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Compound Detail

CHEMBL3613601

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COC(=O)c1cccc(NC(=O)C2(N)CCN(c3ncnc4[nH]cc(C)c34)CC2)c1

Basic Information

ChEMBL ID CHEMBL3613601
Phase Preclinical
Structure Type MOL
InChI Key LBMPEUDJKWLTOC-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

408.5
MW (Da)
1.99
ALogP
7
HBA
3
HBD
126.2
PSA (Ų)
0.56
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C21H24N6O3
MW 408.46
Aromatic Rings 3
Heavy Atoms 30
NP-Likeness -0.92

Activity Summary

IC50 4 meas. best 8.13

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
LIM domain kinase 2
CHEMBL5932
IC50 8.13 8.13 7.4 1
LIM domain kinase 1
CHEMBL3836
IC50 7.75 7.75 18.0 1
cAMP-dependent protein kinase (PKA)
CHEMBL2094138
IC50 7.09 7.09 81.0 1
Rho-associated protein kinase 2
CHEMBL2973
IC50 7.0 7.0 100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26233434 10.1016/j.bmcl.2015.07.009 LIM domain kinase 2 1
26233434 10.1016/j.bmcl.2015.07.009 LIM domain kinase 1 1
26233434 10.1016/j.bmcl.2015.07.009 Rho-associated protein kinase 2 1
26233434 10.1016/j.bmcl.2015.07.009 cAMP-dependent protein kinase (PKA) 1

Data from ChEMBL 36 via Core Engine