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Compound Detail

CHEMBL3608512

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Clc1cc(-c2cncc([C@H]3C[C@H]4CC[C@H]3N4)c2)ccn1

Basic Information

ChEMBL ID CHEMBL3608512
Phase Preclinical
Structure Type MOL
InChI Key SDONYPAESJRRLK-RBSFLKMASA-N
3
Targets
4
Activities
2
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

285.8
MW (Da)
3.40
ALogP
3
HBA
1
HBD
37.8
PSA (Ų)
0.86
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C16H16ClN3
MW 285.78
Aromatic Rings 2
Heavy Atoms 20
NP-Likeness 0.28

Activity Summary

IC50 3 meas. best 4.96
Ki 1 meas. best 9.54

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907596
Ki 9.54 9.54 0.3 1
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907596
IC50 4.96 4.96 11000.0 1
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907593
IC50 4.7 4.7 20000.0 1
Neuronal acetylcholine receptor subunit alpha-7
CHEMBL4980
IC50 4.01 4.01 97000.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
26233800 10.1016/j.bmc.2015.07.021 Mus musculus 6
26233800 10.1016/j.bmc.2015.07.021 Neuronal acetylcholine receptor; alpha4/beta2 4
26233800 10.1016/j.bmc.2015.07.021 Neuronal acetylcholine receptor; alpha3/beta4 3
26233800 10.1016/j.bmc.2015.07.021 Neuronal acetylcholine receptor subunit alpha-7 3

Data from ChEMBL 36 via Core Engine