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Compound Detail

CHEMBL126087

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O=C1NC(=O)c2c1c1c3ccccc3[nH]c1c1c2c2ccccc2n1CCCO

Basic Information

ChEMBL ID CHEMBL126087
Phase Preclinical
Structure Type MOL
InChI Key LHYCLKRBIKAHMK-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

383.4
MW (Da)
3.70
ALogP
4
HBA
3
HBD
87.1
PSA (Ų)
0.42
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 C23H17N3O3
MW 383.41
Aromatic Rings 5
Heavy Atoms 29
NP-Likeness 0.08

Activity Summary

IC50 4 meas. best 7.16

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 7.16 7.16 70.0 1
Cyclin-dependent kinase 2/cyclin E
CHEMBL2094126
IC50 6.75 6.75 180.0 1
NCI-H460
CHEMBL396
IC50 5.92 5.92 1200.0 1
HCT-116
CHEMBL394
IC50 5.72 5.72 1890.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14552792 10.1016/s0960-894x(03)00792-3 HCT-116 2
14552792 10.1016/s0960-894x(03)00792-3 NCI-H460 2
14552792 10.1016/s0960-894x(03)00792-3 Cyclin-dependent kinase 4/cyclin D1 1
14552792 10.1016/s0960-894x(03)00792-3 Cyclin-dependent kinase 2/cyclin E 1
14552792 10.1016/s0960-894x(03)00792-3 cAMP-dependent protein kinase (PKA) 1

Data from ChEMBL 36 via Core Engine