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Compound Detail

CHEMBL268800

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COc1ccc2[nH]c(C)c(CCN)c2c1

Basic Information

ChEMBL ID CHEMBL268800
Phase Preclinical
Structure Type MOL
InChI Key TYAPSMFCSAKSOR-UHFFFAOYSA-N
5
Targets
6
Activities
1
Assay Types
0
PK Parameters
10
Publications
0
Known Names

Molecular Properties

204.3
MW (Da)
1.99
ALogP
2
HBA
2
HBD
51.0
PSA (Ų)
0.80
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C12H16N2O
MW 204.27
Aromatic Rings 2
Heavy Atoms 15
NP-Likeness -0.38

Activity Summary

Ki 6 meas. best 7.1

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 7.1 7.055 80.0 2
5-hydroxytryptamine receptor 2C
CHEMBL324
Ki 6.16 6.16 690.0 1
5-hydroxytryptamine receptor 1B
CHEMBL3459
Ki 6.1 6.1 800.0 1
5-hydroxytryptamine receptor 1D
CHEMBL1983
Ki 5.97 5.97 1060.0 1
5-hydroxytryptamine receptor 1A
CHEMBL273
Ki 5.89 5.89 1300.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
12825922 10.1021/jm030030n 5-hydroxytryptamine receptor 6 1
12825922 10.1021/jm030030n 5-hydroxytryptamine receptor 3A 1
10715164 10.1021/jm990550b 5-hydroxytryptamine receptor 6 1
10715164 10.1021/jm990550b 5-hydroxytryptamine receptor 3A 1
2299641 10.1021/jm00164a046 5-hydroxytryptamine receptor 1A 1
2299641 10.1021/jm00164a046 5-hydroxytryptamine receptor 1B 1
2299641 10.1021/jm00164a046 5-hydroxytryptamine receptor 2C 1
2299641 10.1021/jm00164a046 5-hydroxytryptamine receptor 1D 1
2299641 10.1021/jm00164a046 5-hydroxytryptamine receptor 1E 1
2299641 10.1021/jm00164a046 Serotonin 2 (5-HT2) receptor 1

Data from ChEMBL 36 via Core Engine