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Compound Detail

CHEMBL130213

6,7-DICHLORO-3-HYDROXY-2-QUINOXALINECARBOXYLIC ACID
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O=C(O)c1nc2cc(Cl)c(Cl)cc2nc1O

Basic Information

ChEMBL ID CHEMBL130213
Name 6,7-DICHLORO-3-HYDROXY-2-QUINOXALINECARBOXYLIC ACID
Phase Preclinical
Structure Type MOL
InChI Key LWFDMVFVKWWYFN-UHFFFAOYSA-N
4
Targets
4
Activities
1
Assay Types
6
PK Parameters
8
Publications
0
Known Names

Molecular Properties

259.1
MW (Da)
2.34
ALogP
4
HBA
2
HBD
83.3
PSA (Ų)
0.82
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

Natural Product First in Class Prodrug

Extended Properties

Molecular Formula C9H4Cl2N2O3
MW 259.05
Aromatic Rings 2
Heavy Atoms 16
NP-Likeness -0.82

Activity Summary

IC50 4 meas. best 6.34

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate NMDA receptor
CHEMBL1907608
IC50 6.34 6.34 460.0 1
Glutamate [NMDA] receptor
CHEMBL2094124
IC50 6.34 6.34 460.0 1
Glutamate receptor ionotropic AMPA
CHEMBL2096670
IC50 5.17 5.17 6700.0 1
Glutamate receptor ionotropic kainate
CHEMBL2109241
IC50 4.49 4.49 32600.0 1

Pharmacokinetic Data

Parameter Value Units Species
Fu 0.284 - Rattus norvegicus
Fu 1.0 - Rattus norvegicus
Fu 0.476 - Rattus norvegicus
Fu 0.0414 - Rattus norvegicus
Fu 0.24 - Rattus norvegicus
Fu 0.435 - Rattus norvegicus

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
31732255 10.1016/j.ejmech.2019.111813 ADMET 18
- 10.1016/S0960-894X(00)80095-5 Glutamate [NMDA] receptor 1
- 10.1016/S0960-894X(00)80095-5 Glutamate receptor ionotropic AMPA 1
- 10.1016/S0960-894X(00)80095-5 Glutamate receptor ionotropic kainate 1
- 10.1016/S0960-894X(00)80095-5 No relevant target 1
7990104 10.1021/jm00050a001 Glutamate NMDA receptor 1
23571415 10.1124/mol.112.084152 Solute carrier organic anion transporter family member 1B3 1
23571415 10.1124/mol.112.084152 Solute carrier organic anion transporter family member 1B1 1

Data from ChEMBL 36 via Core Engine