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Compound Detail

CHEMBL53904

ZUCLOPENTHIXOL
🧪 Phase III
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🧪 Phase III
OCCN1CCN(CC/C=C2/c3ccccc3Sc3ccc(Cl)cc32)CC1

Basic Information

ChEMBL ID CHEMBL53904
Name ZUCLOPENTHIXOL
Phase Phase III
Structure Type MOL
InChI Key WFPIAZLQTJBIFN-DVZOWYKESA-N

Known Names

Clopenthixol cis(z)-form Clopixol Zoclopenthixol Zuclopenthixol Zuclopentixol
2
Targets
2
Activities
2
Assay Types
1
PK Parameters
20
Publications
5
Known Names
5
Indications

Molecular Properties

401.0
MW (Da)
4.24
ALogP
4
HBA
1
HBD
26.7
PSA (Ų)
0.69
QED
0
Ro5 Violations
5
Rot. Bonds

Drug Information

Molecule Type Small molecule
Chirality Single Enantiomer

Flags

Natural Product

Extended Properties

Molecular Formula C22H25ClN2OS
MW 400.98
Aromatic Rings 2
Heavy Atoms 27
NP-Likeness -0.72

Indications

Anxiety Dementia Depressive Disorder Psychotic Disorders Schizophrenia

ATC Classification

N05AF05
zuclopenthixol
Level 1: NERVOUS SYSTEM
Level 2: PSYCHOLEPTICS

Activity Summary

IC50 1 meas. best 5.47
Ki 1 meas. best 6.77

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
5-hydroxytryptamine receptor 6
CHEMBL3371
Ki 6.77 6.77 169.0 1
Histone deacetylase 6
CHEMBL1865
IC50 5.47 5.47 3377.0 1

Pharmacokinetic Data

Parameter Value Units Species
F 79.0 % Homo sapiens

Activity Data Samples

Top measurements by pChEMBL value

Literature References

PubMed DOI Target Context # Activities
15646539 10.1016/s0399-8320(04)95062-2 Unchecked 11
15646539 10.1016/s0399-8320(04)95062-2 NON-PROTEIN TARGET 8
- 10.6019/CHEMBL4651402 SARS-CoV-2 6
- 10.6019/CHEMBL4808148 Histone deacetylase 6 4
37468498 10.1038/s41467-023-40064-9 Alpha-2A adrenergic receptor 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2A 3
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 2B 3
37468498 10.1038/s41467-023-40064-9 Mu-type opioid receptor 2
37468498 10.1038/s41467-023-40064-9 Muscarinic acetylcholine receptor M2 2
37468498 10.1038/s41467-023-40064-9 Gamma-aminobutyric acid receptor subunit alpha-1 2
37468498 10.1038/s41467-023-40064-9 Progesterone receptor 2
37468498 10.1038/s41467-023-40064-9 5-hydroxytryptamine receptor 1A 2
- 10.6019/CHEMBL4651402 Vero C1008 2
9599232 10.1021/jm970786k MCF7-DOX 2
10891117 10.1021/jm0000564 ADMET 2
10891117 10.1021/jm0000564 No relevant target 2
37468498 10.1038/s41467-023-40064-9 Voltage-dependent L-type calcium channel subunit alpha-1C 1
37468498 10.1038/s41467-023-40064-9 Glutamate receptor ionotropic, NMDA 1 1
37468498 10.1038/s41467-023-40064-9 Voltage-gated inwardly rectifying potassium channel KCNH2 1
38318365 10.1016/j.isci.2024.108907 Deoxynucleoside triphosphate triphosphohydrolase SAMHD1 1

Data from ChEMBL 36 via Core Engine