General
Preferred name
CLOZAPINE
Synonyms
CPD000058365 ()
HF 1854 ()
LX 100-129 ()
HF 1854, LX 100-129 ()
Clozapine hydrochloride ()
Clozapine-d4 ()
Fazaclo ()
Clozapine (Clozaril) ()
Clozapine (versacloz) ()
Clozapine resolution mixture ()
Clozapine (caraco) ()
NSC-757429 ()
HF-1854 ()
Versacloz ()
Fazaclo Odt ()
Zaponex ()
Clozaril ()
Clozapine (udl) ()
Leponex ()
Clozapine (fazaclo) ()
Clozapine (teva) ()
Clozapina ()
Clozapine (ivax) ()
Clozapine (mylan) ()
Clozapine (hydrochloride) ()
Clozapine (CRM) ()
P&D ID
PD001633
CAS
5786-21-0
204395-52-8
2711603-38-0
Tags
available
drug
biased GPCR ligand
Approved by
FDA
First approval
1989
Drug indication
Schizophrenia
Psychosis
Drug Status
approved
withdrawn
Max Phase
4.0
Structure
Probe scores
P&D probe-likeness score
[[ v.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)
DESCRIPTION Clozapine (HF 1854) is an antipsychotic used for the research of schizophrenia. Clozapine has high affinity for a number of neuroreceptors. Clozapine is a potent antagonist of dopamine D2 with a Ki of 75 nM. Clozapine inhibits the muscarinic M1 receptor and serotonin 5HT2A receptor with Kis of 9.5 nM and 4 nM, respectively[1][2][3]. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM)[4].
PRICE 29
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 is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Clozapine is a selective monoaminergic antagonist with high affinity for the 5HT2, dopamine 2, 1 and 2 adrenergic, and H1 histaminergic receptors. (Enamine Bioactive Compounds)
DESCRIPTION Clozapine (HF 1854) is a tricylic dibenzodiazepine, classified as an atypical antipsychotic agent. It binds several types of central nervous system receptors, and displays a unique pharmacological profile. Clozapine is a serotonin antagonist, with strong binding to 5-HT 2A/2C receptor subtype. It also displays strong affinity to several dopaminergic receptors, but shows only weak antagonism at the dopamine D2 receptor, a receptor commonly thought to modulate neuroleptic activity. (TargetMol 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)
Cell lines
2
Organisms
3
Compound Sets
41
Axon Medchem Screening Library
1146
BiasDB
Clozapine
Bioprocess diversity set
BOC Sciences Bioactive Compounds
clozapine-hydrochloride-291582
Cayman Chemical Bioactives
12059
30674
31084
17513
25779
ChEMBL Approved Drugs
CHEMBL42
ChEMBL Drugs
CHEMBL42
Concise Guide to Pharmacology 2017/18
38
Concise Guide to Pharmacology 2019/20
38
Concise Guide to Pharmacology 2021/22
38
Concise Guide to Pharmacology 2023/24
38
CZ-OPENSCREEN Bioactive Library
Drug Repurposing Hub
DrugBank
DB00363
DrugBank Approved Drugs
DB00363
DrugCentral
722
DrugCentral Approved Drugs
722
DrugMAP
DMFC71L
DrugMAP Approved Drugs
DMFC71L
DrugMatrix
Enamine Bioactive Compounds
EBC-00671
Enamine BioReference Compounds
EU-OPENSCREEN Bioactive Compound Library
EOS100602
Guide to Pharmacology
38
LOPAC library
LSP-MoA library (Laboratory of Systems Pharmacology)
CHEMBL42
MedChem Express Bioactive Compound Library
HY-14539
NCATS Inxight Approved Drugs
J60AR2IKIC
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
Clozapine(Clozaril)
TargetMol Bioactive Compound Library
T0455
The Spectrum Collection
Tocris Bioactive Compound Library
0444
Tocriscreen Total
Withdrawn 2.0
w219
ZINC Tool Compounds
ZINC000019796155
External IDs
62
Properties
(calculated by RDKit )
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
Target
D2
M1 mAChR
α2-adrenoceptor
¦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
Pathway
GPCR/G protein
Neuroscience
Neuronal Signaling
Therapeutic Class
Antipsychotic Agents
Source data