
InChI Key DAKDAHXOZZPTEN-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
1
PK Parameters
3
Publications
0
Known Names

Molecular Properties

449.5
MW (Da)
5.33
ALogP
6
HBA
2
HBD
80.5
PSA (Ų)
0.35
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C27H23N5O2
MW 449.51
Aromatic Rings 5
Heavy Atoms 34
NP-Likeness -1.48

Activity Summary

IC50 2 meas. best 7.26

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity protein kinase TTK
CHEMBL3983
IC50 7.26 7.26 55.0 1
HeLa
CHEMBL399
IC50 5.64 5.64 2300.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 9.0 % 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 1
32338514 10.1021/acs.jmedchem.9b02035 HeLa 1

Data from ChEMBL 36 via Core Engine