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Compound Detail

CHEMBL2407901

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COCCOc1ccc2cc1OCC(=O)N(C)CCCN(C)Cc1c[nH]c3ncnc(c13)N2

Basic Information

ChEMBL ID CHEMBL2407901
Phase Preclinical
Structure Type MOL
InChI Key HGGMHYCPDXPSRF-UHFFFAOYSA-N
6
Targets
7
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

454.5
MW (Da)
2.40
ALogP
8
HBA
2
HBD
104.8
PSA (Ų)
0.58
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H30N6O4
MW 454.53
Aromatic Rings 3
Heavy Atoms 33
NP-Likeness -0.16

Activity Summary

IC50 6 meas. best 8.3
Ki 1 meas. best 7.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
HCT-116
CHEMBL394
IC50 8.3 8.3 5.0 1
MDA-MB-231
CHEMBL400
IC50 8.3 8.3 5.0 1
NCI-H1299
CHEMBL612255
IC50 8.3 8.3 5.0 1
A2780
CHEMBL614004
IC50 8.3 8.3 5.0 1
U-87 MG
CHEMBL614247
IC50 8.3 8.3 5.0 1
Serine/threonine-protein kinase PLK4
CHEMBL3788
IC50 7.6 7.6 25.0 1
Serine/threonine-protein kinase PLK4
CHEMBL3788
Ki 7.6 7.6 25.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23829549 10.1021/jm400380m Serine/threonine-protein kinase PLK4 1
38199166 10.1016/j.ejmech.2023.116115 Serine/threonine-protein kinase PLK4 1
38199166 10.1016/j.ejmech.2023.116115 A2780 1
38199166 10.1016/j.ejmech.2023.116115 HCT-116 1
38199166 10.1016/j.ejmech.2023.116115 NCI-H1299 1
38199166 10.1016/j.ejmech.2023.116115 MDA-MB-231 1
38199166 10.1016/j.ejmech.2023.116115 U-87 MG 1

Data from ChEMBL 36 via Core Engine