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Compound Detail

CHEMBL1645351

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COCCN([11CH3])Cc1ccc2nc3sc(C(=O)N(C)C4CCCCC4)cn3c2c1

Basic Information

ChEMBL ID CHEMBL1645351
Phase Preclinical
Structure Type MOL
InChI Key AQINBUDFKZIGCN-BJUDXGSMSA-N
Parent Compound CHEMBL2068815
Active Moiety CHEMBL2068815
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
1
Publications
0
Known Names

Molecular Properties

414.6
MW (Da)
4.03
ALogP
6
HBA
0
HBD
50.1
PSA (Ų)
0.59
QED
0
Ro5 Violations
7
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H30N4O2S
MW 413.58
Aromatic Rings 3
Heavy Atoms 29
NP-Likeness -1.82

Activity Summary

Ki 1 meas. best 8.32

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 1
CHEMBL3772
Ki 8.32 8.32 4.8 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Metabotropic glutamate receptor 1 Ki = 4.8 nM 8.32 Binding affinity to mGluR1 21172734

Literature References

PubMed DOI Target Context # Activities
21172734 10.1016/j.bmc.2010.11.048 Metabotropic glutamate receptor 1 1

Data from ChEMBL 36 via Core Engine