General
Preferred name
CLOZAPINE
Synonyms
CPD000058365 ()
HF 1854 ()
LX 100-129 ()
Clozapine hydrochloride ()
HF 1854, LX 100-129 ()
Clozapine-d4 ()
Clozapine (hydrochloride) ()
Clozapine (CRM) ()
Zaponex ()
Clozaril ()
Clozapine (Clozaril) ()
Clozapine (ivax) ()
Fazaclo Odt ()
Clozapine (fazaclo) ()
Clozapine (teva) ()
Clozapine (udl) ()
Clozapine (mylan) ()
Leponex ()
Clozapine resolution mixture ()
Clozapine (versacloz) ()
Clozapine (caraco) ()
HF-1854 ()
Versacloz ()
NSC-757429 ()
P&D ID
PD001633
CAS
5786-21-0
204395-52-8
2711603-38-0
Tags
drug
biased GPCR ligand
natural product
available
Approved by
FDA
First approval
1989
Drug indication
Antipsychotic
Schizophrenia
Drug Status
approved
withdrawn
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
Note that PubChem CID 2818 has different double bond structure on the central heptane ring which results in a different InChIKey. Our structure is an exact match for the chemical structure in the INN record for this compound.
The major active metabolite of clozapine is . (GtoPdb)
The major active metabolite of clozapine is . (GtoPdb)
DESCRIPTION
Atypical neuroleptic agent which display greater affinity for the D4 dopamine receptors over D2 or D3
(LOPAC library)
DESCRIPTION
Dopamine antagonist with some D4 selectivity. Also 5-HT2A/2C antagonist
(Tocriscreen Total)
DESCRIPTION
5-HT1 agonist; also has high affinity for 5-ht5a and 5-HT7
(Tocris Bioactive Compound Library)
DESCRIPTION
Clozapine (HF 1854) is an antipsychotic used to treat schizophrenia. Clozapine is a potent antagonist of dopamine and a number of other receptors. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor. Clozapine is a partial agonist of the serotonin (5-HT) receptor subtype 5-HT1A. It also binds to the 5-HT2A, 5-HT2C, 5-HT3, 5-HT6, and 5-HT7 receptors, as well as the histamine H1 and α1-adrenergic receptors.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
2
Organisms
3
Compound Sets
40
Axon Medchem Screening Library
BiasDB
Bioprocess diversity set
BOC Sciences Bioactive Compounds
ChEMBL Approved Drugs
ChEMBL Drugs
Concise Guide to Pharmacology 2017/18
Concise Guide to Pharmacology 2019/20
Concise Guide to Pharmacology 2021/22
Concise Guide to Pharmacology 2023/24
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP
DrugMAP Approved Drugs
DrugMatrix
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
Guide to Pharmacology
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
MedChem Express Bioactive Compound Library
NCATS Inxight Approved Drugs
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Other bioactive compounds
Prestwick Chemical Library
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
The Spectrum Collection
Tocris Bioactive Compound Library
Tocriscreen Total
Withdrawn 2.0
ZINC Tool Compounds
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
57
Molecular Weight
326.13
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
0
Ring Count
4
Aromatic Ring Count
2
cLogP
3.72
TPSA
30.87
Fraction CSP3
0.28
Chiral centers
0.0
Largest ring
7.0
QED
0.8
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Selectivity
D4 > D2,D3
Biological process
Vesicle traffic
Pathway
GPCR/G protein
Neuroscience
Neuronal Signaling
Target
M1 mAChR
??2-adrenoceptor
D2
¦Á2-adrenoceptor
ADRA1A, ADRA1B, ADRA1D, ADRA2A, ADRA2B, ADRA2C, CALY, CHRM1, CHRM2, CHRM3, CHRM4, CHRM5, DRD1, DRD2, DRD3, DRD4, DRD5, HRH1, HRH4, HTR1A, HTR1B, HTR1D, HTR1E, HTR1F, HTR2A, HTR2B, HTR2C, HTR3A, HTR5A, HTR6, HTR7
Atypical antipsychotic
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
mAChR
Primary Target
Non-selective Dopamine
MOA
AChR antagonist
Adrenergic Receptor agonist
Antagonist
Dopamine D4 Antagonists
5-HT2 Antagonists
ADRA1B gene inhibitor
dopamine receptor antagonist, serotonin receptor antagonist
Member status
member
Indication
schizophrenia
ATC
N05AH02
Toxicity type
hematological
Therapeutic Class
Antipsychotic Agents
Source data
