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Compound Detail

CHEMBL105762

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C[C@@H]1CC[C@@H](C)N1CCCOc1ccc(-c2ccc(C#N)cc2)cc1

Basic Information

ChEMBL ID CHEMBL105762
Phase Preclinical
Structure Type MOL
InChI Key QJFIAPPKZLXTPP-QZTJIDSGSA-N
4
Targets
4
Activities
1
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

334.5
MW (Da)
4.87
ALogP
3
HBA
0
HBD
36.3
PSA (Ų)
0.71
QED
0
Ro5 Violations
6
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H26N2O
MW 334.46
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.05

Activity Summary

Ki 4 meas. best 9.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Histamine H3 receptor
CHEMBL264
Ki 9.17 9.17 0.7 1
Histamine H3 receptor
CHEMBL4124
Ki 8.19 8.19 6.5 1
Histamine H1 receptor
CHEMBL231
Ki 6.25 6.25 562.3 1
Histamine H2 receptor
CHEMBL1941
Ki 5.04 5.04 9120.1 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12372505 10.1016/s0960-894x(02)00648-0 Histamine H3 receptor 2
12372505 10.1016/s0960-894x(02)00648-0 Histamine H1 receptor 1
12372505 10.1016/s0960-894x(02)00648-0 Histamine H2 receptor 1

Data from ChEMBL 36 via Core Engine