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Compound Detail

CHEMBL270926

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COc1ccnc2[nH]cc(-c3ccnc(SC)n3)c12

Basic Information

ChEMBL ID CHEMBL270926
Phase Preclinical
Structure Type MOL
InChI Key AJLTWCLIFVXAEJ-UHFFFAOYSA-N
6
Targets
8
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

272.3
MW (Da)
2.75
ALogP
5
HBA
1
HBD
63.7
PSA (Ų)
0.59
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C13H12N4OS
MW 272.33
Aromatic Rings 3
Heavy Atoms 19
NP-Likeness -0.77

Activity Summary

IC50 8 meas. best 6.22

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
IC50 6.22 5.71 600.0 3
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL5508
IC50 6.0 6.0 1000.0 1
CDK9/cyclin T1
CHEMBL2111389
IC50 5.96 5.96 1100.0 1
Cyclin-dependent kinase 2/cyclin A
CHEMBL2094128
IC50 5.68 5.68 2100.0 1
Cyclin-dependent kinase 5/CDK5 activator 1
CHEMBL1907600
IC50 5.64 5.64 2300.0 1
HEK293
CHEMBL614818
IC50 4.18 4.18 66000.0 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