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Compound Detail

CHEMBL2403090

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NC1CCC(Nc2nc(NCc3ccc(-c4ccccc4)nc3)c3ncn(C4CCCC4)c3n2)CC1

Basic Information

ChEMBL ID CHEMBL2403090
Phase Preclinical
Structure Type MOL
InChI Key HARUFAXNYVLWKF-UHFFFAOYSA-N
7
Targets
8
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

482.6
MW (Da)
5.30
ALogP
8
HBA
3
HBD
106.6
PSA (Ų)
0.33
QED
1
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H34N8
MW 482.64
Aromatic Rings 4
Heavy Atoms 36
NP-Likeness -0.99

Activity Summary

IC50 8 meas. best 7.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2/cyclin E1
CHEMBL1907605
IC50 7.51 7.51 31.0 1
HeLa
CHEMBL399
IC50 6.94 6.94 114.0 1
Cyclin-dependent kinase 1
CHEMBL308
IC50 6.74 6.74 184.0 1
HOS
CHEMBL614736
IC50 6.69 6.69 206.0 1
MCF7
CHEMBL387
IC50 6.32 6.32 483.0 1
HCT-116
CHEMBL394
IC50 6.25 6.25 563.0 1
G-361
CHEMBL614036
IC50 6.05 6.05 895.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
23829517 10.1021/jm4006884 HeLa 1
23829517 10.1021/jm4006884 HCT-116 1
23829517 10.1021/jm4006884 HOS 1
23829517 10.1021/jm4006884 G-361 1
23829517 10.1021/jm4006884 MCF7 1
23829517 10.1021/jm4006884 K562 1
23829517 10.1021/jm4006884 Cyclin-dependent kinase 2/cyclin E1 1
23829517 10.1021/jm4006884 Cyclin-dependent kinase 1 1

Data from ChEMBL 36 via Core Engine