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Compound Detail

CHEMBL4637246

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COc1cc2c3c(c1O)-c1cc(N)ccc1CC3N(C)CC2

Basic Information

ChEMBL ID CHEMBL4637246
Phase Preclinical
Structure Type MOL
InChI Key LVGQSPSRQGIUSM-UHFFFAOYSA-N
4
Targets
7
Activities
1
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

296.4
MW (Da)
2.74
ALogP
4
HBA
2
HBD
58.7
PSA (Ų)
0.79
QED
0
Ro5 Violations
1
Rot. Bonds

Drug Information

Molecule Type Unknown
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C18H20N2O2
MW 296.37
Aromatic Rings 2
Heavy Atoms 22
NP-Likeness 1.43

Activity Summary

Ki 7 meas. best 6.64

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
D(2) dopamine receptor
CHEMBL217
Ki 6.64 6.64 231.0 2
D(1A) dopamine receptor
CHEMBL2056
Ki 6.52 6.52 301.0 2
D(1B) dopamine receptor
CHEMBL1850
Ki 6.38 6.38 418.0 2
5-hydroxytryptamine receptor 2A
CHEMBL224
Ki 6.07 6.07 850.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
32107165 10.1016/j.bmcl.2020.127053 D(1B) dopamine receptor 1
32107165 10.1016/j.bmcl.2020.127053 D(2) dopamine receptor 1
32107165 10.1016/j.bmcl.2020.127053 D(1A) dopamine receptor 1
32107165 10.1016/j.bmcl.2020.127053 5-hydroxytryptamine receptor 2A 1
32107165 10.1016/j.bmcl.2020.127053 5-hydroxytryptamine receptor 1A 1
39038276 10.1021/acs.jmedchem.4c00537 D(1B) dopamine receptor 1
39038276 10.1021/acs.jmedchem.4c00537 D(1A) dopamine receptor 1
39038276 10.1021/acs.jmedchem.4c00537 D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine