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Compound Detail

CHEMBL144768

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COc1cc2nc(N(C)CCCCCCN(C)C(=O)c3ccc(CN4CCSC4)cc3)nc(N)c2cc1OC

Basic Information

ChEMBL ID CHEMBL144768
Phase Preclinical
Structure Type MOL
InChI Key YFEUUISKXLCYAK-UHFFFAOYSA-N
3
Targets
3
Activities
1
Assay Types
0
PK Parameters
4
Publications
0
Known Names

Molecular Properties

552.8
MW (Da)
4.50
ALogP
9
HBA
1
HBD
97.0
PSA (Ų)
0.31
QED
1
Ro5 Violations
13
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C29H40N6O3S
MW 552.75
Aromatic Rings 3
Heavy Atoms 39
NP-Likeness -1.11

Activity Summary

Kd 3 meas. best 8.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1D adrenergic receptor
CHEMBL326
Kd 8.17 8.17 6.8 1
Alpha-1B adrenergic receptor
CHEMBL315
Kd 8.01 8.01 9.8 1
Alpha-1A adrenergic receptor
CHEMBL319
Kd 7.23 7.23 58.9 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
9822553 10.1021/jm9810654 Alpha-1A adrenergic receptor 1
9822553 10.1021/jm9810654 Alpha-1B adrenergic receptor 1
9822553 10.1021/jm9810654 Alpha-1D adrenergic receptor 1
9822553 10.1021/jm9810654 Adrenergic receptor alpha-2 1

Data from ChEMBL 36 via Core Engine