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Compound Detail

CHEMBL226232

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O=C1NCCc2[nH]c(-c3ccnc(Cl)c3)cc21

Basic Information

ChEMBL ID CHEMBL226232
Phase Preclinical
Structure Type MOL
InChI Key JTRXEPCDEVNYPE-UHFFFAOYSA-N
9
Targets
10
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

247.7
MW (Da)
2.02
ALogP
2
HBA
2
HBD
57.8
PSA (Ų)
0.76
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 C12H10ClN3O
MW 247.69
Aromatic Rings 2
Heavy Atoms 17
NP-Likeness -0.60

Activity Summary

Ki 8 meas. best 8.0
IC50 2 meas. best 6.83

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity protein kinase CLK4
CHEMBL4203
Ki 8.0 8.0 10.0 1
Mitogen-activated protein kinase kinase kinase kinase 4
CHEMBL6166
Ki 7.0 7.0 100.0 1
Cell division cycle 7-related protein kinase
CHEMBL5443
Ki 6.9 6.9 125.9 1
Cell division cycle 7-related protein kinase
CHEMBL5443
IC50 6.83 6.83 147.0 1
MAP kinase-activated protein kinase 2
CHEMBL2208
IC50 6.22 6.22 608.0 1
Glycogen synthase kinase-3 beta
CHEMBL262
Ki 6.1 6.1 794.3 1
Homeodomain-interacting protein kinase 2
CHEMBL4576
Ki 5.8 5.8 1584.9 1
Cyclin-dependent kinase 2
CHEMBL301
Ki 5.7 5.7 1995.3 1
Rho-associated protein kinase 2
CHEMBL2973
Ki 5.2 5.2 6309.6 1
Interleukin-1 receptor-associated kinase 4
CHEMBL3778
Ki 5.2 5.2 6309.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17480064 10.1021/jm0611004 MAP kinase-activated protein kinase 2 1
18201066 10.1021/jm700956r Cell division cycle 7-related protein kinase 1

Data from ChEMBL 36 via Core Engine