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Compound Detail

CHEMBL1200916

THIORIDAZINE HYDROCHLORIDE
💊 Approved Drug
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💊 Approved Drug
CSc1ccc2c(c1)N(CCC1CCCCN1C)c1ccccc1S2.Cl
ChEMBL ↗ Properties Compare Identifier

Basic Information

ChEMBL ID CHEMBL1200916
Name THIORIDAZINE HYDROCHLORIDE
Phase Approved
Structure Type MOL
InChI Key NZFNXWQNBYZDAQ-UHFFFAOYSA-N
Therapeutic ✓ Yes
Parent Compound CHEMBL479
Active Moiety CHEMBL479

Known Names

Mellaril NSC-186060 Thioridazine hcl Thioridazine hydrochloride Thioridazine hydrochloride intensol
2
Targets
14
Activities
2
Assay Types
0
PK Parameters
17
Publications
5
Known Names
3
Mechanisms

Molecular Properties

370.6
MW (Da)
5.89
ALogP
4
HBA
0
HBD
6.5
PSA (Ų)
0.62
QED
1
Ro5 Violations
4
Rot. Bonds

Drug Information

Molecule Type Small molecule
First Approval 1962
Availability Prescription
Chirality Racemic

Routes of Administration

Oral

Flags

Black Box Warning Withdrawn

Extended Properties

Molecular Formula C21H27ClN2S2
MW 407.05
Aromatic Rings 2
Heavy Atoms 25
NP-Likeness -1.03

Mechanism of Action

Mechanism Action Type Target Direct Efficacy
Serotonin 2a (5-HT2a) receptor antagonist ANTAGONIST 5-hydroxytryptamine receptor 2A ✓ ✓
Serotonin 2c (5-HT2c) receptor antagonist ANTAGONIST 5-hydroxytryptamine receptor 2C ✓ ✓
D2-like dopamine receptor antagonist ANTAGONIST D2-like dopamine receptor ✓ ✓

Drug Warnings

Withdrawn
cardiotoxicity
Cardiac arrythmias
Country: Worldwide   Year: 2005
Black Box Warning
cardiotoxicity
Country: United States
Black Box Warning
infectious disease
Country: United States

Activity Summary

IC50 9 meas. best 5.4
EC50 5 meas. best 5.46

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Unchecked
CHEMBL612545
 EC50 5.46 5.084 3430.0 5
Plasmodium falciparum
CHEMBL364
 IC50 5.4 5.1571 3981.1 7
Unchecked
CHEMBL612545
 IC50 4.43 4.28 37220.0 2

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Unchecked EC50 = 3430.0 nM 5.46 PUBCHEM_BIOASSAY: Fluorescent HTS Cytotoxicity/Cell viability assay (HPDE-C7K ce... -
Plasmodium falciparum IC50 = 3981.07 nM 5.4 Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 5011.87 nM 5.3 Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 5011.87 nM 5.3 Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR gr... 19734910
Plasmodium falciparum IC50 = 7943.28 nM 5.1 Antiplasmodial activity against Plasmodium falciparum 3D7 after 72 hrs by SYBR g... 19734910
Plasmodium falciparum IC50 = 7943.28 nM 5.1 Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR g... 19734910
Unchecked EC50 = 8180.0 nM 5.09 PUBCHEM_BIOASSAY: Fluorescent HTS Cytotoxicity/Cell viability assay (HPDE-C7 cel... -
Unchecked EC50 = 9281.0 nM 5.03 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Plasmodium falciparum IC50 = 10000.0 nM 5.0 Antiplasmodial activity against Plasmodium falciparum D10 after 72 hrs by SYBR g... 19734910
Unchecked EC50 = 11113.0 nM 4.95 PUBCHEM_BIOASSAY: High Throughput Screen to Identify Compounds that Suppress the... -
Plasmodium falciparum IC50 = 12589.25 nM 4.9 Antiplasmodial activity against Plasmodium falciparum Dd2 after 72 hrs by SYBR g... 19734910
Unchecked EC50 = 12980.0 nM 4.89 PUBCHEM_BIOASSAY: A cytotoxicity screen of small molecule inhibitors of the PhoP... -
Unchecked IC50 = 37220.0 nM 4.43 PUBCHEM_BIOASSAY: A counter screen for small molecule screen for inhibitors of t... -
Unchecked IC50 = 74000.0 nM 4.13 PUBCHEM_BIOASSAY: A small molecule screen for inhibitors of the PhoP region in S... -

Literature References

PubMed DOI Target Context # Activities
19734910 10.1038/nchembio.215 Plasmodium falciparum 7
- 10.6019/CHEMBL4808148 Histone deacetylase 6 2
- 10.6019/CHEMBL4495565 SARS-CoV-2 2
23571415 10.1124/mol.112.084152 Solute carrier organic anion transporter family member 1B1 1
19627 10.1021/jm00218a005 Saimiri 1
- 10.1101/2020.04.03.023846 SARS-CoV-2 1
- 10.21203/rs.3.rs-23951/v1 SARS-CoV-2 1
- 10.6019/CHEMBL4495564 Replicase polyprotein 1ab 1
23571415 10.1124/mol.112.084152 Solute carrier organic anion transporter family member 1B3 1
- 10.6019/CHEMBL4513141 Candida albicans 1
- 10.6019/CHEMBL4513141 Cryptococcus neoformans 1
- 10.6019/CHEMBL4513141 Escherichia coli 1
- 10.6019/CHEMBL4513141 Klebsiella pneumoniae 1
- 10.6019/CHEMBL4513141 Pseudomonas aeruginosa 1
- 10.6019/CHEMBL4513141 Acinetobacter baumannii 1
- 10.6019/CHEMBL4513141 Staphylococcus aureus 1
17417631 10.1038/nchembio873 Unchecked 1

Data from ChEMBL 36 via Core Engine