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Compound Detail

CHEMBL3894175

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CC(C)Oc1ccccc1OCCN1CCC(CNS(=O)(=O)c2cccc3cccnc23)CC1

Basic Information

ChEMBL ID CHEMBL3894175
Phase Preclinical
Structure Type MOL
InChI Key HVOJLKOTYQGALX-UHFFFAOYSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
8
Publications
0
Known Names

Molecular Properties

483.6
MW (Da)
4.09
ALogP
6
HBA
1
HBD
80.8
PSA (Ų)
0.47
QED
0
Ro5 Violations
10
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C26H33N3O4S
MW 483.63
Aromatic Rings 3
Heavy Atoms 34
NP-Likeness -1.56

Activity Summary

EC50 2 meas. best 7.47
Ki 2 meas. best 7.02

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL229
EC50 7.47 7.47 34.1 1
Adrenergic receptor alpha-1
CHEMBL1907610
Ki 7.02 7.02 95.0 1
Alpha-1B adrenergic receptor
CHEMBL232
EC50 6.98 6.98 104.8 1
Adrenergic receptor alpha-2
CHEMBL2093864
Ki 6.02 6.02 947.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
27658792 10.1016/j.bmc.2016.09.017 5-hydroxytryptamine receptor 7 2
27658792 10.1016/j.bmc.2016.09.017 Adrenergic receptor alpha-1 1
27658792 10.1016/j.bmc.2016.09.017 Alpha-1A adrenergic receptor 1
27658792 10.1016/j.bmc.2016.09.017 Unchecked 1
27658792 10.1016/j.bmc.2016.09.017 Adrenergic receptor alpha-2 1
27658792 10.1016/j.bmc.2016.09.017 Alpha-1B adrenergic receptor 1
27658792 10.1016/j.bmc.2016.09.017 ADMET 1
27658792 10.1016/j.bmc.2016.09.017 5-hydroxytryptamine receptor 1A 1

Data from ChEMBL 36 via Core Engine