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Compound Detail

CHEMBL5555123

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COc1ccccc1-c1cccc(NC(=O)N2CC=C(c3ncnc4[nH]cc(C5CC5)c34)CC2)c1

Basic Information

ChEMBL ID CHEMBL5555123
Phase Preclinical
Structure Type MOL
InChI Key RNWWENPLWXLLTK-UHFFFAOYSA-N
3
Targets
3
Activities
2
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

465.6
MW (Da)
5.83
ALogP
4
HBA
2
HBD
83.1
PSA (Ų)
0.39
QED
1
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C28H27N5O2
MW 465.56
Aromatic Rings 4
Heavy Atoms 35
NP-Likeness -0.91

Activity Summary

Ki 2 meas. best 8.15
EC50 1 meas. best 4.85

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
LIM domain kinase 2
CHEMBL5932
Ki 8.15 8.15 7.0 1
LIM domain kinase 1
CHEMBL3836
Ki 7.68 7.68 21.0 1
HeLa
CHEMBL399
EC50 4.85 4.85 14000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38669909 10.1016/j.ejmech.2024.116391 LIM domain kinase 1 1
38669909 10.1016/j.ejmech.2024.116391 LIM domain kinase 2 1
38669909 10.1016/j.ejmech.2024.116391 Rho-associated protein kinase 1 1
38669909 10.1016/j.ejmech.2024.116391 Rho-associated protein kinase 2 1
38669909 10.1016/j.ejmech.2024.116391 HeLa 1
38669909 10.1016/j.ejmech.2024.116391 Fibroblast 1
38669909 10.1016/j.ejmech.2024.116391 Unchecked 1

Data from ChEMBL 36 via Core Engine