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Compound Detail

CHEMBL293898

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Cn1c2ccccc2c2c3c(c4c5ccc(Br)cc5[nH]c4c21)C(=O)NC3=O

Basic Information

ChEMBL ID CHEMBL293898
Phase Preclinical
Structure Type MOL
InChI Key SFQZZXBCKCLFFC-UHFFFAOYSA-N
4
Targets
7
Activities
1
Assay Types
0
PK Parameters
14
Publications
0
Known Names

Molecular Properties

418.2
MW (Da)
4.61
ALogP
3
HBA
2
HBD
66.9
PSA (Ų)
0.36
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 C21H12BrN3O2
MW 418.25
Aromatic Rings 5
Heavy Atoms 27
NP-Likeness 0.14

Activity Summary

IC50 7 meas. best 7.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cyclin-dependent kinase 4/cyclin D1
CHEMBL1907601
IC50 7.13 7.045 74.0 2
CaM kinase II
CHEMBL2097164
IC50 6.76 6.76 174.0 1
NCI-H460
CHEMBL396
IC50 5.91 5.91 1230.0 2
HCT-116
CHEMBL394
IC50 5.63 5.63 2360.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
14552792 10.1016/s0960-894x(03)00792-3 Cyclin-dependent kinase 4 3
14552792 10.1016/s0960-894x(03)00792-3 HCT-116 2
14552792 10.1016/s0960-894x(03)00792-3 NCI-H460 2
12747775 10.1021/jm0256169 Cyclin-dependent kinase 4 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
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