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Compound Detail

CHEMBL4557026

ERKi-NC
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C[C@H](NC(=O)Nc1cc2[nH]ncc2c(CO)n1)c1ccccn1

Basic Information

ChEMBL ID CHEMBL4557026
Name ERKi-NC
Phase Preclinical
Structure Type MOL
InChI Key XACXTPQNHGFQOD-VIFPVBQESA-N
2
Targets
5
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

312.3
MW (Da)
1.73
ALogP
5
HBA
4
HBD
115.8
PSA (Ų)
0.59
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C15H16N6O2
MW 312.33
Aromatic Rings 3
Heavy Atoms 23
NP-Likeness -1.93

Activity Summary

Ki 3 meas. best 6.27
IC50 2 meas. best 5.75

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 2B
CHEMBL1833
Ki 6.27 6.27 537.0 3
Mitogen-activated protein kinase 1
CHEMBL4040
IC50 5.75 5.75 1780.0 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL4507286 Tyrosine-protein kinase ABL1 15
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL4507286 Epidermal growth factor receptor 12
- 10.6019/CHEMBL4507286 Receptor-type tyrosine-protein kinase FLT3 11
- 10.6019/CHEMBL4689842 U2OS 10
- 10.6019/CHEMBL4507286 Phosphatidylinositol 4,5-bisphosphate 3-kinase catalytic subunit alpha isoform 10
- 10.6019/CHEMBL4689842 Fibroblast 9
- 10.6019/CHEMBL4507286 Mast/stem cell growth factor receptor Kit 9
- 10.6019/CHEMBL4507286 Unchecked 8
- 10.6019/CHEMBL5724696 U2OS 8
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
- 10.6019/CHEMBL4689842 HEK-293T 5
- 10.6019/CHEMBL4507286 Proto-oncogene tyrosine-protein kinase receptor Ret 4
- 10.6019/CHEMBL4507286 Mitogen-activated protein kinase 1 4
- 10.6019/CHEMBL4507286 Hepatocyte growth factor receptor 3
- 10.6019/CHEMBL4507286 5-hydroxytryptamine receptor 2B 3
- 10.6019/CHEMBL4507286 ALK tyrosine kinase receptor 3
- 10.6019/CHEMBL4507286 Ribosomal protein S6 kinase alpha-4 2

Data from ChEMBL 36 via Core Engine