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Compound Detail

CHEMBL213713

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COc1cc(F)c(F)c(F)c1C(=O)c1cnc(NC2CCN(S(C)(=O)=O)CC2)nc1N

Basic Information

ChEMBL ID CHEMBL213713
Phase Preclinical
Structure Type MOL
InChI Key AAOLDQJTTACKSD-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

459.4
MW (Da)
1.55
ALogP
8
HBA
2
HBD
127.5
PSA (Ų)
0.49
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H20F3N5O4S
MW 459.45
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -1.54

Activity Summary

Ki 3 meas. best 9.0
IC50 1 meas. best 6.66

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
Ki 9.0 9.0 1.0 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 8.7 8.7 2.0 1
Cyclin-dependent kinase 1
CHEMBL308
Ki 8.3 8.3 5.0 1
HCT-116
CHEMBL394
IC50 6.66 6.66 220.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17064073 10.1021/jm0606138 Cyclin-dependent kinase 4/cyclin D1 1
17064073 10.1021/jm0606138 Cyclin-dependent kinase 1 1
17064073 10.1021/jm0606138 Cyclin-dependent kinase 2 1
17064073 10.1021/jm0606138 HCT-116 1

Data from ChEMBL 36 via Core Engine