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Compound Detail

CHEMBL406102

MERIOLIN 8
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Cn1cc(-c2ccnc(N)n2)c2c(O)ccnc21

Basic Information

ChEMBL ID CHEMBL406102
Name MERIOLIN 8
Phase Preclinical
Structure Type MOL
InChI Key PYDJIICXCHAWOI-UHFFFAOYSA-N
5
Targets
7
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

241.2
MW (Da)
1.32
ALogP
6
HBA
2
HBD
89.8
PSA (Ų)
0.67
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H11N5O
MW 241.25
Aromatic Rings 3
Heavy Atoms 18
NP-Likeness -0.11

Activity Summary

IC50 7 meas. best 5.92

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
CDK9/cyclin T1
CHEMBL2111389
IC50 5.92 5.92 1200.0 1
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL5508
IC50 5.92 5.92 1200.0 1
Unchecked
CHEMBL612545
IC50 5.92 5.6333 1200.0 3
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 5.75 5.75 1800.0 1
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 5.26 5.26 5500.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
18232649 10.1021/jm700940h Unchecked 3
18232649 10.1021/jm700940h Cyclin-dependent kinase 3
18232649 10.1021/jm700940h Cyclin-dependent kinase 2/cyclin A 1
18232649 10.1021/jm700940h Cyclin-dependent kinase 5/CDK5 activator 1 1
18232649 10.1021/jm700940h CDK9/cyclin T1 1
18232649 10.1021/jm700940h Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1
18232649 10.1021/jm700940h SH-SY5Y 1
18232649 10.1021/jm700940h HEK293 1
18232649 10.1021/jm700940h GBM 1
18232649 10.1021/jm700940h KMS-11 1
18232649 10.1021/jm700940h LS174T 1

Data from ChEMBL 36 via Core Engine