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Compound Detail

CHEMBL270346

MERIOLIN 9
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COc1ccnc2c1c(-c1ccnc(N)n1)cn2C

Basic Information

ChEMBL ID CHEMBL270346
Name MERIOLIN 9
Phase Preclinical
Structure Type MOL
InChI Key CPQCGVRZSBLZLT-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
15
Publications
0
Known Names

Molecular Properties

255.3
MW (Da)
1.62
ALogP
6
HBA
1
HBD
78.8
PSA (Ų)
0.75
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 C13H13N5O
MW 255.28
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -0.41

Activity Summary

IC50 2 meas. best 4.6

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 4.6 4.6 25000.0 1
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 4.14 4.14 73000.0 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
27171036 10.1021/acs.jmedchem.6b00150 CDK9/cyclin T1 1
27171036 10.1021/acs.jmedchem.6b00150 Cyclin-dependent kinase 5/CDK5 activator 1 1
27171036 10.1021/acs.jmedchem.6b00150 CDK2/Cyclin A2 1
27171036 10.1021/acs.jmedchem.6b00150 Unchecked 1

Data from ChEMBL 36 via Core Engine