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Compound Detail

CHEMBL524439

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COc1cc2c(cc1O)C[C@H]1c3c(c(Cl)c(O)c(OC)c3-2)CCN1C

Basic Information

ChEMBL ID CHEMBL524439
Phase Preclinical
Structure Type MOL
InChI Key HRPJZDTZANKXQI-LBPRGKRZSA-N
4
Targets
4
Activities
2
Assay Types
0
PK Parameters
5
Publications
0
Known Names

Molecular Properties

361.8
MW (Da)
3.52
ALogP
5
HBA
2
HBD
62.2
PSA (Ų)
0.86
QED
0
Ro5 Violations
2
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C19H20ClNO4
MW 361.83
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness 1.74

Activity Summary

IC50 2 meas. best 7.09
Ki 2 meas. best 8.65

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Alpha-1A adrenergic receptor
CHEMBL319
Ki 8.65 8.65 2.2 1
D(1A) dopamine receptor
CHEMBL265
IC50 7.09 7.09 81.0 1
Alpha-1B adrenergic receptor
CHEMBL315
Ki 6.57 6.57 269.1 1
D(2) dopamine receptor
CHEMBL339
IC50 6.14 6.14 720.0 1

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
10785418 10.1021/np990433j Unchecked 2
10785418 10.1021/np990433j D(1A) dopamine receptor 1
10785418 10.1021/np990433j D(2) dopamine receptor 1
10785418 10.1021/np990433j Alpha-1A adrenergic receptor 1
10785418 10.1021/np990433j Alpha-1B adrenergic receptor 1

Data from ChEMBL 36 via Core Engine