General
Preferred name
JNJ-39758979
Synonyms
JNJ 39758979 dihydrochloride ()
JNJ-39758979 dihydrochloride ()
JNJ-39758979, (-)- ()
JNJ39758979 ()
Jnj 39758979 ()
JNJ_39758979 ()
JNJ 39758979 ()
P&D ID
PD050062
CAS
1046447-90-8
1620648-30-7
Tags
available
free of charge
probe
drug candidate
Drug Status
investigational
Max Phase
2.0
Drug indication
Asthma
Probe info
Probe type
P&D approved
experimental probe
Probe selectivity
protein-selective
Probe targets
[[ compound.targets[t].gene_name ]]
Probe control
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
DESCRIPTION
JNJ-39758979 is a selective histamine H4 receptor antagonist with anti-inflammatory potential.
(GtoPdb)
DESCRIPTION
JNJ-39758979 is a selective, orally active, and high-affinity histamine H4 receptor antagonist with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 shows good anti-inflammatory and antipruritic activity[1][2].
PRICE
149
MOA
Antagonist
(Chemical Probes.org)
DESCRIPTION
JNJ-39758979 is a selective and high-affinity histamine H4 receptor antagonist (Kis: 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively). JNJ-39758979 functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells.
(TargetMol Bioactive Compound Library)
DESCRIPTION
GPR171 antagonist
(Tocris Bioactive Compound Library)
DESCRIPTION
JNJ-39758979 is a potent and selective histamine H4 antagonist (Ki = 12.5 nM) with >80-fold selectivity for H4 over other histamine receptors. It was shown to inhibit histamine-induced pruritus in healthy subjects.
(BOC Sciences Bioactive Compounds)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Compound Sets
19
BOC Sciences Bioactive Compounds
Cayman Chemical Bioactives
ChEMBL Drugs
Chemical Probes.org
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
EUbOPEN Chemogenomics Library
Guide to Pharmacology
High-quality chemical probes
MedChem Express Bioactive Compound Library
Open Science Probes
ReFrame library
TargetMol Bioactive Compound Library
Tocris Bioactive Compound Library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
27
Molecular Weight
221.16
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
2
Rotatable Bonds
2
Ring Count
2
Aromatic Ring Count
1
cLogP
0.72
TPSA
81.06
Fraction CSP3
0.64
Chiral centers
1.0
Largest ring
6.0
QED
0.77
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Pathway
GPCR/G protein
Immunology/Inflammation
Neuroscience
Neuronal Signaling
Primary Target
Histamine H4 Receptors
MOA
Antagonist
Histamine Receptor antagonist
Control name
JNJ-39668551
Target
HRH4
H4 receptor
Target class
GPCR
Target subclass
Histamine Receptor
Recommended Cell Concentration
10 uM
Source data

