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Compound Detail

CHEMBL5567330

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COc1ccc2c(c1)N(CCN(C)C)/C(=C/C(C)=O)S2.O=C(O)/C=C/C(=O)O

Basic Information

ChEMBL ID CHEMBL5567330
Phase Preclinical
Structure Type MOL
InChI Key SDNZQQUMVZIGGM-XAYIRVKOSA-N
Parent Compound CHEMBL6070285
Active Moiety CHEMBL6070285
3
Targets
6
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

292.4
MW (Da)
2.60
ALogP
5
HBA
0
HBD
32.8
PSA (Ų)
0.78
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H24N2O6S
MW 408.48
Aromatic Rings 1
Heavy Atoms 20
NP-Likeness -0.94

Activity Summary

IC50 4 meas. best 6.25
Ki 2 meas. best 6.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Dual specificity tyrosine-phosphorylation-regulated kinase 1A
CHEMBL2292
IC50 6.25 6.25 561.0 1
5-hydroxytryptamine receptor 2C
CHEMBL225
Ki 6.02 6.02 955.0 2
5-hydroxytryptamine receptor 2C
CHEMBL225
IC50 5.26 5.26 5495.4 2
5-hydroxytryptamine receptor 2A
CHEMBL224
IC50 4.36 4.36 43651.6 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
38648167 10.1021/acs.jmedchem.3c01696 5-hydroxytryptamine receptor 2A 5
38648167 10.1021/acs.jmedchem.3c01696 5-hydroxytryptamine receptor 2C 5
38648167 10.1021/acs.jmedchem.3c01696 Cortical neurone 2
38648167 10.1021/acs.jmedchem.3c01696 Dual specificity tyrosine-phosphorylation-regulated kinase 1A 1
38648167 10.1021/acs.jmedchem.3c01696 Microtubule-associated protein tau 1

Data from ChEMBL 36 via Core Engine