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Compound Detail

CHEMBL540084

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Br.CCOC(=O)Cc1csc(NCc2cc(Br)cc3nc(O)c(O)nc23)n1

Basic Information

ChEMBL ID CHEMBL540084
Phase Preclinical
Structure Type MOL
InChI Key GNHBMWFAQHCGAP-UHFFFAOYSA-N
Parent Compound CHEMBL1190082
Active Moiety CHEMBL1190082
1
Targets
1
Activities
1
Assay Types
0
PK Parameters
2
Publications
0
Known Names

Molecular Properties

439.3
MW (Da)
2.98
ALogP
9
HBA
3
HBD
117.5
PSA (Ų)
0.50
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H16Br2N4O4S
MW 520.20
Aromatic Rings 3
Heavy Atoms 26
NP-Likeness -1.47

Activity Summary

IC50 1 meas. best 9.47

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate NMDA receptor
CHEMBL1907608
IC50 9.47 9.47 0.3 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glutamate NMDA receptor IC50 = 0.34 nM 9.47 Inhibition of [3H]MDL-105,519 binding to NMDA receptor glycine-binding site 9871631

Literature References

PubMed DOI Target Context # Activities
9871631 10.1016/s0960-894x(97)10187-1 Glutamate receptor ionotropic, AMPA 1
9871631 10.1016/s0960-894x(97)10187-1 Glutamate NMDA receptor 1

Data from ChEMBL 36 via Core Engine