General
Preferred name
FANAPANEL
Synonyms
ZK 200775 ()
ZK200775 ()
MPQX ()
ZK200775 (hydrate) ()
MPQX (hydrate) ()
ZK-200775 ()
Fanapanel (hydrate) ()
ZK200775 hydrate ()
P&D ID
PD012705
CAS
161605-73-8
1255517-78-2
Tags
available
drug candidate
Drug indication
Coronary artery disease
Drug Status
investigational
Max Phase
2.0
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 Competitive AMPA/kainate antagonist (Tocriscreen Plus)
DESCRIPTION Competitive AMPA/kainate antagonist (Tocriscreen Total)
DESCRIPTION Competitive AMPA/kainate antagonist. In rat cortical membranes, displays high affinity for [3H]-AMPA (Ki = 120 nM) and [3H]-CNQX (Ki = 32 nM) binding sites and low affinity for kainate and NMDA channel-associated binding sites (IC50 values range from 2.5 to 11 μM). Inhibits currents induced by AMPA, kainate and NMDA with IC50 values of 21 nM, 27 nM, and > 1 μM respectively. Displays anxiolytic, anticonvulsant and muscle relaxant activity in vivo. (BOC Sciences Bioactive Compounds)
DESCRIPTION Potent and selective NMDA antagonist; acts at the glycine site (Tocris Bioactive Compound Library)
DESCRIPTION ZK200775 hydrate(Fanapanel; MPQX) is a highly selective AMPA/kainate antagonist with little activity against NMDA; have Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively. (BOC Sciences Bioactive Compounds)
Cell lines
0
Organisms
1
Compound Sets
12
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugMAP
Guide to Pharmacology
MedChem Express Bioactive Compound Library
NPC Screening Collection
ReFrame library
Tocris Bioactive Compound Library
Tocriscreen Plus
Tocriscreen Total
External IDs
31
Properties
(calculated by RDKit )
Molecular Weight
409.07
Hydrogen Bond Acceptors
6
Hydrogen Bond Donors
3
Rotatable Bonds
3
Ring Count
3
Aromatic Ring Count
2
cLogP
0.68
TPSA
124.86
Fraction CSP3
0.43
Chiral centers
0.0
Largest ring
6.0
QED
0.5
Structural alerts
0
No structural alerts detected
Custom attributes
(extracted from source data)
Target Type
Ion Channels
Primary Target
AMPA Receptors
MOA
Antagonist
Kainate receptor antagonist
Pathway
Membrane Transporter/Ion Channel
Neuronal Signaling
Target
iGluR
Source data