General
Preferred name
CLOBENPROPIT
Synonyms
Clobenpropit dihydrobromide ()
Clobenpropit (dihydrobromide) ()
Clobenpropit (hydrobromide) ()
P&D ID
PD003045
CAS
145231-35-2
145231-45-4
Tags
available
drug candidate
biased GPCR ligand
Drug indication
Discovery agent
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
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR[1]. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and ¦Á2A/¦Á2C adrenoceptors (Ki 17.4/7.8 nM)[2]. Clobenpropit dihydrobromide increases apoptosis[3].
PRICE
147
DESCRIPTION
Clobenpropit (dihydrobromide) is a highly potent H3 receptor antagonist and H4 receptor partial agonist.
(GtoPdb)
DESCRIPTION
Highly selective non-peptide delta agonist
(Tocris Bioactive Compound Library)
DESCRIPTION
Highly potent H3 antagonist and H4 partial agonist
(Tocriscreen Total)
DESCRIPTION
Clobenpropit dihydrobromide is a potent antagonist and inverse agonist of histamine H3R (histamine H3LR,pEC50 of 8.07)
(TargetMol Bioactive Compound Library)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
18
Axon Medchem Screening Library
BiasDB
Cayman Chemical Bioactives
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
DrugMAP
DrugMatrix
Guide to Pharmacology
Ki Database
MedChem Express Bioactive Compound Library
NIH Clinical Collections (NCC)
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
Tocriscreen Total
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
46
Molecular Weight
308.09
Hydrogen Bond Acceptors
3
Hydrogen Bond Donors
3
Rotatable Bonds
6
Ring Count
2
Aromatic Ring Count
2
cLogP
3.45
TPSA
64.56
Fraction CSP3
0.29
Chiral centers
0.0
Largest ring
6.0
QED
0.43
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Pathway
Apoptosis
GPCR/G protein
Immunology/Inflammation
Neuroscience
Neuronal Signaling
Primary Target
Histamine H3 Receptors
MOA
Antagonist
Histamine Receptor antagonist
Target
HRH1, HRH2, HRH3, HRH4
H3 antagonist
Histamine Receptor
H3 receptor
Source data
