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Compound Detail

CHEMBL1098471

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c1ccc2c(c1)c1ccncc1n2CCCCCCCCCn1c2ccccc2c2ccncc21

Basic Information

ChEMBL ID CHEMBL1098471
Phase Preclinical
Structure Type MOL
InChI Key JJAATQLWMKLMJU-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
11
Publications
0
Known Names

Molecular Properties

460.6
MW (Da)
8.12
ALogP
4
HBA
0
HBD
35.6
PSA (Ų)
0.19
QED
1
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C31H32N4
MW 460.63
Aromatic Rings 6
Heavy Atoms 35
NP-Likeness -0.38

Activity Summary

IC50 2 meas. best 6.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Cholinesterase
CHEMBL5763
IC50 6.54 6.54 288.6 1
Acetylcholinesterase
CHEMBL4078
IC50 6.12 6.12 753.2 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
20361801 10.1021/jm1000024 Glutamate NMDA receptor; GRIN1/GRIN2B 2
20361801 10.1021/jm1000024 Glutamate NMDA receptor; GRIN1/GRIN2A 2
20361801 10.1021/jm1000024 ADMET 2
20361801 10.1021/jm1000024 Cholinesterase 2
20361801 10.1021/jm1000024 Acetylcholinesterase 2
26278660 10.1021/acs.jmedchem.5b00958 Glutamate NMDA receptor; GRIN1/GRIN2A 2
26278660 10.1021/acs.jmedchem.5b00958 Glutamate NMDA receptor; GRIN1/GRIN2B 2
26278660 10.1021/acs.jmedchem.5b00958 Cholinesterase 1
26278660 10.1021/acs.jmedchem.5b00958 Acetylcholinesterase 1
26278660 10.1021/acs.jmedchem.5b00958 Amine oxidase [flavin-containing] A 1
26278660 10.1021/acs.jmedchem.5b00958 Amine oxidase [flavin-containing] B 1

Data from ChEMBL 36 via Core Engine