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Compound Detail

CHEMBL1782169

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O=C1Cc2c([nH]c3cc[n+](Cc4ccccc4)cc23)-c2ccccc2N1.[Br-]

Basic Information

ChEMBL ID CHEMBL1782169
Phase Preclinical
Structure Type MOL
InChI Key NDYRLQTTYAQSBB-UHFFFAOYSA-N
Parent Compound CHEMBL1789529
Active Moiety CHEMBL1789529
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
16
Publications
0
Known Names

Molecular Properties

340.4
MW (Da)
3.67
ALogP
1
HBA
2
HBD
48.8
PSA (Ų)
0.54
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H18BrN3O
MW 420.31
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -0.09

Activity Summary

IC50 6 meas. best 6.62

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK9/Cyclin T
CHEMBL5291961
IC50 6.62 6.62 240.0 1
Unchecked
CHEMBL612545
IC50 5.47 5.47 3400.0 1
Cyclin-dependent kinase 1/cyclin B
CHEMBL2094127
IC50 5.24 5.24 5700.0 1
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 5.21 5.21 6200.0 1
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 5.14 5.14 7300.0 1
CDK9/cyclin T1
CHEMBL2111389
IC50 5.13 5.13 7400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20621478 10.1016/j.bmcl.2010.06.024 Unchecked 2
20621478 10.1016/j.bmcl.2010.06.024 Cyclin-dependent kinase 2/cyclin A 1
20621478 10.1016/j.bmcl.2010.06.024 Cyclin-dependent kinase 5/CDK5 activator 1 1
20621478 10.1016/j.bmcl.2010.06.024 CDK9/cyclin T1 1
20621478 10.1016/j.bmcl.2010.06.024 Casein kinase I isoform alpha 1
20621478 10.1016/j.bmcl.2010.06.024 Dual specificity protein kinase CLK1 1
20621478 10.1016/j.bmcl.2010.06.024 Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1
20621478 10.1016/j.bmcl.2010.06.024 Glycogen synthase kinase 3 1
33901899 10.1016/j.ejmech.2021.113445 Cyclin-dependent kinase 1/cyclin B 1
33901899 10.1016/j.ejmech.2021.113445 Cyclin-dependent kinase 2/cyclin A 1
33901899 10.1016/j.ejmech.2021.113445 Unchecked 1
33901899 10.1016/j.ejmech.2021.113445 Casein kinase I 1
33901899 10.1016/j.ejmech.2021.113445 Cyclin-dependent kinase 5/CDK5 activator 1 1
33901899 10.1016/j.ejmech.2021.113445 CDK9/Cyclin T 1
33901899 10.1016/j.ejmech.2021.113445 Dual specificity protein kinase CLK1 1
33901899 10.1016/j.ejmech.2021.113445 Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1

Data from ChEMBL 36 via Core Engine