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Compound Detail

CHEMBL318738

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C1=C(c2c[nH]c3ncccc23)CCN(CCOc2cccc3c2OCCO3)C1

Basic Information

ChEMBL ID CHEMBL318738
Phase Preclinical
Structure Type MOL
InChI Key KINTWXKYQAVVRH-UHFFFAOYSA-N
4
Targets
5
Activities
2
Assay Types
0
PK Parameters
3
Publications
0
Known Names

Molecular Properties

377.4
MW (Da)
3.50
ALogP
5
HBA
1
HBD
59.6
PSA (Ų)
0.74
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C22H23N3O3
MW 377.44
Aromatic Rings 3
Heavy Atoms 28
NP-Likeness -0.92

Activity Summary

Ki 4 meas. best 7.75
IC50 1 meas. best 6.01

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Sodium-dependent serotonin transporter
CHEMBL313
Ki 7.75 7.75 18.0 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.48 7.48 33.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
Ki 7.36 7.36 43.9 1
Sodium-dependent serotonin transporter
CHEMBL228
Ki 6.56 6.56 276.0 1
5-hydroxytryptamine receptor 1A
CHEMBL214
IC50 6.01 6.01 969.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
11814784 10.1016/s0960-894x(01)00746-6 5-hydroxytryptamine receptor 1A 5
11814784 10.1016/s0960-894x(01)00746-6 Sodium-dependent serotonin transporter 2
11814784 10.1016/s0960-894x(01)00746-6 Adrenergic receptor alpha-1 1

Data from ChEMBL 36 via Core Engine