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Compound Detail

CHEMBL27275

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COc1ccc(-c2[nH]nc3c2C(=O)c2c(NC(=O)Cc4ccc(N)cc4)cccc2-3)cc1

Basic Information

ChEMBL ID CHEMBL27275
Phase Preclinical
Structure Type MOL
InChI Key BHTSYKGIHPKWBB-UHFFFAOYSA-N
3
Targets
5
Activities
1
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

424.5
MW (Da)
4.06
ALogP
5
HBA
3
HBD
110.1
PSA (Ų)
0.37
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C25H20N4O3
MW 424.46
Aromatic Rings 4
Heavy Atoms 32
NP-Likeness -0.74

Activity Summary

IC50 5 meas. best 7.42

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 2/cyclin E
CHEMBL2094126
IC50 7.42 7.42 38.0 2
HCT-116
CHEMBL394
IC50 6.4 6.4 400.0 1
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 6.32 6.32 480.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11311054 10.1021/jm0100032 Cyclin-dependent kinase 4/cyclin D1 1
11311054 10.1021/jm0100032 Cyclin-dependent kinase 2/cyclin E 1
11311054 10.1021/jm0100032 HCT-116 1
11311054 10.1021/jm0100032 AG1523 1
12431050 10.1021/jm020171+ Cyclin-dependent kinase 4/cyclin D1 1
12431050 10.1021/jm020171+ Cyclin-dependent kinase 2/cyclin E 1

Data from ChEMBL 36 via Core Engine