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Compound Detail

CHEMBL394109

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Clc1cc(N2C[C@@H]3CN[C@@H]3C2)cnc1Br

Basic Information

ChEMBL ID CHEMBL394109
Phase Preclinical
Structure Type MOL
InChI Key DCXLOOLLUTVXFT-IMTBSYHQSA-N
3
Targets
6
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

288.6
MW (Da)
1.91
ALogP
3
HBA
1
HBD
28.2
PSA (Ų)
0.80
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H11BrClN3
MW 288.58
Aromatic Rings 1
Heavy Atoms 15
NP-Likeness -0.54

Activity Summary

EC50 4 meas. best 6.41
Ki 2 meas. best 9.7

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
Ki 9.7 9.66 0.2 2
Neuronal acetylcholine receptor; alpha4/beta2
CHEMBL1907589
EC50 6.41 6.405 389.1 2
Neuronal acetylcholine receptor; alpha3/beta4
CHEMBL1907594
EC50 6.23 6.225 588.8 2

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
17929796 10.1021/jm070755h Neuronal acetylcholine receptor; alpha4/beta2 3
17929796 10.1021/jm070755h Neuronal acetylcholine receptor; alpha3/beta4 3
17929796 10.1021/jm070755h Unchecked 2

Data from ChEMBL 36 via Core Engine