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Compound Detail

CHEMBL9121

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N=C(NCCO)c1ccc(N2CCCN(c3ccc(/C(N)=N/CCO)cc3)CC2)cc1

Basic Information

ChEMBL ID CHEMBL9121
Phase Preclinical
Structure Type MOL
InChI Key DADMNFYLPGROKK-UHFFFAOYSA-N
1
Targets
2
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

424.6
MW (Da)
1.01
ALogP
6
HBA
5
HBD
121.2
PSA (Ų)
0.32
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C23H32N6O2
MW 424.55
Aromatic Rings 2
Heavy Atoms 31
NP-Likeness -0.65

Activity Summary

IC50 2 meas. best 5.03

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Glutamate NMDA receptor
CHEMBL1907608
IC50 5.03 5.03 9440.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Glutamate NMDA receptor IC50 = 9440.0 nM 5.03 Displacement of [3H]-MK-801 from rat cortical membranes NMDA receptor by beta co... 26117647

Literature References

PubMed DOI Target Context # Activities
26117647 10.1016/j.bmc.2015.06.012 Glutamate NMDA receptor 4
12620080 10.1021/jm020375q Trypanosoma brucei 3
11591500 10.1016/s0960-894x(01)00541-8 Pneumocystis carinii 2
11591500 10.1016/s0960-894x(01)00541-8 Nucleic Acid 1
11591500 10.1016/s0960-894x(01)00541-8 Unchecked 1
12620080 10.1021/jm020375q Calf thymus DNA 1
12620080 10.1021/jm020375q Nucleic Acid 1

Data from ChEMBL 36 via Core Engine