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Compound Detail

CHEMBL4802050

8RK64
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N#CN1CC[C@H](C(=O)Nc2nc3c(s2)CN(C(=O)CN=[N+]=[N-])CC3)C1

Basic Information

ChEMBL ID CHEMBL4802050
Name 8RK64
Phase Preclinical
Structure Type MOL
InChI Key KIWKRCCIHSGWQS-VIFPVBQESA-N
3
Targets
6
Activities
2
Assay Types
0
PK Parameters
20
Publications
0
Known Names

Molecular Properties

360.4
MW (Da)
1.08
ALogP
7
HBA
1
HBD
138.1
PSA (Ų)
0.37
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug Chemical Probe

Extended Properties

Molecular Formula C14H16N8O2S
MW 360.40
Aromatic Rings 1
Heavy Atoms 25
NP-Likeness -1.96

Activity Summary

IC50 4 meas. best 6.64
Ki 2 meas. best 5.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Ubiquitin carboxyl-terminal hydrolase isozyme L1
CHEMBL6159
IC50 6.64 6.64 230.0 2
Mitogen-activated protein kinase 14
CHEMBL260
IC50 6.5 6.5 320.0 1
Sigma non-opioid intracellular receptor 1
CHEMBL287
Ki 5.47 5.465 3388.4 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.6019/CHEMBL5674860 Colon cancer organoid 12
- 10.6019/CHEMBL5724558 Colon cancer organoid 12
- 10.6019/CHEMBL5608141 Colon cancer organoid 6
- 10.6019/CHEMBL5303304 HEK-293T 5
- 10.1158/2159-8290.CD-23-0050 Colon cancer organoid 5
36149939 10.1021/acs.jmedchem.2c01113 Ubiquitin carboxyl-terminal hydrolase isozyme L1 4
- 10.6019/CHEMBL4800724 Sigma non-opioid intracellular receptor 1 3
- 10.6019/CHEMBL4800724 GABA-A receptor; anion channel 2
- 10.6019/CHEMBL5608109 Hepatocyte spheroids 2
- 10.6019/CHEMBL5303304 U2OS 2
- 10.6019/CHEMBL5303304 Fibroblast 2
- 10.6019/CHEMBL4800724 5-hydroxytryptamine receptor 1D 1
- 10.6019/CHEMBL4800724 Mitogen-activated protein kinase 14 1
- 10.6019/CHEMBL4800724 5-hydroxytryptamine receptor 1A 1
- 10.6019/CHEMBL4800724 Sigma intracellular receptor 2 1
- 10.6019/CHEMBL4800724 5-hydroxytryptamine receptor 2A 1
- 10.6019/CHEMBL4800724 5-hydroxytryptamine receptor 2B 1
- 10.6019/CHEMBL4800724 Alpha-1D adrenergic receptor 1
- 10.6019/CHEMBL4800724 Beta-1 adrenergic receptor 1
- 10.6019/CHEMBL4800724 Ubiquitin carboxyl-terminal hydrolase isozyme L5 1

Data from ChEMBL 36 via Core Engine