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Compound Detail

CHEMBL61790

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O=C1NC(=O)c2c1c1c3ccccc3[nH]c1c1[nH]c3cc(C(F)(F)F)ccc3c21

Basic Information

ChEMBL ID CHEMBL61790
Phase Preclinical
Structure Type MOL
InChI Key WMGQBOOUMYHZOR-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

393.3
MW (Da)
4.86
ALogP
2
HBA
3
HBD
77.8
PSA (Ų)
0.33
QED
0
Ro5 Violations
0
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H10F3N3O2
MW 393.32
Aromatic Rings 5
Heavy Atoms 29
NP-Likeness -0.18

Activity Summary

IC50 3 meas. best 5.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 5.95 5.95 1135.0 1
NCI-H460
CHEMBL396
IC50 5.87 5.87 1350.0 1
HCT-116
CHEMBL394
IC50 5.78 5.78 1650.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12747775 10.1021/jm0256169 Cyclin-dependent kinase 4 2
12747775 10.1021/jm0256169 Cyclin-dependent kinase 4/cyclin D1 1
12747775 10.1021/jm0256169 Cyclin-dependent kinase 2/cyclin E 1
12747775 10.1021/jm0256169 CaM kinase II 1
12747775 10.1021/jm0256169 cAMP-dependent protein kinase (PKA) 1
12747775 10.1021/jm0256169 HCT-116 1
12747775 10.1021/jm0256169 NCI-H460 1
12747775 10.1021/jm0256169 Glycogen synthase kinase-3 beta 1

Data from ChEMBL 36 via Core Engine