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Compound Detail

CHEMBL72661

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Cn1ccc2cc(F)c3c(c4c(c5c6ccccc6n(CCCO)c53)C(=O)NC4=O)c21

Basic Information

ChEMBL ID CHEMBL72661
Phase Preclinical
Structure Type MOL
InChI Key BFHMGFVFUUEXOQ-UHFFFAOYSA-N
3
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

415.4
MW (Da)
3.84
ALogP
5
HBA
2
HBD
76.3
PSA (Ų)
0.44
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C24H18FN3O3
MW 415.42
Aromatic Rings 5
Heavy Atoms 31
NP-Likeness -0.16

Activity Summary

IC50 4 meas. best 6.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 6.46 6.405 346.0 2
HCT-116
CHEMBL394
IC50 5.62 5.62 2390.0 1
NCI-H460
CHEMBL396
IC50 5.61 5.61 2480.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12824014 10.1016/s0960-894x(03)00461-x Cyclin-dependent kinase 4/cyclin D1 2
12824014 10.1016/s0960-894x(03)00461-x Cyclin-dependent kinase 2/cyclin E 1
12824014 10.1016/s0960-894x(03)00461-x cAMP-dependent protein kinase (PKA) 1
12824014 10.1016/s0960-894x(03)00461-x HCT-116 1
12824014 10.1016/s0960-894x(03)00461-x NCI-H460 1

Data from ChEMBL 36 via Core Engine