General
Preferred name
AM251
Synonyms
AM 251 ()
CHEMBL285932 ()
1-(2,4-dichlorophenyl)-5-(4-iodophenyl)-4-methyl-N-(piperidin-1-yl)-1H-pyrazole-3-carboxamide ()
[123I]AM251 ()
AM-251 ()
[123I]AM251 ()
P&D ID
PD003150
CAS
183232-66-8
Tags
drug candidate
natural product
probe
available
Drug indication
Discovery agent
Probe info
Probe selectivity
protein-selective
Probe type
P&D approved
calculated probe
Probe sources
High-quality chemical probes
Tool Compound Set
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Probe control not defined
Orthogonal probes
2
No orthogonal probes found
Similar probes
1
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
AM251 is a CB1 receptor antagonist/inverse agonist. Experiments in rats indicate that AM251 has potential as a prophylactic antidote to the cannabinoid receptor mediated, often life-threatening, side-effects that are an increasingly common cause for concern in individuals taking highly potent synthetic cannabinoids recreationally .
(GtoPdb)
DESCRIPTION
Potent CB1 antagonist. Also GPR55 agonist
(Tocriscreen Total)
DESCRIPTION
AM251 block the inhibitory effects of endocannabinoids and synthetic cannabinoid agonists on transmitter release through an action at presynaptic cannabinoid 1 receptors in brain.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
2
Compound Sets
21
AdooQ Bioactive Compound Library
Axon Medchem Screening Library
BOC Sciences Bioactive Compounds
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
Drug Repurposing Hub
High-quality chemical probes
Ki Database
MedChem Express Bioactive Compound Library
NIH Clinical Collections (NCC)
Novartis Chemogenetic Library (NIBR MoA Box)
ReFrame library
Selleckchem Bioactive Compound Library
TargetMol Bioactive Compound Library
Tocriscreen Total
Tool Compound Set
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
32
Molecular Weight
554.01
Hydrogen Bond Acceptors
4
Hydrogen Bond Donors
1
Rotatable Bonds
4
Ring Count
4
Aromatic Ring Count
3
cLogP
5.89
TPSA
50.16
Fraction CSP3
0.27
Chiral centers
0.0
Largest ring
6.0
QED
0.41
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Target
Cannabinoid CB1 receptor
CB1
GPR55
CNR1, GPR18, GPR55
CB-1 antagonist
Cannabinoid Receptor
Pathway
GPCR/G protein
Endocrinology/Hormones
Neuronal Signaling
Member status
member
MOA
ACAT Inhibitors
Cannabinoid CB1 Inverse Agonists
Cannabinoid Receptor antagonist
Source data
