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Compound Detail

CHEMBL4126912

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N#Cc1ccc2[nH]cc(CCN3CCN(c4cccc5nc6c(c(N)c45)CCCC6)CC3)c2c1

Basic Information

ChEMBL ID CHEMBL4126912
Phase Preclinical
Structure Type MOL
InChI Key KLYMURSGAZXARA-UHFFFAOYSA-N
2
Targets
2
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

450.6
MW (Da)
4.41
ALogP
5
HBA
2
HBD
85.0
PSA (Ų)
0.48
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 C28H30N6
MW 450.59
Aromatic Rings 4
Heavy Atoms 34
NP-Likeness -1.16

Activity Summary

IC50 2 meas. best 5.95

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Butyrylcholinesterase
CHEMBL3403
IC50 5.95 5.95 1130.0 1
Acetylcholinesterase
CHEMBL3199
IC50 5.68 5.68 2100.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
29729987 10.1016/j.bmc.2018.04.037 5-hydroxytryptamine receptor 1A 1
29729987 10.1016/j.bmc.2018.04.037 Acetylcholinesterase 1
29729987 10.1016/j.bmc.2018.04.037 Butyrylcholinesterase 1
29729987 10.1016/j.bmc.2018.04.037 No relevant target 1

Data from ChEMBL 36 via Core Engine