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Compound Detail

CHEMBL1946122

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OC1(c2ccc(Cl)cc2)C[C@H]2CC[C@@H](C1)N2CCCOc1ccc(F)cc1

Basic Information

ChEMBL ID CHEMBL1946122
Phase Preclinical
Structure Type MOL
InChI Key AWIYLVWAILOVMX-RLAPIPATSA-N
6
Targets
6
Activities
1
Assay Types
0
PK Parameters
7
Publications
0
Known Names

Molecular Properties

389.9
MW (Da)
4.76
ALogP
3
HBA
1
HBD
32.7
PSA (Ų)
0.72
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 C22H25ClFNO2
MW 389.90
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.86

Activity Summary

Ki 6 meas. best 8.39

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(3) dopamine receptor
CHEMBL234
Ki 8.39 8.39 4.1 1
D(2) dopamine receptor
CHEMBL217
Ki 7.66 7.66 22.0 1
D(4) dopamine receptor
CHEMBL3361
Ki 7.31 7.31 49.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 6.91 6.91 123.0 1
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.63 6.63 236.0 1
Histamine H1 receptor
CHEMBL231
Ki 5.38 5.38 4149.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
22336245 10.1016/j.bmc.2012.01.022 5-hydroxytryptamine receptor 1A 1
22336245 10.1016/j.bmc.2012.01.022 5-hydroxytryptamine receptor 2A 1
22336245 10.1016/j.bmc.2012.01.022 D(2) dopamine receptor 1
22336245 10.1016/j.bmc.2012.01.022 D(3) dopamine receptor 1
22336245 10.1016/j.bmc.2012.01.022 D(4) dopamine receptor 1
22336245 10.1016/j.bmc.2012.01.022 5-hydroxytryptamine receptor 2C 1
22336245 10.1016/j.bmc.2012.01.022 Histamine H1 receptor 1

Data from ChEMBL 36 via Core Engine