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Compound Detail

CHEMBL3797874

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CN(C)C(=O)Oc1cccc(NC(=O)C2(CN)CCN(c3ncnc4[nH]c5c(c34)CCCC5)CC2)c1

Basic Information

ChEMBL ID CHEMBL3797874
Phase Preclinical
Structure Type MOL
InChI Key XSRLKVPNDGGLCH-UHFFFAOYSA-N
2
Targets
5
Activities
1
Assay Types
0
PK Parameters
13
Publications
0
Known Names

Molecular Properties

491.6
MW (Da)
3.08
ALogP
7
HBA
3
HBD
129.5
PSA (Ų)
0.50
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H33N7O3
MW 491.60
Aromatic Rings 3
Heavy Atoms 36
NP-Likeness -1.09

Activity Summary

IC50 5 meas. best 9.15

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
LIM domain kinase 2
CHEMBL5932
IC50 9.15 9.15 0.7 2
LIM domain kinase 1
CHEMBL3836
IC50 7.64 7.64 23.0 3

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1039/C5MD00473J ADMET 2
29908439 10.1016/j.ejmech.2018.06.016 LIM domain kinase 1 2
- 10.1039/C5MD00473J LIM domain kinase 2 1
- 10.1039/C5MD00473J LIM domain kinase 1 1
- 10.1039/C5MD00473J Unchecked 1
- 10.1039/C5MD00473J Rho-associated protein kinase 2 1
- 10.1039/C5MD00473J cAMP-dependent protein kinase catalytic subunit alpha 1
- 10.1039/C5MD00473J Serine/threonine-protein kinase SIK2 1
- 10.1039/C5MD00473J Ribosomal protein S6 kinase alpha-6 1
29908439 10.1016/j.ejmech.2018.06.016 LIM domain kinase 2 1
29908439 10.1016/j.ejmech.2018.06.016 Rho-associated protein kinase 2 1
29908439 10.1016/j.ejmech.2018.06.016 Unchecked 1
29908439 10.1016/j.ejmech.2018.06.016 cAMP-dependent protein kinase (PKA) 1

Data from ChEMBL 36 via Core Engine