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Compound Detail

CHEMBL1783868

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C=C(C)CNc1ccnc2sc3c(=O)n(-c4ccc(C)cc4)cnc3c12

Basic Information

ChEMBL ID CHEMBL1783868
Phase Preclinical
Structure Type MOL
InChI Key AFKSTFXIAKZKBK-UHFFFAOYSA-N
2
Targets
2
Activities
2
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

362.5
MW (Da)
4.29
ALogP
6
HBA
1
HBD
59.8
PSA (Ų)
0.55
QED
0
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C20H18N4OS
MW 362.46
Aromatic Rings 4
Heavy Atoms 26
NP-Likeness -1.51

Activity Summary

IC50 1 meas. best 7.79
Ki 1 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Metabotropic glutamate receptor 1
CHEMBL4477
Ki 9.7 9.7 0.2 1
Metabotropic glutamate receptor 1
CHEMBL3772
IC50 7.79 7.79 16.4 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
19433355 10.1016/j.bmcl.2009.04.104 Metabotropic glutamate receptor 1 2
19433355 10.1016/j.bmcl.2009.04.104 Metabotropic glutamate receptor 5 1

Data from ChEMBL 36 via Core Engine