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Compound Detail

CHEMBL26677

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COc1cccc(C(=O)CCCN2CCN(c3ccccc3OC)CC2)c1

Basic Information

ChEMBL ID CHEMBL26677
Phase Preclinical
Structure Type MOL
InChI Key XGXUWJSIDSMGFX-UHFFFAOYSA-N
6
Targets
7
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

368.5
MW (Da)
3.49
ALogP
5
HBA
0
HBD
42.0
PSA (Ų)
0.67
QED
0
Ro5 Violations
8
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H28N2O3
MW 368.48
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -1.20

Activity Summary

Ki 5 meas. best 9.11
IC50 2 meas. best 8.51

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 9.11 9.11 0.8 1
D(4) dopamine receptor
CHEMBL219
Ki 8.77 8.77 1.7 1
D(2) dopamine receptor
CHEMBL339
Ki 8.52 8.52 3.0 1
D(4) dopamine receptor
CHEMBL219
IC50 8.51 8.51 3.1 1
D(2) dopamine receptor
CHEMBL217
IC50 7.89 7.89 13.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.72 7.72 19.0 1
5-hydroxytryptamine receptor 7
CHEMBL3223
Ki 6.96 6.96 109.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
- 10.1016/S0960-894X(97)00218-7 Unchecked 2
- 10.1016/S0960-894X(97)00218-7 D(4) dopamine receptor 1
- 10.1016/S0960-894X(97)00218-7 D(2) dopamine receptor 1
- 10.1016/S0960-894X(97)00218-7 Adrenergic receptor alpha-1 1
12570387 10.1021/jm020994z 5-hydroxytryptamine receptor 7 1
12570387 10.1021/jm020994z 5-hydroxytryptamine receptor 1A 1
9822559 10.1021/jm981041x D(4) dopamine receptor 1
9822559 10.1021/jm981041x D(2) dopamine receptor 1

Data from ChEMBL 36 via Core Engine